Title:
PENAM DERIVATIVE AND ITS PRODUCTION
Document Type and Number:
Japanese Patent JP3025910
Kind Code:
B2
Abstract:
PURPOSE: To provide a new compound having excellent antibacterial activity to Gram-positive bacteria and Gram-negative bacteria, stable to β-lactamase, exhibiting excellent activity to resistant bacteria and useful as a penam-type antibiotic substance.
CONSTITUTION: The compound of formula I [R1 is H, halogen, amino or protected amino; R2 is H, halogen, lower alkoxy, lower acyl, lower alkyl, etc.; R1 and R2 may together form oxo; R3 is H or carboxylic acid protecting group; (n) is 0-2; Y is halogen, N3, ONO2, OR4, etc., (R4 is lower alkyl, aryl, heterocyclic group, etc.)]. The compound of formula I can be produced by reacting a 2- exomethylenepenamoxide derivative of formula II with a nucleophilic agent of the formula Y-H in the presence of a base (e.g. sodium hydride) in a solvent (e.g. THF) at -78 to +100°C.
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Inventors:
Shigeru Torii
Hideo Tanaka
Masatoshi Taniguchi
Michio Sasaoka
Takashi Kii
Yutaka Kameyama
Hideo Tanaka
Masatoshi Taniguchi
Michio Sasaoka
Takashi Kii
Yutaka Kameyama
Application Number:
JP4708591A
Publication Date:
March 27, 2000
Filing Date:
March 13, 1991
Export Citation:
Assignee:
Otsuka Chemical Co., Ltd.
International Classes:
A61K31/43; A61P31/04; C07D499/04; C07D499/42; C07D499/46; C07D499/86; C07D499/87; C07D499/893; C07D499/897; (IPC1-7): C07D499/86; A61K31/43; A61P31/04; C07D499/04; C07D499/42; C07D499/46; C07D499/87; C07D499/897
Domestic Patent References:
| JP3258784A | ||||
| JP2204494A | ||||
| JP3206038A | ||||
| JP1283288A | ||||
| JP272180A |
Other References:
Ｊ．Ｃｈｅｍ．Ｓｏｃ．，Ｃｈｅｍ．Ｃｏｍｍｕｎ．（１９８６），（３），ｐａｇｅｓ２７３−２７５
Ｊ．Ｃｈｅｍ．Ｓｏｃ．，Ｐｅｒｋｉｎ Ｔｒａｎｓ．１（１９７４），（１），ｐａｇｅｓ２２−２５
Ｊ．Ｃｈｅｍ．Ｓｏｃ．，Ｐｅｒｋｉｎ Ｔｒａｎｓ．１（１９７４），（１），ｐａｇｅｓ２２−２５
Attorney, Agent or Firm:
Eiji Saegusa (4 others)