Hanmi Pharm. Co., Ltd.

Hoe Chul Lee

Gwan Sun Lee

Jae Chul Lee

Young-Kil Chang

Jaeheon Lee

Han Kyong Kim

Moonsub Lee

Gha Seung Park

Hyo-Jeong Bang

Cheol Kyong Kim

Chang-Ju Choi

Provided is an improved method for stereoselectively preparing 2'-deoxy-2&#x2032;,2&#x2032;-difluorocytidine of formula (I), which includes reacting a 1-halo ribofuranose compound with a nucleobase of formula (IV) in a solvent to obtain a nucleo side of formula (II) with removal of a silyl halide ((alkyl)SiX (X=halide)); and deprotecting the nucleoside of formula (II) to obtain 2&#x2032;-deoxy-2&#x2032;,2&#x2032;-difluorocytidine of formula (I). 2&#x2032;-Deoxy-2&#x2032;,2&#x2032;-difluorocytidine of formula (I) is effective for treating various cancers such as non-small cell lung (NSCLC), pancreatic, bladder, breast or ovarian cancers. 

Method for the preparation of 2'-deoxy-2&#x2032;,2&#x2032;-difluorocytidine

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Yongin-si, South Korea

Hoe Chul Lee