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Title:
PRODUCTION OF TAXOL USING AN OXAZINONE
Document Type and Number:
Japanese Patent JPH03232869
Kind Code:
A
Abstract:

NEW MATERIAL: A compound of formula I (R1 is aryl, substd. aryl, alkenyl, alkynyl or alkyl; R8 is H, ethoxyethyl, 2,2,2-trichloroethoxymethyl or other hydroxyl protecting group; R3 is R1).

EXAMPLE: Cis-2,4-diphenyl-5-(1-ethoxyethoxy)-4,5-dihydro-1,3-oxazin-6-one.

USE: Side chain precursors for the synthesis of taxol compounds useful as antitumor agents.

PROCESS: A β-lactam compound of formula II (R2 and R5 are each H, alkyl, alkenyl, aryl, etc.; R3 and R6 are each H, alkyl, aryl, etc.), is subjected to ring opening with potassium hydroxide and then cyclized in the presence of potassium tert.-butoxide and methanesulfonyl chloride to give the compound of formula I.


Inventors:
ROBAATO EI HOORUTON
Application Number:
JP30846390A
Publication Date:
October 16, 1991
Filing Date:
November 14, 1990
Export Citation:
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Assignee:
UNIV FLORIDA STATE (US)
International Classes:
A61K31/335; A61K31/337; A61P35/00; C07C231/10; C07C233/47; C07C233/83; A61K31/215; C07C233/87; C07D265/04; C07D265/06; C07D265/10; C07D305/14; C07D413/00; C07D; (IPC1-7): A61K31/215; A61K31/335; C07C233/47; C07C233/83; C07D265/06; C07D305/14
Attorney, Agent or Firm:
Akira Asamura (3 outside)