Preparation method of anti-migraine drug Almotriptan

A technology for almotriptan and migraine, which is applied in the field of preparing an anti-migraine drug almotriptan, and can solve the problems of unfavorable large-scale production, low total yield, expensive reagents and the like
CN102775342AInactive Publication Date: 2012-11-14SHANGHAI INST OF PHARMA IND CO LTD

Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
SHANGHAI INST OF PHARMA IND CO LTD
Publication Date
2012-11-14
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention provides a preparation method of an anti-migraine drug Almotriptan. The method includes the following steps of: taking an N-protection-3, 5-disubstituted indole derivative as a starting material, removing the N-protection group in a solvent and in the presence of a catalyst, and then collecting Almotriptan from the reaction system. The method provided in the invention for preparing Almotriptan has the advantages of safety, mild reaction condition, easy operation, high yield, cheap and easily available raw materials, easy ''three wastes'' treatment, and convenient industrial implementation. The N-protection-3, 5-disubstituted indole derivative has a chemical structural formula as shown in formula (I).
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Description

technical field

[0001] The invention relates to a method for preparing anti-migraine drug almotriptan. Background technique

[0002] Almotriptan (Almotriptan), the chemical name is 3-[2-(dimethylamino)ethyl]-5-(pyrrolidin-1-ylsulfonylmethyl)-1H-indole, which is Spanish Emero 5-HT developed by the company 1B / 1D Receptor agonists for the treatment of migraine with or without aura. The structural formula is as follows:

[0003]

[0004] In September 2000, the drug was launched in Spain for the first time. In May 2001, it was approved by the FDA for marketing in the United States. In 2009, the US FDA approved almotriptan for the acute treatment of migraine in adolescents (12-17 years old).

[0005] The pathogenesis of migraine is still unclear, but it has been confirmed that the large intracranial blood vessels dilate during headache, and migraine may be mainly related to the stimulation of 5-HT 1B / 1D related to the receptor. Compounds such as ergotamines and 5-HT produc...

Claims

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