Patent ID: 7858804
Filing Date: 2010-12-28
Classification: C07D,C07F

Abstract:
1. A process of making compounds of the formula (Ia): wherein: the imidazole ring is substituted at the 4 or 5-position; R1 is chosen from cyclopropyl, phenyl and 4-(CF R2 is chosen from tert-butyl, 1-methyl-cyclopropyl, hydrogen, 1-methoxycarbonyl-1-methyl-ethyl and 2-hydroxy-1,1-dimethyl-ethyl; R3 is chosen from methoxy or hydrogen; said process comprising: L-proline, a base such as Na 2 CO 3 , a Cu(I) source such as CuI or CuSO 4 in the presence of a reducing agent such as sodium ascorbate and DMSO and subsequently adding alkyne 6, and adding a suitable solvent and water to produce triazole 9; or its hydrochloride salt, and a suitable amine base, to produce the product compound Ia: