Phosphite Catalyzed Aza-Baylis-Hillman Reaction of Imines and Methyl Acrylates

Abstract

本文以一系列亚磷酸酯为催化剂，对催化芳香醛亚胺与丙烯酸甲酯的氮杂Baylis-Hillman反应进行了系统研究。经过对该反应的溶剂、反应温度、底物浓度、催化剂进行了筛选和优化，我们发现亚磷酸二乙酯和1,4-二氮杂二环[2.2.2]辛烷(DABCO)能有效催化该反应。最后对一系列底物进行测试，所有反应能以中等到良好的收率得到α-亚甲基β-磺酰胺基丙烯酸酯产物。 The aza-Bayllis-Hillman reactions of imines and methyl acrylate catalyzed by achiral phosphite were studied. The reaction conditions, such as solvent, temperature, concentration, catalysts, and substrates were screened. The target products of α-methylene--sulfonamido acrylates were obtained with 25% - 78% yield.