A novel one-step synthesis of 2-substituted 6-azaindoles from 3-amino-4-picoline and carboxylic esters

…, F Gallou, J Xu, NK Yee, CH Senanayake

Index: Song, Jinhua J.; Tan, Zhulin; Gallou, Fabrice; Xu, Jinghua; Yee, Nathan K.; Senanayake, Chris H. Journal of Organic Chemistry, 2005 , vol. 70, # 16 p. 6512 - 6514

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Citation Number: 17

Abstract

Azaindoles constitute essential subunits in many pharmaceutically important drug substances. 1 In contrast to a vast array of methods for indole synthesis, 2 there are a limited number of methodologies available for azaindole formation. 3 The often employed method involves a Sonogashira coupling of a terminal alkyne with 4-tert-butoxycarbonylamino-3-iodopyridine followed by deprotection/cyclization in situ or in a separate step. 4 Palladium-catalyzed ...