Abstrait

Methyl 1-alkyl-4-(diethoxyphosphoryl)-5-oxopyrrolidines-3-carboxylate – versatile intermediates in the synthesis of á-methylene--lactams and ,-difunctionalized pyrrol-2(3H)-ones

Feten Beji


A general and efficient one-pot synthesis of a novel class of methyl 1- alkyl-4(diethoxyphosphoryl)-5-oxopyrrolidine-3-carboxylate 2 is presentedfor the first time. This approach is based on the Michael addition of dimethyl 2-(diethoxyphosphoryl)-3methylenesuccinate 1 toprimary amines. Application of the á-phosphono--lactams obtained forthe preparation of á-methylene--lactams is also reported.


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