Scinopharm Taiwan, Ltd.

Scinopharm (kunshan) Biochemical Technology Co., Ltd.

Scniopharm Taiwan, Ltd.

Yung Fa Chen

Julian Paul Henschke

Xiaoheng Zhang

LungHu Wang

Lijun Mei

Xin Huang

Guodong Chu

Chu Guodong

George Charles Schloemer

Aiping Xie

Julian Pual Henschke

Lunghu Wang

A synthetic process for producing bortezomib comprising converting racemic boronic esters, such as the pinacol &#x3b1;-aminoboronic ester, into mixtures of diastereomers [6] by reaction with a suitably protected L-phenylalanine derivative (see Scheme 3), such as N&#x2014;BOC-L-phenylalanine. The protecting group of the L-phenylalanine moiety is then removed, such as by reacting the diastereomers [6] with an acid, such as hydrochloric acid, to form a mixture of amine salt diastereomers [7] which is then subjected to conditions under which the desired diastereomer (R,S)-[7] is selectively isolated, such as by crystallization, chromatography or stereoselective hydrolysis. The separated desired diastereomer (R,S)-[7] is then converted into bortezomib or bortezomib anhydride.

Process for preparing and purifying bortezomib

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.

Process for making 5-azacytosine nucleosides and their derivatives

A compound of formula (A) or salt thereof: 

Process of making 2-deoxy-2,2-difluoro-D-ribofuranosyl nucleosides and intermediates therefor

A novel process for the preparation of N-methyl-N-(2-[4-hydroxyphenyl]ethyl)-5-hydroxy-4-methoxy benzene carboxamide, which is useful as an intermediate in the synthesis of (&#x2212;)-galantamine, comprises the reaction of a 5-hydroxy-4-methoxy benzoic acid derivative with N-methyl-N-(2-[4-hydroxyphenyl]ethyl) amine.

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Chiali, Taiwan

Yung Fa Chen