A kind of ambrisentan degradation product and preparation method thereof

A compound and selected technology, applied in the field of biomedicine, can solve the problems of undisclosed degradation products, unknown structure, etc.
CN104177300BActive Publication Date: 2016-02-24SHANGHAI MEIYUE BIOTECH DEV +1
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
SHANGHAI MEIYUE BIOTECH DEV
Publication Date
2016-02-24

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Abstract

The invention discloses an ambrisentan degradation product and a preparation method thereof. The ambrisentan degradation product is represented by formula I, is one of main impurities of ambrisentan raw materials or preparations thereof and the formula I can be used for analyzing the purity of ambrisentan, and can also be used for controlling the quality of ambrisentan. The preparation method of the product of the formula I is characterized in that a substitution reaction of 2,2-diphenyl acetaldehyde and a compound represented by formula II is carried out under the action of sodium hydride and other alkaline compounds.
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Description

technical field

[0001] The invention belongs to the field of biomedicine, and in particular relates to a degradation product of ambrisentan and a preparation method thereof. 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, GileadScience 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-diphenylpropano...

Claims

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