ELECTROLYTIC PARTIAL FLUORINATION OF ORGANIC-COMPOUNDS .18. ELECTROSYNTHESIS OF 4,4-DIMETHYL-2-ETHOXYCARBONYL-5-FLUORO-3-THIOLANONES - HIGHLY POTENT HUMAN TYPE-II PLA(2) INHIBITORS

被引：33

作者：

NARIZUKA, S ^{[1
]}

FUCHIGAMI, T ^{[1
]}

机构：

[1] TOKYO INST TECHNOL, DEPT ELECTR CHEM, MIDORI KU, YOKOHAMA 226, KANAGAWA, JAPAN

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1995年 / 5卷 / 12期

关键词：

D O I：

10.1016/0960-894X(95)00215-F

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Anodic monofluorination of 2-methyl- and 2-benzyl-4,4-dimethyI-2-ethoxy-carbonyl-3-thiolanones 1 and 2 was successfully performed to provide the corresponding 5-fluorinated products 3 and 4, respectively in good yields. The stereoisomeric mixture of 4 was found to possess comparable or even stronger in vitro human type II phospholipase A, inhibitory activity compared with the known inhibitor, manozlide, and the cis isomer of 4 exhibited higher activity than the trans isomer.

引用

页码：1293 / 1294

页数：2

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