Process for the preparation of cladribine
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.
ScinoPharm Taiwan, Ltd.
C C
C07H C07H
inventional inventional
Lijun Guodong Yung Fa Xiaoheng Julian Paul
Mei Chu Chen Zhang Henschke