Study On The Synthesis Of Novel 5-HT_1A Receptor Agonist (±) Flesinoxan

The mechanism of depression and the development of antidepressants were reviewed briefly, and the research of Flesinoxan, a full 5-HT1A receptor agonist, was summarized in detail.Flesinoxan, which not only inhibits serotonergic neurons but also elicits an (possibly related) increase in VTA dopaminergic output, trails for potential use as an anxiolytic and for the treatment of depression in phase III clin.In this paper, ( ) Flesinoxan was synthesized via a ten-step process starting with catechol and p-fluorobenzoic acid, and was certified by 'HNMR, 13CNMR, IR and MS. The synthetic procedure of the intermediates was studied carefully and optimized in order to reduce the cost and make the operation easy. The overall yield of the main eight steps of reaction was raised to 18%.KEY WORDS: 5-HT_1A receptor agonist; Flesinoxan; antidepressant; synthesis...