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Copper-catalyzed synthesis of primary arylamines via cascade reactions of aryl halides with amidine hydrochlorides

机译:铜通过芳基卤化物与am盐酸盐的级联反应催化合成芳基伯胺

摘要

We have developed an efficient method for the synthesis of primary arylamines from aryl halides using amidine hydrochlorides as the ammonia surrogates. The protocol uses 10 mol % CuI as the catalyst, 20 mol % L-proline as the ligand, CS(2)CO(3) as the base, and DMF as the solvent and proceeds the sequential coupling of aryl halides with amidine hydrochlorides and hydrolysis of intermediates to give the target products. This is a convenient, inexpensive, and practical approach to primary arylamines.
机译:我们已经开发了一种有效的方法,可以使用am盐酸盐作为氨代用品从芳基卤化物合成伯芳基胺。该协议使用10 mol%的CuI作为催化剂,20 mol%的L-脯氨酸作为配体,CS(2)CO(3)作为碱,DMF作为溶剂,并进行芳基卤化物与am盐酸盐的顺序偶联水解中间体,得到目标产物。这是伯芳基胺的方便,廉价且实用的方法。

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