Chiral N-alkylated indoles are privileged structural motifs found in many natural products and pharmaceuticals and a search for effective methods with which to prepare chiral N-alkylated indoles is ongoing.Efficient s...Chiral N-alkylated indoles are privileged structural motifs found in many natural products and pharmaceuticals and a search for effective methods with which to prepare chiral N-alkylated indoles is ongoing.Efficient syntheses of enantioenriched N-alkylated indoles has been developed but not with standing these advances,the develop-ment of a facile method to prepare chiral N-alkylated indoles from simple and available starting materials under mild conditions is still needed.In this paper,we report a nitrogen replacement process driven by dearomatization that directly incorporates naturalα-amino acids into 2-alkynylanilines leading to the formation of a variety of multi-functional chiral N-alkylated indoles.展开更多
基金supported by the National Natural Science Foundation of China(Nos.21572033,21971043)the Science and Technology Commission of Shanghai Municipality(Nos.18XD1400800,19ZR1403400).
文摘Chiral N-alkylated indoles are privileged structural motifs found in many natural products and pharmaceuticals and a search for effective methods with which to prepare chiral N-alkylated indoles is ongoing.Efficient syntheses of enantioenriched N-alkylated indoles has been developed but not with standing these advances,the develop-ment of a facile method to prepare chiral N-alkylated indoles from simple and available starting materials under mild conditions is still needed.In this paper,we report a nitrogen replacement process driven by dearomatization that directly incorporates naturalα-amino acids into 2-alkynylanilines leading to the formation of a variety of multi-functional chiral N-alkylated indoles.
