A kind of preparation method of zolmitriptan intermediate

Abstract

The invention belongs to the technical field of organic synthesis, and in particular relates to a preparation method of a zolmitriptan intermediate. The present invention takes (S)-4-(4-nitrobenzyl)-2-oxazolidinone as raw material, adopts palladium carbon and ammonium formate to react with it, and prepares zolmitriptan intermediate (S)- 4‑(4‑aminobenzyl)‑2‑oxazolidinone. The invention adopts ammonium formate and palladium charcoal for reduction, has low reaction temperature, simple post-treatment, is environmentally friendly, and the catalyst can be recycled and used mechanically. Adopting the present invention, the yield is above 95%, and the purity is above 98%.

Description

technical field

[0001] The invention belongs to the technical field of organic synthesis, and in particular relates to a preparation method of a zolmitriptan intermediate. Background technique

[0002] Zolmitriptan, chemical name (S)-4-[3-[2-(dimethylamino)ethyl]-1H-indole-5-methyl]-2-oxazolidinone, is An anti-migraine drug developed by Glaxo-Wellcome in Germany, it is a highly selective serotonin (5-TH1B and 5-TH1D) receptor agonist, which stimulates intracranial blood vessels (including arteriovenous anastomosis) ) and 5-HTIB / ID receptors on the sympathetic nerves of the trigeminal nervous system, constrict blood vessels and inhibit the release of neuropeptides to relieve migraine attacks. At present, it has been listed in the United Kingdom, the United States and other countries, and the market prospect is good.

[0003] (S)-4-(4-aminobenzyl)-2-oxazolidinone is an important intermediate in the synthesis of zolmitriptan. At present, (S)-4-(4-aminobenzyl)-2-oxazolidinone...

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