NOVEL REACTION CONDITIONS FOR THE CLEAVAGE OF SILYLETHERS IN THE PREPARATION OF PACLITAZEL
Application IN/PCT/2001/01092/MUM published 2006-12-22, filed 2001-09-11
Novel reaction conditions for the cleavage of silyl ethers from silyl protected taxane precursors to afford paclitaxel and paclitaxel analogues in high yield and quality are described. Paclitaxel is prepared from a taxane precursor by treating the taxane precursor with a strong acid such as trifluoroacetic acid in a solvent such as aqueous acetic acid, such that the amount and number of side reactions and taxane impurities are significantly minimized. Also described are the crystallization methods for the isolation of paclitaxel in either of the two crystal forms A or B. Paclitaxel and paclitaxel analogues are anti-cancer agents.
Applicant
1)BRISTOL-MYERS SQUIBB COMPANY
:P.O.BOX 4000, PRINCETON, NEW JERSEY 08543-4000, U.S.A.
Inventor
1)AMBARISH SINGH 2)RAYMOND E. WEAVER 3)GERALD L. POWERS 4)VICTOR W. ROSSO
International Info
Classification: C07D 305/14
Publication Number: WO 00/69840
Application Date: 2000-05-08
Priority Information
60/134,469 U.S.A. 1999-05-17