ol7b02203_si_002.cif (20.52 kB)
Palladium-Catalyzed Dehydrogenative Difunctionalization of Aminoalkenes with Aminals as Oxidants and Electrophiles
dataset
posted on 2017-08-22, 20:29 authored by Lixin Li, Xibing Zhou, Bangkui Yu, Hanmin HuangA 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.