Florida State University Research Foundation, Inc.

Fsu Research Foundation, Inc.

Phong Vu

Robert A Holton

Vincent Reboul

Tawfik Gharbaoui

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 at C(3&#x2032;), pharmaceutical compositions comprising such taxanes, methods of treatment and administration, and methods of preparation of medicaments comprising the taxanes.

C(10) ethyl ester and C(10) cyclopropyl ester substituted taxanes

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&#x2032;.

C10 cyclopentyl ester substituted taxanes

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.

Processes for the production of polycyclic fused ring compounds

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.

Processes for the preparation of docetaxel

The present invention is directed to a process for the preparation of &#x3b2;-lactams. Generally, an imine is cyclocondensed with a ketene acetal or enolate to form the &#x3b2;-lactam product in a 'one pot' synthesis, this process is generally performed at a higher temperature than conventional processes.

&#x3b2;-lactam synthesis

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.

Processes for the preparation of paclitaxel

A process for the resolution of an enantiomeric mixture of &#x3b2;-lactams containing an ester, the process comprising selectively hydrolyzing the ester of one of the enantiomers by combining the mixture with homogenized liver.

Enzymatic process for the resolution for enantiomeric mixtures of &#x3b2;-lactams

Taxane synthesis method and intermediates

A process for the resolution of an enantiomeric mixture of &bgr;-lactams containing an ester, the process comprising selectively hydrolyzing the ester of one of the enantiomers by combining the mixture with homogenized liver.

Enzymatic process for the resolution of enantiomeric mixtures of &bgr;-lactams

Method for the synthesis of taxanes

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.

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Little Falls, NJ, United States of America

Phong Vu