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Title:
SEMI-SYNTHETIC METHOD FOR PRODUCTION OF N-DEBENZOYLPACLITAXEL
Document Type and Number:
Japanese Patent JP2010265274
Kind Code:
A
Abstract:

To provide a new method for producing N-debenzoylpaclitaxel which is a precursor of paclitaxel having antitumor activity.

The method includes condensation of a carboxylic acid expressed by formula (II) (in the formula, R1 is aryl or heteroaryl), its salt or its activated derivative with a 7-protected baccatin, and solvolysis of the obtained condensed compound with an acid catalyst to remove a part of the protective groups and open the oxazoline ring.

COPYRIGHT: (C)2011,JPO&INPIT


Inventors:
BOMBARDELLI EZIO
FONTANA GABRIELE
Application Number:
JP2010137314A
Publication Date:
November 25, 2010
Filing Date:
June 16, 2010
Export Citation:
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Assignee:
INDENA SPA
International Classes:
C07D305/14; C07B51/00; C07B61/00; C07C313/24; C07D263/04; C07D263/06; C07D413/12
Domestic Patent References:
JP2005530729A2005-10-13
Attorney, Agent or Firm:
Hajime Tsukuni
Fusayuki Saito
Keiko Ozawa