| 摘要 |
ABSTRACT - 604081 The disclosure relates to a method for the preparation of agomelatine comprising the steps of: firstly dehydrating N-[2-(1-hydroxyl-7-methoxy-1,2,3,4-tetrahydro-naphthalen-1-yl)ethyl]acetamide (intermediate A) under acidic condition to produce N-[2-(7-methoxy-3,4-dihydro-naphthalen-1-yl)ethyl]acetamide (intermediate B), then reacting compound B with a dehydrogenating agent to obtain the desired agomelatine product. Also disclosed is another method for preparing agomelatine comprising the following steps: (a) reductive acylation of 2-(1-hydroxyl-7-methoxy-1,2,3,4-tetrahydro-naphthalen-1-yl)-acetonitrile (compound C) under the condition of catalytic hydrogenation and in the presence of acetic anhydride to obtain compound A; (b) dehydration and aromatization of the compound A with a dehydrogenating agent, to obtain the desired agomelatine product. |
