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Zhejiang Jiuzhou Pharmaceutical Co., Ltd.

Zhejiang Jiuzhou Pharma Science & Technology Co., Ltd.

Pucha Yan

Daqing Che

Yuanqiang Li

Bin Zhang

Kang Zhen Chen

Xianyi Zhang

Hongjun Gao

Xiangdong Zhang

Xiaowei Hu

Yongliang Yan

Kang Chen

The present invention relates to the technical field of organic chemistry, specifically an asymmetrical hydrogenation of an &#x2202;-ketonic acid compound, the technical proposal being as shown by the following formula:  Wherein Ris a phenyl, a substituted phenyl, a naphthyl a substituted naphthyl, a C-Calkyl or aralkyl, the substitute is a C-Calkyl, a C-Calkoxy, a halogen, the number of the substituents is 1-3. M is a chiral spiro-pyridyl amido phosphine ligand iridium complex having the following structure,  Wherein, R is hydrogen, 3-methyl, 4-Bu or 6-methyl

Asymmetrical hydrogenation reaction of ketonic acid compound

Disclosed are a silodosin intermediate and a preparation method thereof. The silodosin intermediate has the structure shown by the formula (A). X is hydrogen or bromide and Ris hydrogen. The formyl group may be a group having the structure shown by the formula I. Ris a protecting group of carboxyl, and Ris 3-hydroxypropyl or a group having the structure shown by the formula II. W is a protecting group of hydroxyl. A compound of the formula (A) according to the present invention may further be used for preparing a compound having the structure shown by the formula (D). By means of the intermediate and the preparation method therefor provided by the present invention, high-purity optically pure silodosin can be obtained, and the optical purity is above 99%. 

Silodosin intermediate and preparation method therefor

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Taizhou, China

Pucha Yan