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新型吡唑并[4,3 - e][1,4]二氮杂卓 - 5,8 - 二酮

Novel pyrazolo [4,3-e] [1,4] diazepin-5,8-diones.

作者信息

Migliara O, Schillaci D, Maggio B

机构信息

Dipartimento di Chimica e Technologie Farmaceutiche, Università di Palermo.

出版信息

Boll Chim Farm. 1992 Oct;131(9):331-4.

PMID:1492968
Abstract

The synthesis of some pyrazolo [4,3-e] [1,4] diazepin-5,8-diones has been accomplished starting from the readily available 1-ethyl-3-methyl-4-nitro-5-pyrazolecarbonylchloride and the appropriate alpha-aminoesthers, 2a, b, c. The catalytic reduction of the obtained 3a, b, c gave the products 4a, b, c which were, in turn, cyclized into the title compounds 5a, b, c. The intermediates of type 3 and 4 and the pyrazolo-diazepin-diones 5 were tested in vitro for their antimicrobial activity.

摘要

一些吡唑并[4,3 - e][1,4]二氮杂卓 - 5,8 - 二酮的合成是从容易获得的1 - 乙基 - 3 - 甲基 - 4 - 硝基 - 5 - 吡唑甲酰氯和适当的α - 氨基酯2a、b、c开始完成的。对所得到的3a、b、c进行催化还原得到产物4a、b、c,这些产物进而环化生成标题化合物5a、b、c。对3型和4型中间体以及吡唑并二氮杂卓二酮5进行了体外抗菌活性测试。

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