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Title:
PRODUCTION OF 1-METHYLCARBAPENEM-3-CARBOXYLIC ACID
Document Type and Number:
Japanese Patent JPH04368386
Kind Code:
A
Abstract:

PURPOSE: To readily produce the subject compound useful as an antibiotic by subjecting a compound which is produced from two kinds of specific compounds to a ring-closing reaction under heating in a solvent.

CONSTITUTION: A compound of formula I [A is four to seven-membered heterocyclic group containing O, S, NR4 (R4 is H, imino-protecting group, etc.,) in the group; R1 is lower alkyl, alkynyl, etc., which may have a substituent; R2 is H, carboxyl-protecting group] is reacted with a compound of formula: R(R8) 3 (R8 is alkoxy, aryloxy, etc.,) in a solvent-free state or in an aprotic solvent at 30 to 150°C for 2-20hrs, and the acid adduct by-produced is evaporated away under vacuum. The left compound of formula II is subjected to a ring-closing reaction in a solvent such as toluene at 100-170°C for 2-30hrs, followed by distilling away the solvent and further subjecting the product to a crystallization process, etc., to provide the objective compound of formula III.


Inventors:
OIDA SADAO
TANAKA TERUO
MORI MAKOTO
KAWAMOTO ISAO
Application Number:
JP14590691A
Publication Date:
December 21, 1992
Filing Date:
June 18, 1991
Export Citation:
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Assignee:
SANKYO CO
International Classes:
C07D477/00; (IPC1-7): C07D477/00
Attorney, Agent or Firm:
Akio Ohno (2 outside)