Journal of Organic Chemistry 2007-11-23

One-pot cyclization of 2-aminophenethyl alcohols: a novel and direct approach to the synthesis of N-acyl indolines.

Zengxue Wang, Wen Wan, Haizhen Jiang, Jian Hao

Index: J. Org. Chem. 72(24) , 9364-7, (2007)

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Abstract

A unique one-pot cyclization of 2-aminophenethyl alcohols with carboxylic acids in the presence of PPh3, CCl4, and NEt3 furnished the formation of N-acyl indolines in good to excellent yields. This new approach provides an efficient, scalable, low-cost, and direct access to the biologically important indolines which are further oxidizable to indoles and oxindoles.