Acetylaniline compounds and application thereof in preparation of mirabegron

Abstract

The invention discloses a new intermediate (R)-N-(4-amino phenethyl)-2-hydroxy-2-acetylaniline for preparing mirabegron, and a method for preparing the mirabegron through the intermediate. The method is simple and convenient to operate, has low cost, and is applicable to industrial production.

Description

technical field

[0001] The present invention relates to a new preparation method of Mirabegron, in particular to a new intermediate (R)-N-(4-aminophenethyl)-2-hydroxyl-2-phenylacetamide or its salt, and its Application in the synthesis of mirabegron. Background technique

[0002] Mirabegron is a selective β3-adrenergic receptor agonist, which is mainly used clinically for the treatment of overactive bladder in adults. Its chemistry is: (R)-2-(2-amino-1,3-thiazol-4-yl)-4'-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]benzene Acetamide has the following structural formula:

[0003]

[0004] Mirabegron tablet was developed by Japan Astel-las pharmaceutical company, and was listed in Japan on September 16, 2011, and was approved by the FDA on June 28, 2012 for the treatment of adult overactive bladder ( OAB), trade name Myrbetriq.

[0005] The synthetic method of mirabegron in the prior art mainly contains following several kinds:

[0006] Method 1: The synthesis method of mi...

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