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Communication | Special issue | Vol 67, No. 2, 2006, pp.543-547
Published online, 18th November, 2005
DOI: 10.3987/COM-05-S(T)64
Pyridine Metallations in the Synthesis of Triazole Based NK-1 Antagonists

K. Jeff Thrasher, Erik J. Hembre, Kevin M. Gardinier, Kenneth A. Savin, Jian Eric Hong, and Louis N. Jungheim*

*Lilly Reserach Laboratories, Lilly Corporate Center, Eli Lilly & Company, Indianapolis, IN 46285-4813, U.S.A.


Regioselective pyridine metallation chemistry was used to produce N-(3-chloropyridin-4-ylmethyl)-N-methyl-1-(3,5-bis-trifluoromethylbenzyl)-5-phenyl-1H-[1,2,3]triazole-4-carboxamide (9a) and [1-(3,5-bis-trifluoromethylbenzyl)-5-morpholin-4-yl-1H-[1,2,3]triazol-4-yl]-[3-(3-chloropyridin-4-yl)-5-hydroxymethylisoxazol-4-yl]methanone (16a), which exhibit NK-1 antagonist activity.