Title:
【発明の名称】タキサン誘導体の製造法およびそのためのβ‐ラクタム中間体
Document Type and Number:
Japanese Patent JP3492367
Kind Code:
B2
Abstract:
Taxol (I) is a complex diterpene which is currently considered the most exciting lead in cancer chemotherapy. Taxol possesses high cytotoxicity and strong antitumor activity against different cancers which have not been effectively treated by existing antitumor drugs. However, taxol has a problem with solubility in aqueous media, which may impose some serious limitation in its use. TAXOTERE (III) seems to have antitumor activity superior to taxol with better bioavailability. Taxotère has a modified taxol structure with a modified C-13 side chain. This fact strongly indicates that modification on the C-13 side chain would provide a new series of taxol and TAXOTERE analogues which may have higher potency, better bioavailability and less unwanted toxicity. The present invention provides efficient and practical methods for the syntheses of TAXOTERE and its analogues through beta -lactam intermediates and their coupling with baccatin III.
Inventors:
Ojima, Iwao
Application Number:
JP51806494A
Publication Date:
February 03, 2004
Filing Date:
January 28, 1994
Export Citation:
Assignee:
THE RESEARCH FOUNDATION OF STATE UNIVERSITY OF NEW YORK
International Classes:
C07D205/08; C07D305/14; (IPC1-7): C07D305/14
Domestic Patent References:
| JP386860A | ||||
| JP5239044A | ||||
| JP61782A | ||||
| JP72885A | ||||
| JP7505887A | ||||
| JP8506324A |
Other References:
Ｊ．Ｏｒｇ．Ｃｈｅｍ．，（１９９１），５６（５），ｐ．１６８１−３
Ｔｅｔｒａｈｅｄｒｏｎ，（１９８９），４５（１３），ｐ．４１７７−９０
Ｔｅｔｒａｈｅｄｒｏｎ，（１９８９），４５（１３），ｐ．４１７７−９０
Attorney, Agent or Firm:
Kazuo Sato (1 person outside)