Ammonia → 5-[6-({[tert-butyl(dimethyl)silyl]oxy}methyl)-3H-imidazo[4,5-c]pyridin-3-yl]-3-{(1R)-1-[2-(trifluoromethyl)phenyl]ethoxy}thiophene-2-carboxamide

Participants

Reaction Conditions

Reaction Steps

A mixture of 12 g of methyl 5-[6-({[tert-butyl(dimethyl)silyl]oxy}methyl)-3H-imidazo[4,5-c]pyridin-3-yl]-3-{(1R)-1-[2-(trifluoromethyl)phenyl]ethoxy}thiophene-2-carboxylate and 1.3 l of a 7 N solution of ammonia in methanol is stirred in an autoclave at 125° C. for 4 hours. The reaction mixture is concentrated to dryness and the resulting residue is purified by flash chromatography [silica gel, eluent: toluol/dioxane, elution gradient of 7/3 (v/v) to 1/1 (v/v)] to yield the title product.

Provenance & Evidence