Substitution-Controlled Selective Formation of Hexahydrobenz[ e]isoindoles and 3-Benzazepines via In(OTf)3-Catalyzed Tandem Annulations

Org Lett. 2018 Sep 21;20(18):5680-5683. doi: 10.1021/acs.orglett.8b02406. Epub 2018 Sep 6.

Abstract

A dramatic N-substituent controlled tandem annulation of 2-(2-(2-bromoethyl)phenyl)-1-sulfonylaziridines with 1,3-dicarbonyl compounds has been developed. When the N-substituent was a 4-methylbenzenesulfonyl group (Ts), sequential ring opening of aziridines, nucleophilic substitution, and lactamization took place to provide a series of hexahydrobenz[ e]isoindole compounds in good yields with good diastereoselectivities. By contrast, 3-benzazepine compounds were afforded in good yields via ring opening of aziridines and nucleophilic substitution when the N-substituent was the 4-nitrobenzenesulfonyl group (Ns).

Publication types

  • Research Support, Non-U.S. Gov't