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. 2005 Jan 17;15(2):431-4.
doi: 10.1016/j.bmcl.2004.10.055.

Optimization of CRF1R binding affinity of 2-(2,4,6-trichlorophenyl)-4-trifluoromethyl-5-aminomethylthiazoles through rapid and selective parallel synthesis

Dmitry Zuev  1 , Jodi A Michne, Sokhom S Pin, Jie Zhang, Matthew T Taber, Gene M Dubowchik
Affiliations

Optimization of CRF1R binding affinity of 2-(2,4,6-trichlorophenyl)-4-trifluoromethyl-5-aminomethylthiazoles through rapid and selective parallel synthesis

Dmitry Zuev et al. Bioorg Med Chem Lett. .

Abstract

An efficient approach was developed to synthesize 2-(2,4,6-trichlorophenylamino)-4-trifluoromethyl-5-aminomethylthiazoles, corticotropin-releasing factor type 1 receptor (CRF(1)R) antagonists, by monoalkylation of amines with chloromethyl intermediate 5. The effect of variations in aminomethyl side chain of 6 on binding affinity is discussed.

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