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三组分'一锅法'合成吡咯烷类衍生物

         

摘要

This paper reports a new method of the synthesis of the highly substituted pyrrolidine derivatives, which were derived from different series of aromatic aldehyde、glycine methyl ester and diethyl maleate by using silver oxide as catalyst and N,N'-Diisopropylcarbodiimide (DIC) as dehydrant reagent in the 1,3-dipolar cycloaddition reaction. Under optimal conditions, eight endo-8 pyrrolidine adducts were obtained with excellent diastereoselectivities and moderate to high yields. Moreover, the cycloaddition reaction has the following features: a convenient and simple path, mild reaction conditions and a cheap catalyst.%本文报道了以氧化银为催化剂,以N, N'-二异丙基碳二亚胺(DIC)为脱水剂,以不同系列芳香醛、甘氨酸甲酯和马来酸二乙酯为原料,通过1,3-偶极环加成反应合成高度取代的吡咯烷衍生物的新方法.在最优的条件下,以较好的非对映选择性及中等以上的产率,合成了8个endo类型的吡咯衍生物,并且该环加成反应合成途径简捷,反应条件温和,催化剂廉价易得.

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