SYNTHESIS OF THE DIAZA ANALOG OF ELLAGIC ACID

被引：9

作者：

KANOJIA, RM

OHEMENG, KA

SCHWENDER, CF

BARRETT, JF

机构：

[1] Discovery Research, The R.W. Johnson Pharmaceutical Research Institute Rariran

来源：

TETRAHEDRON LETTERS | 1995年 / 36卷 / 47期

关键词：

D O I：

10.1016/0040-4039(95)01872-F

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

The novel diaza analogue 2 of DNA-gyrase inhibitor ellagic acid 1 was synthesized via the Ullmann coupling of methyl 2-bromo-3-nitroveratrate 6 which, in turn, was prepared by a 7-step synthesis from 2-bromopiperonal 10 requiring a contrived, regiospecific 3-nitration as a crucial step. Analogue 2 was two-fold as potent a DNA-Gyrase inhibitor as 1.

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页码：8553 / 8556

页数：4

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