Julian Paul Henschke,Xiaoheng Zhang,Guodong Chu,Lijun Mei,Yung Fa Chen
申请号：
US12857939
公开号：
US08232387B2
申请日:
2010.08.17
申请国别(地区):
US
年份:
2012
代理人:
摘要：
A process for the preparation of cladribine of API grade is provided by direct coupling of O-protected 2-deoxy-ribofuranose with silylated 2-chloroadenine followed by deprotection of the resultant protected nucleoside in a separate step and then a purification step. Following the coupling, the desired N-9-glycosylated β-anomer of the nucleoside is directly isolated as a solid from the coupling reaction mixture by filtration in relatively high purity and yield, and it does not require purification.
