Title:
ANTITUMOR COMPOUND AND ITS PREPARATION
Document Type and Number:
Japanese Patent JP3145993
Kind Code:
B2
Abstract:
PROBLEM TO BE SOLVED: To obtain a new antitumor compound having strong antitumor activity against human breast cancer cell, non-small cell lung cancer cell, ovarian cancer cell and colon carcinoma cell.
SOLUTION: This compound is shown by formula I (R1 is an alkyl, an alkenyl or the like; R2 is an alkyl, a cycloalkyl or the like; R3, R4 and R6 are each H, an acyl or the like; R7 is a 1-20C acyl; R8 is H or a hydroxyl protecting group) such as (-)(1R,2S)-2-phenyl-1-cyclohexyltriisopropylsilyloxyacetate. The compound of formula I is obtained by subjecting a baccatin of formula II (G1, G2 and G4 are each an acyl, an alkyl or the like) and a β-lactam of formula III (G is methoxymethyl, methoxyethyl or the like) in the presence of a base (e.g. sodium hexamethyldisilazide or the like) preferably at a temp. of -50 to 25°C in an inert gas atmosphere to deprotect a hydroxyl protecting group. The ratio of the β-lactam to the baccatin is preferably 1:1.
Inventors:
Ojima
Bombardier Ezzio
Bombardier Ezzio
Application Number:
JP10293599A
Publication Date:
March 12, 2001
Filing Date:
April 09, 1999
Export Citation:
Assignee:
The Research Foundation of the State University of New York
Indena Sochieta Per Azioni
Indena Sochieta Per Azioni
International Classes:
A61K31/00; A61K31/335; A61K31/337; A61P35/00; C07D205/08; C07D305/14; C07F7/18; (IPC1-7): C07D305/14; A61K31/337; C07F7/18
Domestic Patent References:
| JP8508497A |
Attorney, Agent or Firm:
Minoru Nakamura (6 outside)