(4 - methoxyphenyl)(2 - methyl - 1 - (2 - morpholinoethyl) - 1H - indol - 3 - yl)methanone

[3 + 2]-Annulations of N-Hydroxy Allenylamines with Nitrosoarenes: One-Pot Synthesis of Substituted Indole Products

Pankaj Sharma and Rai-Shung Liu^*

Department of Chemistry, National Tsing-Hua University, Hsinchu, Taiwan, R.O.C.

Org. Lett., Article ASAP

DOI: 10.1021/acs.orglett.5b03447

Publication Date (Web): January 8, 2016

Copyright © 2016 American Chemical Society

*E-mail: rsliu@mx.nthu.edu.tw.

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Abstract

In the presence of O₂ and an IPrCuCl additive (5 mol %), [3 + 2]-annulation reactions of N-hydroxyaniline with nitrosobenzenes in cold toluene form isoxazolidin-5-ol derivatives. Heating the same reaction mixture with DBU in toluene affords highly functionalized indole products efficiently. This method provides short synthesis of several bioactive molecules including WIN 48098, WIN 53365, and JWH 015

http://pubs.acs.org/doi/abs/10.1021/acs.orglett.5b03447
http://pubs.acs.org/doi/suppl/10.1021/acs.orglett.5b03447/suppl_file/ol5b03447_si_001.pdf
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