CO6592020A2 - Agomelatine intermediates and method of preparation of these - Google Patents

Agomelatine intermediates and method of preparation of these

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Publication number
CO6592020A2
CO6592020A2 CO12221476A CO12221476A CO6592020A2 CO 6592020 A2 CO6592020 A2 CO 6592020A2 CO 12221476 A CO12221476 A CO 12221476A CO 12221476 A CO12221476 A CO 12221476A CO 6592020 A2 CO6592020 A2 CO 6592020A2
Authority
CO
Colombia
Prior art keywords
agomelatine
preparation
intermediate compounds
present
intermediates
Prior art date
Application number
CO12221476A
Other languages
Spanish (es)
Inventor
Peng Zhang
Yu Huang
Zhedong Yuan
Hanbin Shan
Xiong Yu
Original Assignee
Servier Lab
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Servier Lab filed Critical Servier Lab
Priority to CO12221476A priority Critical patent/CO6592020A2/en
Publication of CO6592020A2 publication Critical patent/CO6592020A2/en

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  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

La presente invención se refiere a los compuestos intermedios para la preparación de agomelatina, así como a los métodos de preparación de éstos. El intermedio de la presente invención para la preparación de agomelatina es el compuesto A corno se muestra en la fórmula siguiente. También se proporcionan dos compuestos intermedios nuevos. Cuando se usan estos compuestos intermedios nuevos para preparar agomelatina, es sencillo de manipular, bien controlado y con alta pureza, sin operaciones complicadas tales como rectificación y separación por cromatografía en columna, y adecuado para la producción industrial. Por otro lado, los métodos de preparación de los dos intermedios nuevos en sí mismos son sencillos y con alto rendimiento, usando sólo la usada muy comúnmente 7- metoxi-tetralona como material de partida original y que experimenta una etapa de reacción para obtener los intermedios, seguido de una etapa más para convertir los compuestos intermedios en el producto deseado agomelatina. Dichos procesos de reacción están muy simplificados, mejorándose el rendimiento de la reacción y superando la dificultad de purificación del método previo, comparado con la técnica anterior para la preparación de agomelatina. Típicamente, el rendimiento de la presente invención es mayor del 70%.The present invention relates to the intermediate compounds for the preparation of agomelatine, as well as to the methods of preparing them. The intermediate of the present invention for the preparation of agomelatine is compound A as shown in the following formula. Two new intermediate compounds are also provided. When these new intermediate compounds are used to prepare agomelatine, it is simple to handle, well controlled and with high purity, without complicated operations such as rectification and separation by column chromatography, and suitable for industrial production. On the other hand, the methods of preparing the two new intermediates themselves are simple and high yielding, using only the very commonly used 7- methoxy-tetralone as the original starting material and experiencing a reaction step to obtain the intermediates , followed by a further step to convert the intermediate compounds into the desired agomelatine product. Said reaction processes are very simplified, improving the yield of the reaction and overcoming the difficulty of purification of the previous method, compared with the prior art for the preparation of agomelatine. Typically, the yield of the present invention is greater than 70%.

CO12221476A 2012-12-06 2012-12-06 Agomelatine intermediates and method of preparation of these CO6592020A2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CO12221476A CO6592020A2 (en) 2012-12-06 2012-12-06 Agomelatine intermediates and method of preparation of these

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
CO12221476A CO6592020A2 (en) 2012-12-06 2012-12-06 Agomelatine intermediates and method of preparation of these

Publications (1)

Publication Number Publication Date
CO6592020A2 true CO6592020A2 (en) 2013-01-02

Family

ID=49110908

Family Applications (1)

Application Number Title Priority Date Filing Date
CO12221476A CO6592020A2 (en) 2012-12-06 2012-12-06 Agomelatine intermediates and method of preparation of these

Country Status (1)

Country Link
CO (1) CO6592020A2 (en)

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