Scinopharm Taiwan, Ltd.

Scinopharm (Kunshan) Biochemical Technology Co., Ltd.

Scniopharm Taiwan, Ltd.

University of Michigan

Scinopharm Biochemical Technology Co., Ltd.

Julian Paul Henschke

Jason Christopher Rech

Yung-Fa Chen

Xiaoheng Zhang

Yung Fa Chen

Yuanlian Liu

Lijun Mei

Ping-Yu Wu

TsungYu Hsiao

LungHu Wang

Tsung-Yu Hsiao

Lei Zhang

Jyh-Hsiung Liao

YuanChang Huang

MengFen Ho

Lizhen Xia

Chen-Wei Lin

Guodong Chu

Xin Huang

Yue Chen

Shu-Ping Chen

Tsung Yu Hsiao

Meng-Fen Ho

Dechao Meng

Hsyueh-Liang Wu

Mukesh K Nyati

Ting Sun

Wen-Hsien Wen

HsinChang Tseng

George Charles Schloemer

Chu Guodong

ChunFang Xu

Aiping Xie

Kun Hu

Jianbo Yu

Yong Mu

YiJing Chen

Chi-Nung Hsiao

Yungfa Chen

This invention provides a novel method for the preparation of 2,3-disubstituted -4-oxy-cyclopentan1-one compounds that are useful for the synthesis of prostaglandins and prostaglandin analogs of industrial relevance. The method comprises the metal-catalyzed asymmetric 1,4-conjugate addition of vinylboron compounds to 2-substituted -4-oxy-cyclopent-2-en-1-ones. This method relies on the use of less toxic, easily-handled reagents, and can be performed under milder conditions than offered by some conventional methods, affording 2,3-disubstituted-4-oxy-cyclopentan-1-one compounds enantio- and diastereoselectively, which are precursors to the said prostaglandin and prostaglandin analogs, in high yield.

Metal-catalyzed asymmetric 1,4-conjugate addition of vinylboron compounds to 2-substituted-4-oxy-cyclopent-2-en-1-ones yielding prostaglandins and prostaglandin analogs

The present application discloses a stereoselective process for the preparation of &#x3b2;-C-arylglucosides that does not require the use of conventional carbohydrate protecting groups. In one embodiment, the stereoselective process comprises the preparation of the compound of formula I: the process comprising: a) contacting 1,6-anhydro-&#x3b2;-D-glucopyranose with a compound of formula II, RRRAl, in a solvent to form a first reaction mixture; b) contacting the first reaction mixture of step a) with a second reaction mixture to form a third reaction mixture, wherein the second reaction mixture is prepared by contacting an organoaluminum compound of formula III, RRAlX, with a compound of formula IV, ArM; and c) contacting the third reaction mixture with a reagent to form the compound of the formula I.

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The present invention relates to a novel process of making ixabepilone, ixabepilone derivatives and analogues, and intermediates thereof.

Process for ixabepilone, and intermediates thereof

Intermediates of the following formulae for the preparation of lubiprostone: 

Intermediates for the preparation of lubiprostone

The present invention provides amorphous forms and the crystalline complexes of SGLT2 inhibitors as a novel material, in particular in pharmaceutically acceptable form. The crystalline forms of SGLT2 inhibitor canagliflozin are designated as Forms CS1, CS2, CS3, CS4 and CS5.

Crystalline and non-crystalline forms of SGLT2 inhibitors

The present invention provides processes (e.g., arylation reaction) for stereoselectively preparing C-arylglucosides that can be useful as synthetic building block or drugs, including SGLT2 inhibitors. A representative process of the present application includes the preparation of the compound of formula IV starting from a compound of the formula II with a metalated aryl compound, as disclosed below: 

Process for the preparation of &#x3b2;-C-aryl glucosides

The present invention provides efficient and economical methods for synthesis of (&#x2212;)-2-exo-morpholinoisoborne-10-thiol, its enantiomer, and related chiral catalysts. Novel compounds and methods of asymmetric synthesis are also disclosed.

Process for the manufacture of chiral catalysts and their salts

Processes for preparing and purifying lubiprostone are disclosed. Intermediates and preparation thereof are also disclosed.

Process for the preparation of lubiprostone

The present invention provides for synthetic processes for the making of substituted 3-((pyrrol-2-yl)methylene)-2-pyrrolones, including sunitinib. The present invention also provides for a process of crystallizing substantially pure sunitinib L-malate.

Processes for the preparation of 3-(pyrrol-2-yl)methylene)-2-pyrrolones using 2-silyloxy-pyrroles

A process for preparing a prostaglandin analogue comprising a step of converting a compound of formula (8'): to the prostaglandin analogue, wherein Rrepresents hydrogen or a hydroxyl protecting group.

Process for the preparation of prostaglandin analogues

The present invention provides crystalline forms, including an anhydrate form, of cabazitaxel and processes for the preparation of these forms, designated as Forms C1, C2, C3, C4, C5, C6, C7, C8, C8b, C9 and C9p.

Crystalline forms of cabazitaxel

The present invention relates to processes for making cabazitaxel, cabazitaxel analogues and intermediates thereof. The invention provides novel compounds useful in the synthesis of cabazitaxel.

Process for cabazitaxel, and intermediates thereof

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:

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Summertown, Australia

Julian Paul Henschke