Method for preparing novel agomelatine key intermediates
A compound and methoxy technology, applied in the field of intermediates for the preparation of agomelatine, can solve the problems of reduced total yield, difficulty in implementation, and difficulty in reproducing, and achieves low cost, simplified process and high yield Effect
Active Publication Date: 2010-09-29
万全万特制药江苏有限公司
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Problems solved by technology
The formula (II) obtained by the above method is purified and then carried out in the next step, so that a large amount of products are lost in the purification process, resulting in a greatly reduced overall yield
And used poisonous allyl methacrylate as dehydrogenation agent in formula (II) conversion process to formula (I), not only produced a large amount of environmental pollutions, but also found that this step reaction is harmful in the actual operation process Yields are extremely low and sometimes difficult to reproduce
The synthesis of (7-methoxy-1-naphthyl) acetonitrile was reported in US5194614, which involved six reaction steps to obtain the target compound, and when converted to industrial scale, it was soon found difficult to implement the method
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Abstract
The present invention relates to a preparation method for a compound of (7-methoxyl-1-naphthyl) acetonitrile shown by formula (I), in which a compound with formula (II) undergoes dehydrogenation in melted condition under high temperature, the products of which is separated to obtain the compound with the formula (I), which is the important intermediate used to prepare Agomelatine.
Description
technical field The invention relates to a preparation method of (7-methoxy-1-naphthyl)acetonitrile, which can be used as an intermediate for preparing agomelatine. Background technique Agomelatine is mainly used for the treatment of diseases of the melatoninergic system. It is active in the treatment of jet lag-induced insomnia and fatigue, appetite disorders and obesity and has valuable pharmacological properties. Therefore, the development of agomelatine will bring better economic and social benefits, and its chemical structural formula is as follows: agomelatine The compound represented by formula (I) is an important intermediate for the synthesis of agomelatine. The conventional method of synthetic compound (I) is reported in the patent CN1680284, as shown in the following formula: 7-Methoxy-1-tetralone (II) (I) The method first reacts with cyanoacetic acid to generate an intermediate formula (II) compound by 7-methoxy-1-tetralone, and the intermediate ...
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IPC IPC(8): C07C255/37C07C253/30
Inventor 杨利民卢文
Owner 万全万特制药江苏有限公司