Copper-Catalyzed (4+1) Cascade Annulation of Terminal Alkynes with 2‑(Tosylmethyl)anilines: Synthesis of 2,3-Disubstituted Indoles

A novel strategy based on Cu-catalyzed (4+1) cascade annulation of terminal alkynes as one-carbon synthons with 2-(tosylmethyl)­anilines has been developed for the expeditious synthesis of 2,3-disubstituted indoles, in which in situ generations of aza-o-quinone methides and alkynyl-copper­(I) specie...

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Bibliographic Details
Published in:Organic letters 2021-11, Vol.23 (22), p.8905-8909
Main Authors: Yan, Xu, Liu, Chun-Fang, An, Xian-Tao, Ge, Xiao-Min, Zhang, Qing, Pang, Lin-Han, Bao, Xu, Fan, Chun-An
Format: Article
Language:English
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Summary:A novel strategy based on Cu-catalyzed (4+1) cascade annulation of terminal alkynes as one-carbon synthons with 2-(tosylmethyl)­anilines has been developed for the expeditious synthesis of 2,3-disubstituted indoles, in which in situ generations of aza-o-quinone methides and alkynyl-copper­(I) species are involved. This annulation provides an effective method for the assembly of synthetically and structurally interesting 2,3-disubstituted indoles.
ISSN:1523-7060
1523-7052
DOI:10.1021/acs.orglett.1c03402