Abstract

A method to convert tertiary N-propargylamides into 1,2,4-trisubstituted imidazoles using ammonium chloride and zinc triflate as the catalyst is reported. The method is convenient, practical and employs conventional heating. It is also applicable to N-propargyl lactams and tends to populate the so-called ‘lead-like’ chemistry space.

A method to convert tertiary N-propargylamides into 1,2,4-trisubstituted imidazoles using ammonium chloride and zinc triflate as the catalyst is reported. The method is convenient, practical and employs conventional heating. It is also applicable to N-propargyl lactams and tends to populate the so-called ‘lead-like’ chemistry space.

中文翻译：

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通过氢化胺化-环化反应将叔丙炔酰胺高效转化为咪唑

摘要

报道了一种使用氯化铵和三氟甲磺酸锌作为催化剂将叔N-炔丙基酰胺转化为1,2,4-三取代的咪唑的方法。该方法方便，实用并且采用常规加热。它也适用于N-炔丙基内酰胺，并倾向于填充所谓的“铅样”化学空间。

报道了一种使用氯化铵和三氟甲磺酸锌作为催化剂将叔N-炔丙基酰胺转化为1,2,4-三取代的咪唑的方法。该方法方便，实用并且采用常规加热。它也适用于N-炔丙基内酰胺，并倾向于填充所谓的“铅样”化学空间。