Scinopharm Taiwan, Ltd.

Scinopharm (kunshan) Biochemical Technology Co., Ltd.

Lijun Mei

Xiaoheng Zhang

Julian Paul Henschke

Yung Fa Chen

Yung-Fa Chen

Guodong Chu

Jianbo Yu

Kun Hu

Chu Guodong

The present invention provides novel processes for the preparation of regadenoson having the formula (I). In some embodiments, the intermediates for the synthesis of regadenoson are also provided. 

Process for the preparation of regadenoson

A process for making clofarabine comprising: fluorinating a compound of formula VII wherein each Ris independently a hydroxy protecting group, ORis a leaving group, with a fluorinating agent in the presence of guanidine carbonate to give a compound of formula VIII: 

Preparation of 2-chloro-9-(2'-deoxy-2&#x2032;-fluoro-&#x3b2;-D-arabinofuranosyl)-adenine

A method for producing a &#x3b2;-enriched protected decitabine comprising:

Synthesis of decitabine

A method of making cladribine with an increased purity comprising:

Process of making 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 &#x3b2;-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.

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Taihe County, China

Lijun Mei