The Antimigraine Drug Succinate Sumatriptan Synthesis Process

The mechanisms of migraine and clinical anti-migraine drugs in common use were reviewed briefly, and the research of triptans, a class of anti-migraine drug, was summarized in detail. Sumatriptan , developed and brought into the Holand market by Glaxo, was the first triptan used in acute migraine treatment. As a 5-HT_1B/1D receptor agonist, sumatriptan have dual effects, which cause selective cranial vasoconstriction, mediated via stimulation of vascular 5-HT_1B receptor and simultaneously restrict the release of neuropeptides by stimulate presynaptic 5-HTid receptor in trigeminal twig that induce neurogenic inflammation.Based on the literature several synthetic routes of Sumatriptan succinate were compared and analyzed to selective a reasonable route.In this paper, it was synthesized via a eleven-step procedure starting with p-nitrobenzylchloride, and was identified by ¹H-NMR, IR and MS. The synthetic process of the intermediates was studied carefully and optimized in order to reduce the cost and make the operation easy. By using "one-pot" reaction twice, the overall yield of the reaction reach to 14%.