Bartels Björn, Bolas Conor Gordon, Cueni Philipp, Fantasia Serena, Gaeng Nicolas, Trita Andrada Stefania
Roche Pharmaceutical Research and Early Development, Roche Innovation Center Basel, preclinical CMC, Process Research, F. Hoffmann-La Roche Ltd. , Grenzacherstrasse 124, 4070 Basel, Switzerland.
J Org Chem. 2015 Jan 16;80(2):1249-57. doi: 10.1021/jo502536t. Epub 2014 Dec 24.
A new method for the straightforward synthesis of 2-amino-[1,2,4]triazolo[1,5-a]pyridines and derivatives is presented. The target products are synthesized in high yields from guanidylpyridines and analogues via copper-catalyzed N-N coupling. The present methodology shows a wide scope, tolerating not only different substituents on the pyridine ring but also different heterocylic rings such as pyrazines, pyrimidines, and pyridazines.
本文介绍了一种直接合成2-氨基-[1,2,4]三唑并[1,5-a]吡啶及其衍生物的新方法。目标产物由胍基吡啶及其类似物通过铜催化的N-N偶联反应高产率合成。该方法适用范围广，不仅能耐受吡啶环上的不同取代基，还能耐受不同的杂环，如吡嗪、嘧啶和哒嗪。
