Patent ID: 7767831
Filing Date: 2010-08-03
Classification: A61P,C07C,C07D,Y02P

Abstract:
1. A process for the manufacture of a compound of the formula III, wherein R is hydrogen, alkyl or alkoxyalkyl; R R R PG is an amino protecting group, especially one removable by hydrolysis, e.g. lower alkoxycarbonyl, such as tert-butoxycarbonyl or benzyloxycarbonyl; or a salt thereof; said process comprising reacting a compound of the formula I, wherein R, R 1 , R 2 , R 3 and PG are as defined for a compound of the formula III, with a reagent able to transform hydroxy in formula I into X where X is a group other than hydroxy or hydrogen, especially a leaving group, especially a reagent selected from a hydrohalic acid, a thionyl halogenide, PX* 3 , POX* 3 , PX* 5 , POX* 5 wherein X* is a halogennide, a combination of triphenylphosphine and halogen, and an active derivative of an organic sulfonic acid.