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9-desoxotaxanes and process for the preparation of 9-desoxotaxanes
Description:
Process for the preparation of a derivative or analog of baccatin III or 10-desacetyl baccatin III having a C9 substituent other than keto in which the C9 keto substituent of taxol, a taxol analog, baccatin III or 10-desacetyl baccatin...
Compositions comprising a taxane having a carbamoyloxy substituent at C(10), a hydroxy substituent at C(7), and a range of C(2), C(9), C(14), and side chain substituents.
Process for the preparation of 10-desacetoxybaccatin III
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.
A taxane having a cyclopentyl ester substituent at C10, a keto substituent at C9, a hydroxy substituent at C2, a 2-thienyl substituent at C3′ and an isopropoxycarbamate substituent at C3′.
Process for the preparation of baccatin III analogs bearing new C2 and C4 functional groups
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...
Process for the preparation of a derivative or analog of baccatin III or 10-desacetyl baccatin III having a C9 substituent other than keto in which the C9 keto substituent of taxol, a taxol analog, baccatin III or 10-desacetyl baccatin...
A process for the preparation of a composition having the formula: in which a compound having the formula: is treated with a base and a silylating agent.
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...
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...
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...
Method for preparation of taxol using .beta.-lactam
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, acyl, acetal, ethoxyethyl, or other hydroxyl protecting group; and R.sub.3 is aryl, substituted...
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...
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.
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.
Certain alkoxy substituted taxanes and pharmaceutical compositions containing them
Description:
A taxane derivative of the formula ##STR1## wherein R.sub.1 is phenyl or substituted phenyl, PA0 R.sub.3 is CH.sub.3 O--, or CH.sub.3 CH.sub.2 O--, PA0 Z is --OT.sub.1, PA0 T.sub.1 is hydrogen, hydroxyl protecting group, or --COT.sub.2....
Semi-synthesis of taxane derivatives using metal alkoxides and oxazinones
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...
Process for the preparation of baccatin III analogs bearing new C2 and C4 functional groups
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...
A taxane having a cyclopentyl ester substituent at C10, a keto substituent at C9, a hydroxy substituent at C2, a 2-thienyl substituent at C3′ and an isopropoxycarbamate substituent at C3′.
Heteroaryl substituted oxazinone compounds for the preparation of taxol
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, ...
Preparation of substituted isoserine esters using &bgr;-lactams and metal or ammonium alkoxides
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.
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...
C(10) ethyl ester and C(10) cyclopropyl ester substituted taxanes
Description:
Taxanes having an ethyl ester or cyclopropyl ester substituent at C(10), a keto substituent at C(9), a hydroxy substituent at C(7), a thienyl substituent at C(3′) and a cyclobutyloxycarbamate or cyclopentyloxycarbamate substituent...
Preparation of substituted isoserine esters using .beta.-lactams and metal or ammonium alkoxides
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.
Processes for the production of polycyclic fused ring compounds
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...
Process for the preparation of 10-desacetoxybaccatin III and 10-desacetoxytaxol and derivatives thereof
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.
Process for the preparation of 9-desoxotaxol, 9-desoxobaccatin III and analogs thereof
Description:
Process for the preparation of a derivative or analog of baccatin III or 10-desacetyl baccatin III having a C9 substituent other than keto in which the C9 keto substituent of taxol, a taxol analog, baccatin III or 10-desacetyl baccatin...
Method for preparation of taxol using an oxazinone
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, ...
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