The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.

The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.

Date of Patent:
Jul. 15, 2014

Filed:

Jun. 08, 2011
Applicants:

Peng Zhang, Shanghai, CN;

Yu Huang, Shanghai, CN;

Zhedong Yuan, Shanghai, CN;

Hanbin Shan, Jiangxi province, CN;

Xiong Yu, Shanghai, CN;

Inventors:

Peng Zhang, Shanghai, CN;

Yu Huang, Shanghai, CN;

Zhedong Yuan, Shanghai, CN;

Hanbin Shan, Jiangxi province, CN;

Xiong Yu, Shanghai, CN;

Assignee:

Les Laboratoires Servier, Suresnes Cedex, FR;

Attorney:
Primary Examiner:
Int. Cl.
CPC ...
C07C 233/22 (2006.01); C07C 231/06 (2006.01); C07C 233/18 (2006.01); C07C 231/12 (2006.01);
U.S. Cl.
CPC ...
C07C 231/06 (2013.01); C07C 233/18 (2013.01); C07C 2102/10 (2013.01); C07C 233/22 (2013.01); C07C 231/12 (2013.01);
Abstract

The present invention relates to the intermediate compounds for preparation of agomelatine, as well as the preparation methods thereof The intermediate of the present invention for preparation of agomelatine is compound A as shown in the following formula. Also provided are two novel intermediate compounds. When we use these new intermediate compounds to prepare agomelatine, it is simple to manipulate, well-controlled and with high purity, without complicated operations such as rectification and column chromatography separation, and suitable for industrial production. Meanwhile, the preparation methods of the two new intermediates themselves is simple and high yield, only using the most commonly-used 7-methoxy-tetralone as original starting material and undergoing one step of reaction to obtain the intermediates, followed by one more step of converting the intermediate compounds to desired product agomelatine. Said reaction processes are greatly simplified, with the reaction yield being improved and the difficulty in purification of previous method being overcome, as compare with the previous technique for preparation of agomelatine. Typically, the yield of the present invention is over 70%.


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