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Pages
- Title
- Intermediates for tricyclic or tetracyclic taxanes.
- Creator
-
Holton, Robert A., Somoza, Carmen, Shindo, Mitsuru, Biediger, Ronald J., Boatman, P. Douglas, Smith, Chase C., Liang, Feng, Murthi, Krishna K., Kim, Hyeong Baik
- Abstract/Description
-
The synthesis of taxol and other tricyclic and tetracyclic taxanes.
- Date Issued
- 2001-08-21
- Identifier
- FSU_uspto_6278026, 6278026, 711524, 09/333382, 600b83161da1122888348587dc18798c
- Format
- Citation
- Title
- Method for the synthesis of taxanes.
- Creator
-
Holton, Robert A., Vu, Phong H., Gharbaoui, Tawfik, Reboul, Vincent
- Abstract/Description
-
A process for the preparation of a compound having the formula: the process comprising treating a compound having the formula: with an alkyl metal species or with a Lewis acid in the presence of a tertiary amine base, wherein P2 is hydrogen or a hydroxyl protecting group.
- Date Issued
- 2002-08-27
- Identifier
- FSU_uspto_6441253, 6441253, 711524, 09/617555, 600b83161da1122888348587dc18798c
- Format
- Citation
- Title
- Method for the synthesis of a taxane intermediate.
- Creator
-
Holton, Robert A., Vu, Phong H., Gharbaoui, Tawfik, Reboul, Vincent
- Abstract/Description
-
A process for the preparation of a compound having the formula: ##STR1## in which a compound having the formula: ##STR2## is treated with a base and a silylating agent.
- Date Issued
- 2000-08-29
- Identifier
- FSU_uspto_6111144, 6111144, 711524, 09/136827, 600b83161da1122888348587dc18798c
- Format
- Citation
- Title
- Metal alkoxide taxane and &bgr;-lactam compounds.
- Creator
-
Holton, Robert A.
- Abstract/Description
-
A process for preparing N-acyl, N-sulfonyl and N-phosphoryl substituted isoserine esters in which a metal alkoxide is reacted with a &bgr;-lactam.
- Date Issued
- 2002-11-12
- Identifier
- FSU_uspto_6479678, 6479678, 711524, 09/517791, 600b83161da1122888348587dc18798c
- Format
- Citation
- Title
- Metal alkoxides.
- Creator
-
Holton, Robert A.
- Abstract/Description
-
A metal alkoxide having the following formula: ##STR1## wherein T.sub.1 is hydrogen or a hydroxy protecting group, Z is --OT.sub.2, or --OCOCH.sub.3, T.sub.2 is hydrogen or a hydroxy protecting group, and M is selected from the group comprising Group IA, IIA and transition metals are useful in the preparation of biologically active derivatives of baccatin III and 10-deacetyl baccatin III.
- Date Issued
- 1993-12-28
- Identifier
- FSU_uspto_5274124, 5274124, 711524, 07/949066, 600b83161da1122888348587dc18798c
- Format
- Citation
- Title
- Metal alkoxide compounds.
- Creator
-
Holton, Robert A.
- Abstract/Description
-
A process for preparing N-acyl, N-sulfonyl and N-phosphoryl substituted isoserine esters in which a metal alkoxide is reacted with a .beta.-lactam.
- Date Issued
- 1998-03-03
- Identifier
- FSU_uspto_5723634, 5723634, 711524, 08/483309, 600b83161da1122888348587dc18798c
- Format
- Citation
- Title
- Metal alkoxide taxane derivatives.
- Creator
-
Holton, Robert A.
- Abstract/Description
-
A process for preparing N-acyl, N-sulfonyl and N-phosphoryl substituted isoserine esters in which a metal alkoxide is reached with a β-lactam.
- Date Issued
- 2006-07-11
- Identifier
- FSU_uspto_7074945, 7074945, 711524, 10/673897, 600b83161da1122888348587dc18798c
- Format
- Citation
- Title
- Oxazinone compounds for the preparation of taxol.
- Creator
-
Holton, Robert A.
- Abstract/Description
-
Process for the preparation of a taxol intermediate comprising contacting an alcohol with an oxazinone having the formula: ##STR1## wherein R.sub.1 is aryl, heteroaryl, alkyl, alkenyl, alkynyl or OR.sub.7 wherein R.sub.7 is alkyl, alkenyl, alkynyl, aryl or heteroaryl; R.sub.2 and R.sub.5 are independently selected from hydrogen, alkyl alkenyl, alkynyl, aryl, heteroaryl, and OR.sub.8 wherein R.sub.8 is alkyl, alkenyl, alkynyl, aryl, heteroaryl, or hydroxyl protecting group; and R.sub.3 and R...
Show moreProcess for the preparation of a taxol intermediate comprising contacting an alcohol with an oxazinone having the formula: ##STR1## wherein R.sub.1 is aryl, heteroaryl, alkyl, alkenyl, alkynyl or OR.sub.7 wherein R.sub.7 is alkyl, alkenyl, alkynyl, aryl or heteroaryl; R.sub.2 and R.sub.5 are independently selected from hydrogen, alkyl alkenyl, alkynyl, aryl, heteroaryl, and OR.sub.8 wherein R.sub.8 is alkyl, alkenyl, alkynyl, aryl, heteroaryl, or hydroxyl protecting group; and R.sub.3 and R.sub.6 are independently selected from hydrogen, alkyl, alkenyl, alkynyl, aryl and heteroaryl.
Show less - Date Issued
- 1995-01-24
- Identifier
- FSU_uspto_5384399, 5384399, 711524, 07/898438, 600b83161da1122888348587dc18798c
- Format
- Citation
- Title
- 1-deoxy taxol analogs.
- Creator
-
Holton, Robert A., Somoza, Carmen, Liang, Feng, Tang, Suhan
- Abstract/Description
-
1-Deoxybaccatin III, 1-deoxytaxol and 1-deoxy taxol analogs and method for the preparation thereof.
- Date Issued
- 2006-03-28
- Identifier
- FSU_uspto_7019150, 7019150, 711524, 10/636017, 600b83161da1122888348587dc18798c
- Format
- Citation
- Title
- 10-desacetoxytaxol derivatives.
- Creator
-
Farina, Vittorio, Holton, Robert A., Chen, Shu-Hui
- Abstract/Description
-
The present invention relates to 10-desacetoxytaxol and derivatives thereof, which are useful as antitumor agents. These compounds have the formula ##STR1## wherein R.sub.2 is hydrogen, hydroxy or a protected hydroxy group; R.sub.3 and R.sub.4 are independently hydrogen, hydroxy, a protected hydroxy group, methyl, --SH, --NH.sub.2, or --NR.sub.8 R.sub.9 ; R.sub.5 is R.sub.10, or --OR.sub.10 ; R.sub.6 and R.sub.7 are independently hydrogen, alkyl, or aryl; R.sub.8 and R.sub.9 are independently...
Show moreThe present invention relates to 10-desacetoxytaxol and derivatives thereof, which are useful as antitumor agents. These compounds have the formula ##STR1## wherein R.sub.2 is hydrogen, hydroxy or a protected hydroxy group; R.sub.3 and R.sub.4 are independently hydrogen, hydroxy, a protected hydroxy group, methyl, --SH, --NH.sub.2, or --NR.sub.8 R.sub.9 ; R.sub.5 is R.sub.10, or --OR.sub.10 ; R.sub.6 and R.sub.7 are independently hydrogen, alkyl, or aryl; R.sub.8 and R.sub.9 are independently hydrogen, alkyl, alkenyl, alkynyl, or aryl; and R.sub.10 is alkoxy, alkyl, alkenyl, alkynl, or aryl.
Show less - Date Issued
- 1994-09-27
- Identifier
- FSU_uspto_5350866, 5350866, 691280, 07/949449, 600b83161da1122888348587dc18798c
- Format
- Citation
- Title
- 1-deoxy baccatin III, 1-deoxy taxol and 1-deoxy taxol analogs and method for the preparation thereof.
- Creator
-
Holton, Robert A., Somoza, Carmen, Liang, Feng, Tang, Suhan
- Abstract/Description
-
1-Deoxybaccatin III, 1-deoxytaxol and 1-deoxy taxol analogs and method for the preparation thereof.
- Date Issued
- 2003-04-08
- Identifier
- FSU_uspto_6545168, 6545168, 711524, 08/850942, 600b83161da1122888348587dc18798c
- Format
- Citation
- Title
- .beta.-lactams used in preparing taxol.
- Creator
-
Holton, Robert A.
- Abstract/Description
-
A .beta.-lactam of the formula: ##STR1## wherein R.sub.1 is aryl, substituted aryl, alkyl, alkenyl, or alkynyl; R.sub.2 is hydrogen, alkyl, acyl, acetal, ethoxyethyl, or other hydroxyl protecting group; and R.sub.3 is aryl, substituted aryl, alkyl, alkenyl, or alkynyl; and the enantiomers and diastereomers thereof.
- Date Issued
- 1996-11-12
- Identifier
- FSU_uspto_5574156, 5574156, 711524, 08/254561, 600b83161da1122888348587dc18798c
- Format
- Citation
- Title
- β-lactam synthesis.
- Creator
-
Holton, Robert A., Vu, Phong H.
- Abstract/Description
-
The present invention is directed to a process for the preparation of β-lactams. Generally, an imine is cyclocondensed with a ketene acetal or enolate to form the β-lactam product in a “one pot” synthesis, this process is generally performed at a higher temperature than conventional processes.
- Date Issued
- 2009-06-02
- Identifier
- FSU_uspto_7541458, 7541458, 711524, 11/449462, 6c9256d97d167832cbab694dc904bd27
- Format
- Citation
- Title
- .beta.-lactams as taxol intermediates N-acylated.
- Creator
-
Holton, Robert A.
- Abstract/Description
-
.beta.-lactam compounds which are reacted with a metal alkoxide for preparing N-acyl, N-sulfonyl and phosphoryl substituted isoserine esters.
- Date Issued
- 1996-07-23
- Identifier
- FSU_uspto_5539103, 5539103, 711524, 08/351532, 600b83161da1122888348587dc18798c
- Format
- Citation
- Title
- C7 taxane derivatives and pharmaceutical compositions containing them.
- Creator
-
Holton, Robert A., Chai, Ki-byung
- Abstract/Description
-
Taxane derivatives having alternative C7 substituents.
- Date Issued
- 1998-02-24
- Identifier
- FSU_uspto_5721268, 5721268, 711524, 08/462123, 600b83161da1122888348587dc18798c
- Format
- Citation
- Title
- C2 taxane derivaties and pharmaceutical compositions containing them.
- Creator
-
Holton, Robert A., Tao, Chunlin
- Abstract/Description
-
Taxane derivatives having alternative C2 substituents.
- Date Issued
- 1998-03-17
- Identifier
- FSU_uspto_5728725, 5728725, 711524, 08/462124, 600b83161da1122888348587dc18798c
- Format
- Citation
- Title
- C2 substituted phenyl taxane derivatives and pharmaceutical compositions containing them.
- Creator
-
Holton, Robert A., Tao, Chunlin
- Abstract/Description
-
Taxane derivatives having alternative C2 substituents.
- Date Issued
- 2002-01-15
- Identifier
- FSU_uspto_6339164, 6339164, 711524, 09/465035, 600b83161da1122888348587dc18798c
- Format
- Citation
- Title
- Furyl or thienyl carbonyl substituted taxanes and pharmaceutical compositions containing them.
- Creator
-
Holton, Robert A., Nadizadeh, Hossain, Rengan, Kasthuri
- Abstract/Description
-
Taxane derivatives of the formula ##STR1## wherein R.sub.1 is phenyl or p-nitrophenyl, PA1 R.sub.3 is furyl or thienyl, PA1 T.sub.1 is hydrogen, hydroxyl protecting group, or --COT.sub.2, PA1 T.sub.2 is H, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl or monocylic aryl, PA1 Ac is acetyl, and PA1 E.sub.1 and E.sub.2 are independently selected from hydrogen and functional groups which increase the water solubility of the taxane derivative are useful as antitumor...
Show moreTaxane derivatives of the formula ##STR1## wherein R.sub.1 is phenyl or p-nitrophenyl, PA1 R.sub.3 is furyl or thienyl, PA1 T.sub.1 is hydrogen, hydroxyl protecting group, or --COT.sub.2, PA1 T.sub.2 is H, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl or monocylic aryl, PA1 Ac is acetyl, and PA1 E.sub.1 and E.sub.2 are independently selected from hydrogen and functional groups which increase the water solubility of the taxane derivative are useful as antitumor agents.
Show less - Date Issued
- 1994-02-01
- Identifier
- FSU_uspto_5283253, 5283253, 711524, 07/975723, 600b83161da1122888348587dc18798c
- Format
- Citation
- Title
- Furyl and thienyl substituted taxanes and pharmaceutical compositions containing them.
- Creator
-
Holton, Robert A., Nadizadeh, Hossain, Beidiger, Ronald J.
- Abstract/Description
-
A taxane derivative of the formula ##STR1## wherein ##STR2## Z is --OT.sub.1, T.sub.1 is hydrogen, hydroxyl protecting group, or --COT.sub.2, PA0 T.sub.2 is H, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkenyl, C.sub.1 -C.sub.6 alkynyl or monocylic aryl, PA0 R.sub.3 is benzoyl, substituted benzoyl or C.sub.1 -C.sub.6 alkoxycarbonyl, PA0 Ac is acetyl, and PA0 E.sub.1 and E.sub.2 are independently selected from hydrogen and functional groups which increase the water solubility of the taxane...
Show moreA taxane derivative of the formula ##STR1## wherein ##STR2## Z is --OT.sub.1, T.sub.1 is hydrogen, hydroxyl protecting group, or --COT.sub.2, PA0 T.sub.2 is H, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkenyl, C.sub.1 -C.sub.6 alkynyl or monocylic aryl, PA0 R.sub.3 is benzoyl, substituted benzoyl or C.sub.1 -C.sub.6 alkoxycarbonyl, PA0 Ac is acetyl, and PA0 E.sub.1 and E.sub.2 are independently selected from hydrogen and functional groups which increase the water solubility of the taxane derivative are useful as antitumor agents.
Show less - Date Issued
- 1993-07-13
- Identifier
- FSU_uspto_5227400, 5227400, 711524, 07/862819, 600b83161da1122888348587dc18798c
- Format
- Citation
- Title
- Heteroaryl substituted oxazinone compounds for the preparation of taxol.
- Creator
-
Holton, Robert A.
- Abstract/Description
-
Process for the preparation of a taxol intermediate comprising contacting an alcohol with an oxazinone having the formula: ##STR1## wherein R.sub.1 is aryl, heteroaryl, alkyl, alkenyl, alkynyl or OR.sub.7 wherein R.sub.7 is alkyl, alkenyl, alkynyl, aryl or heteroaryl; R.sub.2 and R.sub.5 are independently selected from hydrogen, alkyl alkenyl, alkynyl, aryl, heteroaryl, and OR.sub.8 wherein R.sub.8 is alkyl, alkenyl, alkynyl, aryl, heteroaryl, or hydroxyl protecting group; and R.sub.3 and R...
Show moreProcess for the preparation of a taxol intermediate comprising contacting an alcohol with an oxazinone having the formula: ##STR1## wherein R.sub.1 is aryl, heteroaryl, alkyl, alkenyl, alkynyl or OR.sub.7 wherein R.sub.7 is alkyl, alkenyl, alkynyl, aryl or heteroaryl; R.sub.2 and R.sub.5 are independently selected from hydrogen, alkyl alkenyl, alkynyl, aryl, heteroaryl, and OR.sub.8 wherein R.sub.8 is alkyl, alkenyl, alkynyl, aryl, heteroaryl, or hydroxyl protecting group; and R.sub.3 and R.sub.6 are independently selected from hydrogen, alkyl, alkenyl, alkynyl, aryl and heteroaryl.
Show less - Date Issued
- 1996-07-02
- Identifier
- FSU_uspto_5532363, 5532363, 711524, 08/335495, 600b83161da1122888348587dc18798c
- Format
- Citation
- Title
- Method for preparation of taxol using an oxazinone.
- Creator
-
Holton, Robert A.
- Abstract/Description
-
Process for the preparation of a taxol intermediate comprising contacting an alcohol with an oxazinone having the formula: ##STR1## wherein R.sub.1 is aryl, substituted aryl, alkyl, alkenyl, or alkynyl; R.sub.2 is hydrogen, ethoxyethyl, 2,2,2-trichloroethoxymethyl or other hydroxyl protecting group; and R.sub.3 is aryl, substituted aryl, alkyl, alkenyl, or alkynyl; the contacting of said alcohol and oxazinone being carried out in the presence of a sufficient amount of an activating agent...
Show moreProcess for the preparation of a taxol intermediate comprising contacting an alcohol with an oxazinone having the formula: ##STR1## wherein R.sub.1 is aryl, substituted aryl, alkyl, alkenyl, or alkynyl; R.sub.2 is hydrogen, ethoxyethyl, 2,2,2-trichloroethoxymethyl or other hydroxyl protecting group; and R.sub.3 is aryl, substituted aryl, alkyl, alkenyl, or alkynyl; the contacting of said alcohol and oxazinone being carried out in the presence of a sufficient amount of an activating agent under effective conditions to cause the oxazinone to react with the alcohol to form a .beta.-amido ester which is suitable for use as an intermediate in the synthesis of taxol.
Show less - Date Issued
- 1991-05-14
- Identifier
- FSU_uspto_5015744, 5015744, 711524, 07/436235, 600b83161da1122888348587dc18798c
- Format
- Citation
- Title
- Method for preparation of taxol using .beta.-lactam.
- Creator
-
Holton, Robert A.
- Abstract/Description
-
A .beta.-lactam of the formula: ##STR1## wherein R.sub.1 is aryl, substituted aryl, alkyl, alkenyl, or alkynyl; R.sub.2 is hydrogen, alkyl, acyl, acetal, ethoxyethyl, or other hydroxyl protecting group; and R.sub.3 is aryl, substituted aryl, alkyl, alkenyl, or alkynyl; and process for the preparation of taxol comprising contacting said .beta.-lactam and an alcohol in the presence of an activating agent to provide a taxol intermediate, and converting the intermediate to taxol.
- Date Issued
- 1992-12-29
- Identifier
- FSU_uspto_5175315, 5175315, 711524, 07/415028, 600b83161da1122888348587dc18798c
- Format
- Citation
- Title
- Method for preparation of taxol using an oxazinone.
- Creator
-
Holton, Robert A.
- Abstract/Description
-
Process for the preparation of a taxol intermediate comprising contacting an alcohol with an oxazinone having the formula: ##STR1## wherein R.sub.1 is aryl, heteroaryl, alkyl, alkenyl, alkynyl or OR.sub.7 wherein R.sub.7 is alkyl, alkenyl, alkynyl, aryl or heteroaryl; R.sub.2 and R.sub.5 are independently selected from hydrogen, alkyl alkenyl, alkynyl, aryl, heteroaryl, and OR.sub.8 wherein R.sub.8 is alkyl, alkenyl, alkynyl, aryl, heteroaryl, or hydroxyl protecting group; and R.sub.3 and R...
Show moreProcess for the preparation of a taxol intermediate comprising contacting an alcohol with an oxazinone having the formula: ##STR1## wherein R.sub.1 is aryl, heteroaryl, alkyl, alkenyl, alkynyl or OR.sub.7 wherein R.sub.7 is alkyl, alkenyl, alkynyl, aryl or heteroaryl; R.sub.2 and R.sub.5 are independently selected from hydrogen, alkyl alkenyl, alkynyl, aryl, heteroaryl, and OR.sub.8 wherein R.sub.8 is alkyl, alkenyl, alkynyl, aryl, heteroaryl, or hydroxyl protecting group; and R.sub.3 and R.sub.6 are independently selected from hydrogen, alkyl, alkenyl, alkynyl, aryl and heteroaryl.
Show less - Date Issued
- 1992-08-04
- Identifier
- FSU_uspto_5136060, 5136060, 711524, 07/603041, 600b83161da1122888348587dc18798c
- Format
- Citation
- Title
- Method for preparation of taxol.
- Creator
-
Holton, Robert A.
- Abstract/Description
-
A .beta.-lactam of the formula: ##STR1## wherein R.sub.1 is aryl, substituted aryl, alkyl, alkenyl, or alkynyl; R.sub.2 is hydrogen, alkyl, acyl, acetal, ethoxyethyl, or other hydroxyl protecting group; and R.sub.3 is aryl, substituted aryl, alkyl, alkenyl, or alkynyl; and process for the preparation of taxol comprising contacting said .beta.-lactam and an alcohol in the presence of an activating agent to provide a taxol intermediate, and converting the intermediate to taxol.
- Date Issued
- 1994-08-09
- Identifier
- FSU_uspto_5336785, 5336785, 711524, 07/968003, 600b83161da1122888348587dc18798c
- Format
- Citation
- Title
- Method for the preparation of 1-deoxy baccatin III, 1-deoxy taxol and 1-deoxy taxol analogs.
- Creator
-
Holton, Robert A., Somoza, Carmen, Liang, Feng, Tang, Suhan
- Abstract/Description
-
1-Deoxybaccatin III, 1-deoxytaxol and 1-deoxy taxol analogs and method for the preparation thereof.
- Date Issued
- 2003-09-16
- Identifier
- FSU_uspto_6620950, 6620950, 711524, 10/236798, 600b83161da1122888348587dc18798c
- Format
- Citation
- Title
- Processes for the production of polycyclic fused ring compounds.
- Creator
-
Holton, Robert A., Vu, Phong H.
- Abstract/Description
-
The present invention provides processes for the production of polycyclic fused ring compounds. The polycyclic fused ring compounds are produced by protecting a polycyclic fused ring polyol with a bridging silicon-based protecting group and attaching a suitable side chain. Polycyclic fused ring compounds and intermediate compounds are also described.
- Date Issued
- 2010-02-23
- Identifier
- FSU_uspto_7667055, 7667055, 711524, 11/449535, 6c9256d97d167832cbab694dc904bd27
- Format
- Citation
- Title
- Processes for the preparation of paclitaxel.
- Creator
-
Holton, Robert A., Vu, Phong H.
- Abstract/Description
-
The present invention provides processes for the production of paclitaxel. Paclitaxel is produced by protecting the C(7) and the C(10) hydroxy groups of 10-DAB with a bridging silicon-based protecting group. The resulting 7,10-protected 10-DAB derivative is then derivatized and deprotected to form paclitaxel.
- Date Issued
- 2008-04-15
- Identifier
- FSU_uspto_7358378, 7358378, 711524, 11/449075, 6c9256d97d167832cbab694dc904bd27
- Format
- Citation
- Title
- Processes for the preparation of docetaxel.
- Creator
-
Holton, Robert A., Vu, Phong H.
- Abstract/Description
-
The present invention provides processes for the production of docetaxel. Docetaxel is produced by protecting the C(7) and the C(10) hydroxy groups of 10-DAB with a bridging silicon-based protecting group. The resulting 7,10-protected 10-DAB derivative is then derivatized and deprotected to form docetaxel.
- Date Issued
- 2009-06-23
- Identifier
- FSU_uspto_7550608, 7550608, 711524, 11/449048, 6c9256d97d167832cbab694dc904bd27
- Format
- Citation
- Title
- Semi-synthesis of taxane derivatives using metal alkoxides and oxazinones.
- Creator
-
Holton, Robert A.
- Abstract/Description
-
A process for preparing taxane derivatives taxol by providing a metal alkoxide having the bi, tri-, or tetracyclic taxane nucleus, reacting the metal alkoxide with an oxazinone to form an intermediate, and converting the intermediate to the taxane derivative.
- Date Issued
- 1993-10-19
- Identifier
- FSU_uspto_5254703, 5254703, 711524, 07/863829, 600b83161da1122888348587dc18798c
- Format
- Citation
- Title
- Synthetic process for the preparation of taxol and other tricyclic and tetracyclic taxanes.
- Creator
-
Holton, Robert A., Somoza, Carmen, Kim, Hyeong B., Shindo, Mitsuru, Biediger, Ronald J., Boatman, P. Douglas, Smith, Chase C., Liang, Feng, Murthi, Krishna K.
- Abstract/Description
-
Process for the synthesis of taxol and other tricyclic and tetracyclic taxanes.
- Date Issued
- 1995-04-11
- Identifier
- FSU_uspto_5405972, 5405972, 711524, 08/189058, 600b83161da1122888348587dc18798c
- Format
- Citation
- Title
- Synthetic process for the preparation of tricyclic and tetracyclic taxanes.
- Creator
-
Holton, Robert A., Somoza, Carmen, Shindo, Mitsuru, Biediger, Ronald J., Boatman, P. Douglas, Smith, Chase C., Liang, Feng, Murthi, Krishna K., Kim, Hyeong Baik
- Abstract/Description
-
Process for the synthesis of taxol and other tricyclic and tetracyclic taxanes.
- Date Issued
- 1998-06-02
- Identifier
- FSU_uspto_5760252, 5760252, 711524, 08/769935, 600b83161da1122888348587dc18798c
- Format
- Citation
- Title
- Synthetic process for the preparation of tricyclic and tetracyclic taxanes.
- Creator
-
Holton, Robert A., Somoza, Carmen, Kim, Hyeong B., Shindo, Mitsuru, Biediger, Ronald J., Boatman, P. Douglas, Smith, Chase C., Liang, Feng, Murthi, Krishna K.
- Abstract/Description
-
Process for the synthesis of taxol and other tricyclic and tetracyclic taxanes.
- Date Issued
- 1997-04-08
- Identifier
- FSU_uspto_5618952, 5618952, 711524, 08/383956, 600b83161da1122888348587dc18798c
- Format
- Citation
- Title
- Preparation of substituted isoserine esters using &bgr;-lactams and metal or ammonium alkoxides.
- Creator
-
Holton, Robert A.
- Abstract/Description
-
A process for preparing N-acyl, N-sulfonyl and N-phosphoryl substituted isoserine esters in which a metal or an ammonium alkoxide is reacted with a &bgr;-lactam.
- Date Issued
- 2002-10-01
- Identifier
- FSU_uspto_6458977, 6458977, 711524, 09/516870, 600b83161da1122888348587dc18798c
- Format
- Citation
- Title
- Preparation of substituted isoserine esters using .beta.-lactams and metal or ammonium alkoxides.
- Creator
-
Holton, Robert A.
- Abstract/Description
-
A process for preparing N-acyl, N-sulfonyl and N-phosphoryl substituted isoserine esters in which a metal or an ammonium alkoxide is reacted with a .beta.-lactam.
- Date Issued
- 1995-07-04
- Identifier
- FSU_uspto_5430160, 5430160, 711524, 08/034247, 600b83161da1122888348587dc18798c
- Format
- Citation
- Title
- Preparation of substituted isoserine esters using metal alkoxides and &bgr;-lactams.
- Creator
-
Holton, Robert A.
- Abstract/Description
-
A process for preparing N-acyl, N-sulfonyl and N-phosphoryl substituted isoserine esters in which a metal alkoxide is reacted with a &bgr;-lactam.
- Date Issued
- 2003-05-13
- Identifier
- FSU_uspto_6562962, 6562962, 711524, 09/804821, 600b83161da1122888348587dc18798c
- Format
- Citation
- Title
- Pyridyl substituted B-lactam compounds.
- Creator
-
Holton, Robert A., Rengan, Kasthuri
- Abstract/Description
-
Pyridyl substituted .beta.-lactam compounds used in preparing taxane derivatives having a 3' pyridyl substituted C13 side chain.
- Date Issued
- 1998-06-02
- Identifier
- FSU_uspto_5760219, 5760219, 711524, 08/717136, 600b83161da1122888348587dc18798c
- Format
- Citation
- Title
- Process for selective derivatization of taxanes.
- Creator
-
Holton, Robert A., Zhang, Zhuming, Clarke, Paul A.
- Abstract/Description
-
Processes for the preparation of taxol and other taxanes through selective derivatization of the C(7) and C(10) hydroxyl groups of 10-DAB, particularly a novel process using a new strategy in which the C(10) hydroxyl group is protected or derivatized prior to the C(7) hydroxyl group; and the provision of C(7) and C(10) derivatized 10-DAB compounds.
- Date Issued
- 2001-02-20
- Identifier
- FSU_uspto_6191287, 6191287, 711524, 09/335408, 600b83161da1122888348587dc18798c
- Format
- Citation
- Title
- Process for selective derivatization of taxanes.
- Creator
-
Holton, Robert A., Zhang, Zhuming, Clarke, Paul A.
- Abstract/Description
-
Processes for the preparation of taxol and other taxanes through selective derivatization of the C(7) and C(10) hydroxyl groups of 10-DAB, particularly a novel process using a new strategy in which the C(10) hydroxyl group is protected or derivatized prior to the C(7) hydroxyl group; and the provision of C(7) and C(10) derivatized 10-DAB compounds.
- Date Issued
- 2004-03-16
- Identifier
- FSU_uspto_6706896, 6706896, 711524, 09/672270, 600b83161da1122888348587dc18798c
- Format
- Citation
- Title
- Process for selective derivatization of taxanes.
- Creator
-
Holton, Robert A., Zhang, Zhuming, Clarke, Paul A.
- Abstract/Description
-
Processes for the preparation of taxol and other taxanes through selective derivatization of the C(7) and C(10) hydroxyl groups of 10-DAB, particularly a novel process using a new strategy in which the C(10) hydroxyl group is protected or derivatized prior to the C(7) hydroxyl group; and the provision of C(7) and C(10) derivatized 10-DAB compounds.
- Date Issued
- 2007-10-30
- Identifier
- FSU_uspto_7288665, 7288665, 711524, 09/063477, 600b83161da1122888348587dc18798c
- Format
- Citation
- Title
- Preparation of substituted isoserine esters using metal alkoxides and .beta .
- Creator
-
Holton, Robert A.
- Abstract/Description
-
A process for preparing N-acyl, N-sulfonyl and N-phosphoryl substituted isoserine esters in which a metal alkoxide is reacted with a .beta.-lactam.
- Date Issued
- 1995-11-14
- Identifier
- FSU_uspto_5466834, 5466834, 711524, 08/314532, 600b83161da1122888348587dc18798c
- Format
- Citation
- Title
- Process for the preparation of metal alkoxides.
- Creator
-
Holton, Robert A.
- Abstract/Description
-
A process for preparing N-acyl, N-sulfonyl and N-phosphoryl substituted isoserine esters in which a metal alkoxide is reacted with a &bgr;-lactam.
- Date Issued
- 2004-01-27
- Identifier
- FSU_uspto_6683196, 6683196, 711524, 10/289103, 600b83161da1122888348587dc18798c
- Format
- Citation
- Title
- Process for the preparation of baccatin III analogs bearing new C2 and C4 functional groups.
- Creator
-
Holton, Robert A., Kim, Seokchan
- Abstract/Description
-
Process for the preparation of a derivative or analog of baccatin III or 10-desacetyl baccatin III having a C2 substituent other than benzoate and/or a C4 substituent other than acetate in which the C2 benzoate substituent and/or the C4 acetate substituent of a derivative of baccatin III or 10-desacetyl baccatin III is/are selectively reduced to the corresponding hydroxy group(s) and converted to R.sub.7 COO- and/or R.sub.8 COO-, respectively, wherein R.sub.7 and R.sub.8 are independently H,...
Show moreProcess for the preparation of a derivative or analog of baccatin III or 10-desacetyl baccatin III having a C2 substituent other than benzoate and/or a C4 substituent other than acetate in which the C2 benzoate substituent and/or the C4 acetate substituent of a derivative of baccatin III or 10-desacetyl baccatin III is/are selectively reduced to the corresponding hydroxy group(s) and converted to R.sub.7 COO- and/or R.sub.8 COO-, respectively, wherein R.sub.7 and R.sub.8 are independently H, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, moncyclic aryl, or monocyclic heteroaryl.
Show less - Date Issued
- 1995-03-21
- Identifier
- FSU_uspto_5399726, 5399726, 711524, 08/010798, 600b83161da1122888348587dc18798c
- Format
- Citation
- Title
- Process for the preparation of ammonium alkoxides.
- Creator
-
Holton, Robert A.
- Abstract/Description
-
A process for preparing N-acyl, N-sulfonyl and N-phosphoryl substituted isoserine esters in which a metal or an ammonium alkoxide is reacted with a &bgr;-lactam.
- Date Issued
- 2003-11-25
- Identifier
- FSU_uspto_6653490, 6653490, 711524, 10/194343, 600b83161da1122888348587dc18798c
- Format
- Citation
- Title
- Process for selective derivatization of taxanes.
- Creator
-
Holton, Robert A., Zhang, Zhuming, Clarke, Paul A.
- Abstract/Description
-
Processes for the preparation of taxol and other taxanes through selective derivatization of the C(7) and C(10) hydroxyl groups of 10-DAB, particularly a novel process using a new strategy in which the C(10) hydroxyl group is protected or derivatized prior to the C(7) hydroxyl group; and the provision of C(7) and C(10) derivatized 10-DAB compounds.
- Date Issued
- 2001-09-18
- Identifier
- FSU_uspto_6291691, 6291691, 711524, 09/588933, 600b83161da1122888348587dc18798c
- Format
- Citation
- Title
- Process for the preparation of 10-desacetoxybaccatin III and 10-desacetoxytaxol and derivatives thereof.
- Creator
-
Holton, Robert A., Somoza, Carmen
- Abstract/Description
-
A process for the preparation of a 10-desacetoxy and 10-desoxy tetracyclic taxane in which a tetracyclic taxane having a C10 hydroxy or acetoxy substituent is reacted with samarium diiodide.
- Date Issued
- 1994-08-16
- Identifier
- FSU_uspto_5338872, 5338872, 711524, 08/005229, 600b83161da1122888348587dc18798c
- Format
- Citation
- Title
- Process for the preparation of 10-desacetoxybaccatin III.
- Creator
-
Holton, Robert A., Somoza, Carmen
- Abstract/Description
-
A process for abstracting a C10 hydroxy, acyloxy or sulfonyloxy substituent from a taxane in which the C10 hydroxy, acyloxy or sulfonyloxy substituted taxane is reacted with samarium diiodide.
- Date Issued
- 1997-08-05
- Identifier
- FSU_uspto_5654447, 5654447, 711524, 08/500868, 600b83161da1122888348587dc18798c
- Format
- Citation
- Title
- Radiosensitizing taxanes and their pharmaceutical preparations.
- Creator
-
Holton, Robert A., Nadizadeh, Hossain, Yang, Li-Xi
- Abstract/Description
-
Taxanes containing electron-affinic radiosensitizing functional groups, their pharmaceutical preparations, and methods of making and using this new class of highly potent radiosensitizers of tumor cells.
- Date Issued
- 2006-06-27
- Identifier
- FSU_uspto_7067552, 7067552, 711524, 09/978436, 600b83161da1122888348587dc18798c
- Format
- Citation