Tetrahedron Letters

Heck cross-coupling reaction of 3-iodoindazoles with methyl acrylate: a mild and flexible strategy to design 2-aza tryptamines

V Collot, D Varlet, S Rault

Index: Collot, Valerie; Varlet, Didier; Rault, Sylvain Tetrahedron Letters, 2000 , vol. 41, # 22 p. 4363 - 4366

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Citation Number: 46

Abstract

In order to design 2-aza bioisosteres of tryptamine, serotonin or melatonin, the conditions of the Heck coupling reaction of 3-iodoindazoles with methyl acrylate are studied. This reaction authorizes the synthesis of 3-indazolylpropenoates as key intermediates to prepare 3- indazolylpropionic acids and 3-indazolylethylamines. The flexible synthetic strategy allows molecular diversity.

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