Patent ID: 6777560
Filing Date: 2004-08-17
Classification: A61P,C07D

Abstract:
A process for the preparation of a compound of formula (I) comprising:(a) contacting in a solvent a compound of formula (II) with a transition metal catalyst, a hydrogen source, and a base wherein the base is selected from the group consisting of NaOH and an anune base, to give a compound of formula (III): wherein R1 is defined as â€”XR, wherein X is O, S, or Se, or â€ƒwherein R2 and R3 are independently alkyl, cycloalkyl, arylalkyl, or aryl, or R2 and R3 taken together are â€”(CH2)4â€”, â€”(CH2)5â€”, â€”(CH(R4)â€”CH2)3â€”, â€”(CH(R4)â€”CH2)4â€”, â€”(CH(R4)â€”(CH2)2â€”CH(R4))â€”, â€”(CH(R4)â€”(CH2)3â€”CH(R4))â€”, â€”CH2â€”CH2â€”Aâ€”CH2â€”CH2â€”, â€”CH(R4)â€”CH2â€”Aâ€”CH2CH2â€”, â€”CH(R4)â€”CH2â€”Aâ€”CH2â€”CH(R4)â€”, wherein R4 is alkyl of from one to four carbon atoms, A is O, S, or N and R is defined as alkyl, aryl, arylalkyl, or heteroaryl; (b) conversion of the compound of formula (III) wherein R1 is as defined above to a compound of formula (IV) using base in aqueous methanol or aqueous THF; and (c) contacting in a solvent the compound of formula (IV) with an acid to afford a compound of Formula (I).