Acceleration of the Arbuzov-type reaction via double activation of imine and H-phosphonate

Abstract

The synthesis of pyrrolidine derivatives containing an organophosphorus moiety at the 2-position of the ring is based on the reaction of an imine, 3-arylidene-1-pyrrolinium trifluoroacetate, with various H-phosphonates. The proposed method is characterized by a high reaction rate, mild reaction conditions, and the ability to use a variety of solvents, including water. The yield of the isolated product reaches 99%. All these advantages are achieved through the simultaneous activation of the imine and H-phosphonates.