Gilead Sciences, Inc.

Hauser, Inc.

Natural Pharmaceuticals, Inc.

Xiaoqin Cheng

Choung U Kim

Zheng-Yu Yang

John C Rohloff

Gary Paul Cook

Gong-Xin He

Jianying Wang

Manoj C Desai

William A Lee

Christopher K Murray

Edward Doerffler

Qun Y Zheng

S Kent Peterson

Gary P Cook

Quy Y Zheng

Compounds and compositions of Formula I are described, useful as anti-proliferative agents, and in particular anti-HPV, wherein:

Anti-proliferative compounds, compositions, and methods of use thereof

The invention relates to a process for converting Taxol A, B and C to Taxol primary amine which can then be easily and efficiently converted to Taxol A or docetaxel, thereby significantly increasing the yield of these products from biomass. The method includes the removal of the amide from the side-chain with Schwartz's reagent to form an imine, followed by the hydrolysis of the imine to the primary amine. The primary amine can then be converted to Taxol A or docetaxel. New Taxol imine compounds and primary amine salts have been formed by this process.

Preparation of Taxol and docetaxel through primary amines

Preparation of taxol and docetaxel through primary amines

Growing community of inventors

Broomfield, CO, United States of America

Xiaoqin Cheng