Patent ID: 8466275
Filing Date: 2013-06-18
Classification: C07H,Y02P

Abstract:
1. A method for producing 2-chloro-2′-deoxyadenosine comprising the steps of: (a) converting the 6-oxo group of a 2′-deoxyguanosine compound having the formula into a 6-leaving group selected from (alkyl, substituted alkyl, cycloalkyl, aryl or substituted aryl)-sulfonyl, -phosphoryl, and -phosphonyl, wherein substituted alkyl is fluoroalkyl and substituted aryl is aryl substituted with alkyl, and wherein R is a protecting group selected from acyl, silyl, amide, and benzyl; (b) replacing the 2-amino group with a 2-chloro group in a diazotization/chloro-dediazoniation reaction; (c) replacing the 6-leaving group with a 6-amino group; and (d) removing the R protecting groups, to produce 2-chloro-2′-deoxyadenosine.