主权项 |
1. A process for the preparation of a compound of formula (I) wherein b is an integer from 0 to 4; each R5 is independently selected from the group consisting of halogen and C1-4alkyl; and pharmaceutically acceptable salts thereof; comprising reacting a mixture of a compound of formula (V) and a compound of formula (VI), wherein R1 is selected from the group consisting of C1-4alkyl, C2-4alkenyl, substituted aryl, aralkyl, heteroaryl, —O—C1-4alkyl, —O—C2-4alkenyl, —O— (substituted aryl), —O-aralkyl and —O-heteroaryl, with a base; in an organic solvent or mixture of solvents; at a temperature in the range of from about −10° C. to about 25° C.; to yield a mixture of the corresponding compound of formula (VII-a) and the corresponding compound of formula (VII-b), wherein Cation+ is the corresponding base cation; reacting the mixture of the compound of formula (VII-a) and the compound of formula (VII-b) with a compound of formula (IX), an (R)-glycidyl-(substituted aryl)sulfonate wherein R2 is selected from the group consisting of hydrogen, halogen, methyl, ethyl, nitro, cyano and dichloro; to yield a mixture of the corresponding compound of formula (VIII-a) and the corresponding compound of formula (VIII-b); reacting the mixture of the compound of formula (VIII-a) and the compound of formula (VIII-b) with an aqueous base or a mixture of an aqueous base and an alcohol; in an organic solvent or mixture of organic solvents; at a temperature in the range of from about −10° C. to about 25° C.; to yield the corresponding compound of formula (I). |