American Chemical Society
ol7b02203_si_004.cif (487.22 kB)

Palladium-Catalyzed Dehydrogenative Difunctionalization of Aminoalkenes with Aminals as Oxidants and Electrophiles

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posted on 2017-08-22, 20:29 authored by Lixin Li, Xibing Zhou, Bangkui Yu, Hanmin Huang
A novel palladium-catalyzed aminomethylamination of aminoalkenes with an aminal, functioning not only as an aminomethylation reagent but also as an oxidant, was developed. This direct and operationally simple protocol provides a fundamentally novel and unique approach toward the synthesis of 2-(2-aminoethyl)­indoles and 2-(2-aminoethyl)­pyrrolidines, which are important building blocks in synthetic organic chemistry. The unity of this method was highlighted by the rapid synthesis of Alosetron, a drug used for the treatment of irritable bowel syndrome.