SYNTHESIS OF NOVEL CEPHEM-4-KETONES - A NEW SERIES OF HUMAN-LEUKOCYTE ELASTASE INHIBITORS

被引：16

作者：

ALPEGIANI, M ^{[1
]}

BISSOLINO, P ^{[1
]}

PERRONE, E ^{[1
]}

CASSINELLI, G ^{[1
]}

FRANCESCHI, G ^{[1
]}

机构：

[1] FARMITALIA CARLO ERBA SPA,RES & DEV,VIA GRACCHI 35,I-20146 MILAN,ITALY

来源：

TETRAHEDRON LETTERS | 1991年 / 32卷 / 43期

关键词：

CEPHALOSPORINS; KETONES; PREPARATION OF; ALPHA-BROMOSULPHONES; PREPARATION AND REACTIVITY; PROTEASE INHIBITORS; HUMAN LEUKOCYTE ELASTASE (HLE);

D O I：

10.1016/0040-4039(91)80790-D

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

Alkylation of cephem-4-carbonyl chlorides at the sulphide or sulphone oxidation level with Grignard reagents, stannanes and cuprates is described. Radical or ionic bromination of the 3-methylcephem-4-ketone 8, followed by displacement with heterocyclic thiols, provides an entry to 3'-and 2-thiosubstituted derivatives, which are new potent inhibitors of HLE.

引用

页码：6207 / 6210

页数：4

共 18 条

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