Patent ID: 6620941
Filing Date: 2003-09-16
Classification: A61P,C07D

Abstract:
A process for the preparation of a compound of formula V, wherein R1 is aryl or heteroaryl, and R2 is lower alkyl, aryl or trifluoromethyl; comprising converting a compound of formula VI wherein R3 is lower alkyl, to a compound of formula VIII, wherein R3 is as above, and R4 is lower alkyl, lower-alkyl-carbonyl, lower-alkoxy-carbonyl, aryl-carbonyl, P(O)(OR5)2, or Si(R6)3, wherein each R5 independently represents lower alkyl or aryl, and each R6 independently represents lower alkyl or aryl; brominating the compound of formula VIII to yield a compound of formula X, wherein R3 and R4 are as above, subsequently condensing of the compound of formula X with an amide R1C(O)NH2, wherein R1 is as above, to obtain a compound of formula VII, wherein R1 and R3 are as above, reducing the compound of formula VII to convert the ester group to a corresponding alcohol, and subsequently introducing a â€”SO2R2 group, wherein R2 is as above, to yield said compounds of formula V.