Method for preparing acethydrazide derivatives

乙酰肼衍生物的制备方法

Abstract

本发明属于化学制药技术领域,具体地说提供了具有通式I结构的乙酰肼衍生物的新型制备方法。(R)-2-(2-氯苯基)-2-氨基-乙酸甲酯与水合肼、丙酮或3-戊酮反应,生成中间体II。中间体II与对甲苯磺酸(2-噻吩乙醇)酯反应生成中间体III,中间体III合环反应生成产物I。不需要对产物进行拆分,工艺简便易行,反应时间短,收率高、纯度高,污染小,有利于劳动保护。
The invention belongs to the technical field of chemical pharmacy, and particularly provides a novel method for preparing the acethydrazide derivatives having a structure of a general expression I. The method comprises the following steps of: performing a reaction of (R)-2-(2-chlorphenyl)-2-amido-methyl acetate and hydrazine hydrate, acetone and 3-pentanone to obtain an intermediate II; performing a reaction of the intermediate II and p-toluene sulfonic acid(2- thiophene ethanol)ester to obtain an intermediate III; and performing the cyclization reaction of the intermediate III to obtain an intermediate I. The method has the advantages of no splitting of products, simple process, short reaction time, high yield, high purity, little pollution and the contribution to the labor protection.

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Patent Citations (2)

    Publication numberPublication dateAssigneeTitle
    CN-101260112-ASeptember 10, 2008天津药物研究院含噻吩并[3.2-c]吡啶的乙酰肼衍生物及其制备方法和用途
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NO-Patent Citations (2)

    Title
    《Chinese Chemical Letters》 20081231 CHENG Die等 Synthesis and activity evaluation of some novel derivatives of 第689-692页 1-8 第19卷, 第6期 2
    《Chinese Chemical Letters》 20081231 CHENG Die等 Synthesis, activity evaluation and 3D-QSAR study of some novel derivatives 第1075-1079页 1-8 第19卷, 第9期 2

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