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Title:
TRICYCLIC CARBAPENEMS
Document Type and Number:
Japanese Patent JP2000038387
Kind Code:
A
Abstract:

To provide a novel compound that has high anti-microbial activity, is stable to dehydropeptidase I and shows high urinary content.

This is a novel compound represented by formula I [A is a heteroaryl monocyclic thio group that is represented by formula II (R1 and R2 are each a 1-6C alkyl, a 3-6C cycloalkyl or the like), or contains 1-3N, O or S atoms], its derivatives, their salts, typically (4R, 8S, 9R, 10 S)-4-(dibenzylamino-thiocarbonyl)thiomethyl-10-[(R)-1-hydroxyethyl]-11-oxo-1- azatricyclo[7.2.0.03.8]undeca-2-ene-2-carboxylic acid. This compound is prepared by sulfonylation of a compound of formula III before the sulfonylated product is allowed to react with a compound of the formula: Hap (Ap may be protected, when A includes hydroxyl or amino group), allowing the resultant intermediate to react with a compound of the formula: XCOCOOR14 (R14 is a protecting group of carboxyl; X is a halogen or the like) followed by ring closure reaction and final deprotection of the resultant intermediate.


Inventors:
KAWAMOTO ISAO
SUGANO OSAMU
SHIMOJI YASUO
OYA SATORU
Application Number:
JP13744499A
Publication Date:
February 08, 2000
Filing Date:
May 18, 1999
Export Citation:
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Assignee:
SANKYO CO
International Classes:
C07D477/00; A61K31/00; A61K31/397; A61K31/40; A61K31/407; A61K31/41; A61K31/415; A61K31/4164; A61K31/4178; A61K31/4196; A61K31/425; A61K31/427; A61K31/433; A61K31/435; A61K31/4353; A61K31/437; A61K31/44; A61K31/4427; A61K31/4439; A61K31/445; A61K31/4465; A61K31/4523; A61K31/454; A61K31/47; A61K31/4709; A61K31/495; A61K31/496; A61K31/535; A61K31/5375; A61K31/5377; A61K31/54; A61K31/541; A61P31/00; A61P31/04; C07D513/04; (IPC1-7): C07D477/00; A61P31/04; A61K31/407; A61K31/41; A61K31/4196; A61K31/433; A61K31/4178; A61K31/427; A61K31/435; A61K31/437; A61K31/4439; A61K31/454; A61K31/4709; A61K31/496; A61K31/5377; A61K31/541; C07D513/04
Attorney, Agent or Firm:
Akio Ohno (2 outside)