Preparation method of 4-[(4-Hydroxy-2-pyrimidinyl) amino] benzonitrile

A technology for p-guanidinobenzonitrile and amino, which is applied in the field of synthesis of 4-[amino]benzonitrile, which can solve the problems of unsuitability for large-scale industrial production, large residues of decarboxylation impurities, harsh reaction conditions, etc., and improve safety , less impurity formation, and low reaction temperature
CN103193719BActive Publication Date: 2015-07-22NINGBO CHEMGOO PHAMA TECH CO LTD
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
NINGBO CHEMGOO PHAMA TECH CO LTD
Publication Date
2015-07-22

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Abstract

The invention discloses a preparation method of 4-[(4-Hydroxy-2-pyrimidinyl) amino] benzonitrile. The prepration method comprises the following steps of adding N-guanidine and 3-methoxy-acrylate into reaction solvent, heating and controlling the temperature until the end of the reaction, and separating and purifying the reaction solution to obtain 4-[(4-Hydroxy-2-pyrimidinyl) amino] benzonitrile. 3-methoxy-acrylate is 3-methoxy-methyl acrylate or 3-methoxy-ethyl acrylate. Due to the adoption of the preparation method, the yield and the quality of the product can be improved, the cost is reduced, operation is simple, and the preparation method is a synthesis route which is suitable for the industrial production of a Rilpivirine midbody.
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Description

technical field

[0001] The invention belongs to the technical field of preparation of pharmaceutical products, and relates to the preparation of an important intermediate of a novel non-nucleoside reverse transcriptase inhibitor rilpivirine (rilpivirine). Specifically, the invention relates to 4-[(4-hydroxy- Synthetic process of 2-pyrimidinyl) amino] benzonitrile. Background technique

[0002] Rilpivirine (rilpivirine) is a new type of non-nucleoside reverse transcriptase inhibitor (non-nucleoside reverse tran-scriptase inhibitor, NNRTI) developed by the American company Tibotec. It is used for the treatment of AIDS, and its trade name is Edurant. On May 20, it was approved for marketing by the US FDA. It has the characteristics of easy synthesis, strong antiviral activity, high oral bioavailability, and good safety.

[0003] The existing synthetic route is mainly to cyclize p-guanidinobenzonitrile and diethyl ethoxymethylenemalonate in NMP to generate an intermediate state...

Claims

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