Preparation method of high-purity ramelteon

A ramelteon, high-purity technology, applied in the field of preparation of high-purity ramelteon, can solve the problems of affecting the total yield of the process and product quality, increasing production costs, difficulties, etc., to achieve the suppression of the formation of impurity VIII, Reduced purification pressure and high reaction yield
CN106588840AActive Publication Date: 2017-04-26YANGTZE RIVER PHARM GRP CO LTD
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
YANGTZE RIVER PHARM GRP CO LTD
Publication Date
2017-04-26

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Abstract

The invention discloses a preparation method of high-purity ramelteon. The preparation method comprises the following steps: taking 1,2,6,7-tetrahydro-8H-indene[5,4-b]furan-8-ketone as a starting material; carrying out reduction and amino protection through wittig-horner reaction; carrying out amino deprotection under an acidic condition; carrying out hydrogenation reaction; then carrying out chiral resolution and acrylation reaction, thus obtaining the ramelteon. The ramelteon obtained through the invention is high in product purity and higher in yield; and formation of impurities is inhibited.
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Description

technical field

[0001] The invention belongs to the field of medicinal chemistry, and in particular relates to a preparation method of high-purity ramelteon, wherein the formation of impurities is suppressed. Background technique

[0002] Ramelteon, chemical name (S)-N-(2-(1,6,7,8-tetrahydro-2H-indeno(5,4-b)furan-8-yl)ethyl)propane Amide, a melatonin receptor agonist developed by Takeda Corporation of Japan, can selectively act on MT1 and MT2 receptors. It was approved by the US FDA in 2005 for the treatment of insomnia characterized by difficulty falling asleep. Ramelteon has no affinity for GABA receptors, acetylcholine receptors, and opioid receptors. It has a completely different mechanism of action from traditional sedative-hypnotics, and has a long acting time and few adverse reactions. Obviously addictive, it is the first sedative-hypnotics listed as special control.

[0003] The main structure of ramelteon is the indenofuryl ethylamine part, followed by the propion...

Claims

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