Zhejiang Huahai Pharmaceutical Co., Ltd.

Shanghai Syncores Technologies Inc. Ltd.

Yusheng Wang

Luning Huang

Jian Hong

Eric Gu

Boyu Wang

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. 

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Shanghai, China

Yusheng Wang