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Title:
CARBAPENEM DERIVATIVE
Document Type and Number:
Japanese Patent JPH02223587
Kind Code:
A
Abstract:

NEW MATERIAL:The compound of formula I [R1 is H, (protected) hydroxy-lower alkyl, etc.; COOR2 is (protected) carboxyl, etc.; R3 is lower alkyl; R4 is group of formula II (the group of formula III constituting the partial structure of R4 is 5-membered or 6-membered nitrogen-containing heterocyclic group containing 1-4 hetero atoms selected from O, S and N; R5 is H, nitro, etc.)].

EXAMPLE: (1R,5S,6S,8R)-2-[(6,7-dihydro-5H-pyrrolo-[1, 2-C]imidazol-7-yl)thio]-6-(1- hydroxyethyl)-1-methyl-1-carbapen-2-em-3-carboxylic acid.

USE: Antibacterial agent against bacteria resistant to cephalosporin or penicillin, Gram-positive bacteria and Gram-negative bacteria.

PREPARATION: The objective compound of formula I is produced by oxidizing a compound of formula IV (R2 is ester residue; R7 is methyl, etc.) with peracetic acid, etc., in a solvent, substituting the resultant compound of formula V with a thiol compound of formula VI in methanol, etc., and, as necessary, deprotecting the product.


Inventors:
TAKEMURA MAKOTO
NISHI TOSHIYUKI
SUZAKI HIROSHI
ISHIDA YOHEI
KODA HIROKO
HAYANO TAKESHI
Application Number:
JP28944189A
Publication Date:
September 05, 1990
Filing Date:
November 07, 1989
Export Citation:
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Assignee:
DAIICHI SEIYAKU CO
International Classes:
C07D477/00; A61K31/397; A61K31/41; A61P31/04; C07D519/00; (IPC1-7): A61K31/41; C07D477/00; C07D519/00
Domestic Patent References:
JPS63191004A1988-08-08
JPS6261985A1987-03-18
JPS62149683A1987-07-03