N-protected-3,5-disubstituted indole derivative and its preparation method and application

A technology of indole derivatives and disubstitution, applied to N-protection-3, which can solve the problems of harsh reaction conditions, expensive reagents, unfavorable large-scale production, etc., and achieve the effect of shortening the reaction steps, not easy to store, and easy to operate
CN102775392BInactive Publication Date: 2015-11-18SHANGHAI INST OF PHARMA IND CO LTD
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
SHANGHAI INST OF PHARMA IND CO LTD
Publication Date
2015-11-18
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention provides an N-protection-3, 5-disubstituted indole derivative, its preparation method and application. The N-protection-3, 5-disubstituted indole derivative can be used for preparing the anti-migraine drug Almotriptan. Compared with reported literature, the preparation method provided in the invention has the advantages of: cheap and easily available raw materials, mild reaction conditions, simple operation, greatly shortened reaction steps, quality controllable and high purity product, less pollution of ''three wastes'', and easy industrial production. The N-protection-3, 5-disubstituted indole derivative is a free alkali or salt of the compound having a structural general formula (I).
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Description

technical field

[0001] The present invention relates to N-protected-3,5-disubstituted indole derivatives and their preparation methods and applications. 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. 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).

[0003] 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 produce vasocons...

Claims

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