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硫化合物的环脱硫反应。第12部分:一种从硫脲衍生物合成N-α-取代苯并咪唑的新的简便方法。

The cyclodesulphurization of thio-compounds. Part 12: A new simple method for the synthesis of N-alpha-substituted benzimidazoles from thiourea derivatives.

作者信息

Omar A M, Ragab M S, Farghaly A M, Barghash A M

出版信息

Pharmazie. 1976 Jun;31(6):348-50.

PMID:959294
Abstract

A new facile method has been established for the synthesis of N-alpha-substituted benzimidazoles by cyclodesulphurization of various N-[2-amino]-phenyl-N'-alkyl, -aryl and -aralkylthiourea derivatives with mercuric salts. Besides mercuric chloride, the use of mercuric oxide and mercuric acetate was successful for the first time in effecting ring closure of thio-compounds. The attempted use of acid condensing agents showed phosphoryl chloride to be less efficient than mercuric salts in conducting the cyclization reactions and led to poor yields of cyclized products.

摘要

已经建立了一种新的简便方法,通过各种N-[2-氨基]-苯基-N'-烷基、-芳基和-芳烷基硫脲衍生物与汞盐的环脱硫反应来合成N-α-取代苯并咪唑。除了氯化汞之外,首次成功使用氧化汞和醋酸汞实现硫化合物的闭环反应。尝试使用酸缩合剂时,发现磷酰氯在进行环化反应时不如汞盐有效,且导致环化产物的产率较低。

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