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[肌肉松弛剂/第三次通讯:具有潜在肌肉松弛活性的丙烯酸衍生物的开发(作者译)]

[Muscle relaxants / 3rd communication: Development of acrylic acid derivatives of potential muscle relaxing activity (author's transl)].

作者信息

Kreutzberger A, Kreutzberger E

出版信息

Arzneimittelforschung. 1980;30(2):232-4.

PMID:7378096
Abstract

With reference to the occurrence of C=C partial structures and alkyl carboxylate groupings in muscle relaxants, the synthesis of acrylic acid derivatives by the aminomethinylation procedure has been followed up. From the reaction of s-triazine (1) with methyl acetoacetate (2a) and piperidine (5a), methyl 2-acetyl-3-piperidino acrylate (6a) arises. Analogously, 3-pyrrolidinoacrylophenone (6b) and 3-morpholinoacrylophenone (6c) are formed. In the same manner, the three-component reaction comprising the interaction of 1 with malononitrile (7) and a secondary amine (5) gives rise to the formation of the aminomethylenemalononitrile structure 8.

摘要

关于肌肉松弛剂中碳碳双键部分结构和烷基羧酸酯基团的出现情况,已经对通过氨基甲酰化方法合成丙烯酸衍生物进行了后续研究。由均三嗪(1)与乙酰乙酸甲酯(2a)和哌啶(5a)反应,生成2-乙酰基-3-哌啶基丙烯酸甲酯(6a)。类似地,生成3-吡咯烷基苯乙酮(6b)和3-吗啉代苯乙酮(6c)。同样地,由1与丙二腈(7)和仲胺(5)相互作用组成的三组分反应会生成氨基亚甲基丙二腈结构8。

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