Preparation method of Mirabegron

An intermediate, nitrophenethyl technology, applied in the preparation field of mirabegron, can solve problems such as difficulty in realizing industrialized production, difficulty in obtaining starting materials, and excessively long synthetic route, and achieves fewer steps and wider synthetic route. Prospect and industrial application value, good effect of purity
CN109456277AActive Publication Date: 2019-03-12ANHUI QINGYUN PHARMA & CHEM
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
ANHUI QINGYUN PHARMA & CHEM
Publication Date
2019-03-12

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Abstract

The invention discloses a preparation method of Mirabegron and relates to the technical field of medicine preparation. The preparation method includes the steps of subjecting R-mandelic acid and 4-nitrophenylethylamine to amide condensation reaction to obtain an intermediate (R)-N-(4-nitrophenethyl)-2-hydroxy-2-phenylacetamide, reducing amide carbonyl through diisobutyl aluminium hydride to obtainan intermediate (alphaR)-alpha-[[[2-(4-Nitrophenyl)ethyl]amino]methyl]benzenemethanol hydrochloride, reducing nitryl through a ammonium formate-Pd / C reduction system to obtain an intermediate 2-[2-(4-amino-phenyl)-ethylamino]-1-phenyl-ethanol, and finally subjecting the intermediate and (2-aminothiazole-4-yl)acetic acid to condensation reaction to obtain Mirabegron. The Mirabegron prepared by themethod has high purity and high yield; the preparation method needs fewer steps of synthesis route and mild and controllable reaction conditions, is easy and convenient in operation, low in cost andadaptable to industrial production, and has broad prospect and high industrial application value.
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Description

technical field

[0001] The invention relates to the technical field of medicine preparation, in particular to a preparation method of mirabegron. Background technique

[0002] Mirabegron was developed by Japan's Astellas Pharmaceutical Company (Astellas), and Yamanouchi Pharmaceutical Co., Ltd. applied for the compound patent of Mirabegron in Japan on October 17, 1997, and protected its preparation method. At present, it has applied for patent protection in many countries and regions such as the United States, Europe, and China. On September 16, 2011, Mirabegron was launched for sale in Japan. In June 2012, it was approved by the US FDA for listing in the United States. As the first orally effective β3 adrenergic receptor agonist drug for the treatment of overactive bladder, the successful marketing of Mirabegron has filled the gap in the treatment of overactive bladder with β adrenergic receptor agonists.

[0003] The currently disclosed synthetic routes mainly include the...

Claims

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