Scinopharm Taiwan, Ltd.

Scinopharm (changshu) Pharmaceuticals, Ltd.

Scinopharm (kunshan) Biochemical Technology Co., Ltd.

Xiaoheng Zhang

Julian Paul Henschke

Lijun Mei

Yung-Fa Chen

Yung Fa Chen

Guodong Chu

LungHu Wang

Yuanlian Liu

Kun Hu

Chu Guodong

Jianbo Yu

Yong Mu

ChunFang Xu

YiJing Chen

Xizhou Lv

Julian Pual Henschke

Lunghu Wang

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 concise, efficient and cost- and time-saving process for the preparation of a quinazoline derivative of formula A given below: which is an intermediate for making gefitinib or gefitinib itself, comprising reacting a compound of Formula B: with 3-chloro-4-fluoroaniline (VI) in the presence of a N,N-dialkyl formamide acetal, a Bronsted acid catalyst, and a solvent in a one-pot reaction.

Process of preparing a quinazoline derivative

A compound of formula (X): which can be used as an intermediate to make lapatinib or its pharmaceutically acceptable salt.

Process and intermediates for preparing lapatinib

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

The present invention provides a process for making lapatinib and its pharmaceutically acceptable salt by use of new intermediates. A new process for obtaining a pharmaceutical form of lapatinib ditosylate monohydrate is also provided.

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.

Process for the preparation of cladribine

A process of synthesizing a 5-azacytosine nucleoside, such as azacitidine and decitabine, comprises coupling a silylated 5-azacytosine with a protected D-ribofuranose of formula in the presence of a sulfonic acid catalyst.

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Lianyungang, China

Xiaoheng Zhang