Patent ID: 7169921
Filing Date: 2007-01-30
Classification: A61P,C07D,Y02P

Abstract:
1. A process for the preparation of a compound of formula I, wherein R 1 represents H, an amino protective group or a structural fragment of formula Ia, in which R R R R R R R E represents, at each occurrence, a direct bond or C p represents 1 or 2; A represents -G-, -J-N(R B represents -Z-,-Z-N(R G represents a direct bond or C J represents C Z represents a direct bond or C R n represents 0, 1 or 2; R R R R Het R provided that: (a) when R (b) when R R wherein each aryl and aryloxy group, unless otherwise specified, is optionally substituted by one or more of —OH, cyano, halo, nitro, C which process comprises reaction of a compound of formula II, wherein as defined above, with either: (i) a compound of formula III, wherein R 16 represents unsubstituted C 1-4 alkyl, C 1-4 perfluoroalkyl or phenyl, which latter group is optionally substituted by one or more substituents selected from C 1-6 alkyl, halo, nitro and C 1-6 alkoxy, and R 2 is as defined above; or (ii) acrylamide, followed by reaction of the resulting intermediate of formula IV, wherein R 1 as defined above, with an alcohol of formula R 2 —OH and an agent that promotes, or agents that in combination promote, rearrangement and oxidation of the compound of formula IV to an intermediate isocyanate, which may then react with the alcohol of formula R 2 —OH, wherein R 2 is as defined above.