A Scalable Synthesis of the Antidepressant Agomelatine by a Tandem Allylic Chlorination-Isomerization Process

摘要

A concise, scalable, and industrially applicable process for the synthesis of the antidepressant agomelatine is described. The process relies on a tandem allylic chlorination-isomerization sequence, on a tetralone-derived allyl carbinol, as the key transformation. The target compound is obtained in five steps from commercially available 7-methoxy-1-tetralone, in 52.3% overall yield after final recrystallization.