Zhejiang Huahai Pharmaceutical Co., Ltd.

Shanghai Syncores Technologies Inc. Ltd.

Shanghai Aobo Pharmtech, Inc., Ltd.

Boyu Wang

Luning Huang

Eric Gu

Gang Wang

Yang Liu

Hong Gu

Jian Hong

Jinfeng Yao

Jeannie Zhang

Yinglu Jiao

Caide Tang

Handa Li

Yusheng Wang

Disclosed are a crystal form of brexpiprazole and a preparation method therefor. The X-ray powder diffraction pattern, which is detected with Cu&#x2014;K&#x3b1; radiation, of the crystal form of brexpiprazole has characteristic peaks at the positions where 2&#x3b8; is about 9.1&#xb1;0.2, 15.2&#xb1;0.2, 15.7&#xb1;0.2, 17.6&#xb1;0.2, 18.1&#xb1;0.2, 24.4&#xb1;0.2. The crystal form I of brexpiprazole has a high purity, good stability and good reproducibility, and is suitable for industrial production.

Crystal form of brexpiprazole and preparation method therefor

Disclosed is a method for synthesizing a sitagliptin intermediate, the method comprising: in the presence of hydrogen and a transition metal catalyst having a chiral phosphine ligand, subjecting a compound of formula II to an asymmetric reductive amination with ammonia or ammonium salt in a proper organic solvent under the condition of adding an acidic additive to produce a compound of formula I, wherein, an R- or S-configuration of a stereocenter is represented by *; the compound of formula I of R configuration can be used to prepare sitagliptin, and a reaction formula is as follows: Rand Rare each independently selected from hydrogen, C-Clinear or branched alkyl, C-Ccycloalkyl, C-Calkenyl, C-Calkynyl and C-Carylalkyl. The method has a high yield and a high ee % value, a mild reaction condition and a low production cost, and is simple to operate, convenient to purify, environmental friendly and suitable for industrial production. 

Method for preparing sitagliptin intermediate via asymmetrical reduction method

The present invention provides a new intermediate II and a method for synthesizing the same. The method comprises: (a) firstly diazotizing a compound of formula I as a raw material, and then halogenating to obtain an intermediate II; and (b) reacting the intermediate II with a compound III to obtain a compound IV, hydrolyzing the obtained compound IV directly without being separated to obtain Vortioxetine represented by compound V. The intermediate II can be used for synthesizing Vortioxetine. 

Vortioxetine intermediate and synthesis process thereof

The invention relates to a method for synthesizing an intermediate of Apixaban comprising reacting a compound of formula I with 5-chloro-valeryl chloride in the presence of inorganic base in an inert solvent to obtain a compound of formula II, with the reaction formula of (A), wherein R is selected from nitro group and the group (B). The method is mild in reaction condition, simple in operation, easy in purification, inexpensive in production cost, environmental-friendly, and suitable for industrial production. 

Method for synthesizing key intermediate of apixaban

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Shanghai, China

Boyu Wang