title: Synthesis of Indolizines via Reaction of 2-Substitued Azaarenes with Enals by an Amine-NHC Relay Catalysis.
abstract: A metal-free catalytic strategy for the facile synthesis of biologically relevant molecular architectures indolizines and imidazopyridines has been developed. The process is promoted by amine and N-heterocyclic carbene (NHC) relay catalysis via Michael addition-[3 + 2] fusion of simple azaarenes and α,β-unsaturated aldehydes. The preparative power is demonstrated in the synthesis of anxiolytic drug saripidem via two simple one-pot operations with overall 45% yield.
authors.affiliation: State Key Laboratory of Bioengineering Reactor, Shanghai Key Laboratory of New Drug Design, and School of Pharmacy, East China University of Science and Technology , 130 Mei-long Road, Shanghai 200237, China.
authors.forename: Hongxian
authors.initials: H
authors.lastname: Li
authors.affiliation: State Key Laboratory of Bioengineering Reactor, Shanghai Key Laboratory of New Drug Design, and School of Pharmacy, East China University of Science and Technology , 130 Mei-long Road, Shanghai 200237, China.
authors.forename: Xiangmin
authors.initials: X
authors.lastname: Li
authors.affiliation: State Key Laboratory of Bioengineering Reactor, Shanghai Key Laboratory of New Drug Design, and School of Pharmacy, East China University of Science and Technology , 130 Mei-long Road, Shanghai 200237, China.
authors.forename: Yang
authors.initials: Y
authors.lastname: Yu
authors.affiliation: State Key Laboratory of Bioengineering Reactor, Shanghai Key Laboratory of New Drug Design, and School of Pharmacy, East China University of Science and Technology , 130 Mei-long Road, Shanghai 200237, China.
authors.forename: Jianjun
authors.initials: J
authors.lastname: Li
authors.affiliation: State Key Laboratory of Bioengineering Reactor, Shanghai Key Laboratory of New Drug Design, and School of Pharmacy, East China University of Science and Technology , 130 Mei-long Road, Shanghai 200237, China.
authors.forename: Yuan
authors.initials: Y
authors.lastname: Liu
authors.affiliation: State Key Laboratory of Bioengineering Reactor, Shanghai Key Laboratory of New Drug Design, and School of Pharmacy, East China University of Science and Technology , 130 Mei-long Road, Shanghai 200237, China.
authors.forename: Hao
authors.initials: H
authors.lastname: Li
authors.affiliation: State Key Laboratory of Bioengineering Reactor, Shanghai Key Laboratory of New Drug Design, and School of Pharmacy, East China University of Science and Technology , 130 Mei-long Road, Shanghai 200237, China.|Department of Chemistry and Chemical Biology, University of New Mexico , Albuquerque, New Mexico 87131-0001, United States.
authors.forename: Wei
authors.identifier: 0000-0001-6043-0860
authors.initials: W
authors.lastname: Wang