Highly efficient N-acylation of azoles via cross dehydrogenative coupling

来源 :第十三届全国均相催化学术讨论会 | 被引量 : 0次 | 上传用户:vvchan
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  Azoles are ubiquitous motifs in nature and exhibit potential biological activities and medicinal significance.Their synthesis and further functionalization are of considerable importance.Consequently,the development of highly efficient methods for the synthesis of functional azoles is prevalent in organic synthesis.Recently,the N-arylation and N-alkylation of azoles have advanced significantly.1,2 However,Nacylation of azoles has been reported rarely.Traditionally,synthesis of N-acyl azoles usually required acyl chlorides as the acyl source in a basic system via a nucleophilic substitution process.3 Obviously,using aldehydes as the acyl source without a base via cross dehydrogenative coupling strategy to synthesiz e N-acyl azoles is greener and easy-to-handle.In this communication,we wish to report a protocol for a KI- catalyzed N-acylation of azoles using TBHP as the oxidant
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