Improved method used for preparing ambrisentan

A technology of ambrisentan and metal carbonate, which is applied in the field of chemistry, can solve the problems of cumbersome operation, unsuitability for industrial production, and expensive resolution reagents, and achieve simplified reaction and processing steps, cheap and easy-to-obtain resolution reagents, and The effect of high yield
CN104592129AActive Publication Date: 2015-05-06山东瑞银生物工程有限公司
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
山东瑞银生物工程有限公司
Publication Date
2015-05-06

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Abstract

The invention belongs to the field of chemical synthesis, and discloses an improved method used for preparing ambrisentan. According to the improved method, 2-hydroxy-3-methoxy-3,3-diphenylpropionic ester and 4,6-dimethyl-2-methylsulfonylpyrimidine are subjected to condensation, and one-pot hydrolysis in tetrahydrofuran solvent so as to obtain ambrisentan racemate; and ambrisentan is obtained via resolution with (S)-1-phenylethylamine. The improved method is simple in operation, and high in yield, and is suitable for industrial production.
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Description

technical field

[0001] The invention relates to the field of chemistry, in particular to an improved method for preparing ambrisentan. Background technique

[0002] Ambrisentan is an endothelin receptor antagonist (ERA) originally developed by Abbott of the United States, and Myogen Corporation of the United States has acquired its global development and marketing rights. Subsequently, GlaxoSmithKline (Glaxosmithkline) of the United States signed an agreement with Myogen to obtain the production rights of this product outside the United States. On November 17, 2006, Gilead Science of the United States acquired Myogen as a subsidiary company and obtained the ownership of Ambrisentan. The drug was approved by the US FDA on June 15, 2007. The trade name is Letairis. It is used orally for the treatment of pulmonary arterial hypertension (PAH). The chemical name is (+)-(2S)-2-[(4,6-two Methylpyrimidin-2-yl)oxy]-3-methoxy-3,3-diphenylpropionic acid, the structure of which is sho...

Claims

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