Patent ID: 6686463
Filing Date: 2004-02-03
Classification: C07H

Abstract:
A method for synthesizing a compound of Formula I: wherein R1 and R2 are independently hydrogen, NR10R11, (NR10R11)alkyl, alkyl, fluoro or chloro, wherein R10 and R11 are independently hydrogen, alkyl, alkanoyl, acyl, alkoxy, or arylalkyl optionally substituted with up to three groups that are independently halogen, alkoxy, nitro, or alkyl; and R3 is independently alkyl, alkoxyalkyl, alkyl-thio-alkyl, cyanoalkyl, or arylalkyl optionally substituted with up to three groups that are independently halogen, alkoxy, nitro, or alkyl; comprising:a) introducing a 5â€²,3â€²-bridging silyl protecting group to a compound of Formula II, wherein R1 and R2 are as defined in Formula I, to yield a compound of Formula III; wherein R1 and R2 are as defined in Formula I and each R4 is independently alkyl, aryl or isoalkyl; b) alkylating the product of step (a) to yield a compound of Formula IV; wherein R1, R2 and R3 are as defined in Formula I and R4 is as defined in Formula III; and c) deprotecting the product of step (b) to yield a compound of Formula I.