jo9b02404_si_002.cif (211.84 kB)
Copper-Catalyzed Amination of C(sp3)–H bonds: From Anilides to Indolines
dataset
posted on 2019-12-13, 13:04 authored by Jinguo Long, Liyuan Le, Takanori Iwasaki, Renhua Qiu, Nobuaki KambeCopper-catalyzed oxidative intramolecular cyclization
of o-alkylated anilines via cleavage of C(sp3)–H and N–H bonds for the production of indolines
is described. This approach provides a straightforward strategy for
the synthesis of nitrogen-containing heterocyclic compounds through
the functionalization of unactivated C(sp3)–H bonds
with high site selectivity. The present catalytic system shows high
preference for functionalization of unactivated C(sp3)–H
bonds over C(sp2)–H bonds, leading to C–N
bond formation.