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一些取代喹唑啉二酮作为平滑肌收缩潜在抑制剂的合成。

Synthesis of some substituted quinazolinediones as potential inhibitors of smooth muscle contraction.

作者信息

Akgün H, Hollstein U, Hurwitz L

机构信息

Department of Chemistry, School of Medicine, University of New Mexico, Albuquerque 87131.

出版信息

J Pharm Sci. 1988 Sep;77(9):735-9. doi: 10.1002/jps.2600770902.

Abstract

3-Substituted 2,4(1H,3H)-quinazolinediones were prepared from the corresponding N-substituted 2-aminobenzamides by treatment with ethyl chloroformate and KOH in ethanol. Also, a series of 3-substituted and 1-methyl-3-substituted 2,4(1H,3H)-quinazolinediones were synthesized by the reaction of 1-methyl-1,4-dihydro- and 1,4-dihydro-2,4-dioxo-3(2H)-quinazolineacetic acid with the corresponding N-substituted piperazines. The 13C NMR spectra and mass spectra of the compounds were measured and signals were assigned. Some of the compounds showed inhibitory action on contractile function of smooth muscle.

摘要

通过在乙醇中用氯甲酸乙酯和氢氧化钾处理相应的N-取代-2-氨基苯甲酰胺制备3-取代的2,4(1H,3H)-喹唑啉二酮。此外,通过1-甲基-1,4-二氢-和1,4-二氢-2,4-二氧代-3(2H)-喹唑啉乙酸与相应的N-取代哌嗪反应合成了一系列3-取代和1-甲基-3-取代的2,4(1H,3H)-喹唑啉二酮。测量了这些化合物的13C NMR光谱和质谱并对信号进行了归属。其中一些化合物对平滑肌的收缩功能表现出抑制作用。

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