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Title:
BENZOATE DERIVATIVE OF TAXOL
Document Type and Number:
Japanese Patent JPH069600
Kind Code:
A
Abstract:

PURPOSE: To obtain a new benzoate deriv. of taxol having water solubility and antitumor activity and useful in the treatment of mammalian tumor by forming benzoate of taxol isolated from the cortices of the stalks of western yews and (Taxus brevifolia, the cortices of nuts, etc.

CONSTITUTION: Taxol isolated from the cortices of the stalks of western yews and Taxus breuifolia, the cortices of nuts, etc., is allowed to react with chloromethylbenzoic acid anhydride to form a compd. of formula I (where Ac is acetyl). This compd. is allowed to react successively with a sec. amine of the formula NHRaRb [where Ra and Rb are each H or a 1-6C (substd.) alkyl and Ra and Rb together may form a group of formula II (where (y) is 1-3) or the like] and then with a compd. of formula III [where R3 and R4 are each H, a 1-6C alkyl or the like; R5 is OC(=O)R (R is a 1-6C alkyl) or the like; R6'-R9' are each OP=O(OH)2 or the like; and (n) is 0 or 1] or the like to obtain the objective compd. of formula IV [where R1 is H, a group of formula V (where R5 is the same as R5'; each of R6-R9 is the same as R6'; and (m) is 0 or 1) or the like; and R2 is a group of formula VI].


Inventors:
HENRII UON
TERANSU DOIRU
Application Number:
JP10382093A
Publication Date:
January 18, 1994
Filing Date:
April 30, 1993
Export Citation:
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Assignee:
BRISTOL MYERS SQUIBB CO
International Classes:
A61K31/335; A61K31/337; A61P35/00; C07D305/14; C07F9/655; C07F9/6558; (IPC1-7): C07D305/14; A61K31/335
Attorney, Agent or Firm:
Minoru Nakamura (6 outside)