Zhejiang Jiuzhous Pharmaceutical Co., Ltd.

Zhejiang Jiuzhou Pharmaceutical Co., Ltd.

Novartis Ag

Jie Ying

Guoliang Zhu

Lijun Yang

Ying Lin

Jian Zhang

Qingdan Yao

The invention relates to a novel process, novel process steps and novel intermediates useful in the synthesis of pharmaceutically active compounds, in particular neutral endopeptidase (NEP) inhibitors.

Process for manufacture and resolution of 2-acylamino-3-diphenylpropanoic acid

The present invention relates to Sitagliptin intermediate and preparation method and use thereof. The method comprises reacting compound of formula (II) and trifluorobromobenzene with a Grignard reagent by a Grignard reaction to obtain a compound of formula (I). Compound of formula (I) is a new intermediate compound for the synthesis of Sitagliptin. Compound of formula (I) can be easily used for preparing another important intermediate compound of formula (V) for the synthesis of Sitagliptin. The structures of the compounds mentioned above are as the following: 

Sitagliptin intermediates, preparation methods and uses thereof

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Zhejian, China

Jie Ying