- A facile and convenient synthesis of 9-methyl-3(1H-tetrazol-5-YL)-4H-pyrido[1,2-a]pyrimidin-4-one potassium
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Two convenient synthetic methods of anti-allergy agent, 9-methyl-3-(1H-tetrazol-5-yl)-4H-pyrido[1,2-a]pyrimidin-4-one potassium (1a), are described. Heating of a mixture of malononitrile (2b), 2-amino-3-picoline (4), ethyl orthoformate, and sodium azide in acetic acid, followed by hydrolysis with hydrochloric acid gave 9-methyl-3-(1H-tetrazol-5-yl)-4H-pyrido[1,2-a]pyrimidin-4-one (1b) which was led to 1a by treatment with potassium hydroxide. The use of ethyl cyanoacetate (2a) instead of 2b afforded ethyl 3-(3-methyl-2-pyridylamino)-2-(1H-tetrazol-5-yl)acrylate (8) which was also led to 1a by treatment with potassium hydroxide. 1. The generic name is pemirolast potassium.
- Sano, Atsunori,Ishihara, Masami
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- Process for the preparation of high purity pemirolast
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A novel process for the purification of Pemirolast, whose potassium salt is an anti-allergic pharmaceutical product, is disclosed.
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- A process for the preparation of high purity pemirolast
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A novel process for the purification of Pemirolast, whose potassium salt is an anti-allergic pharmaceutical product, is disclosed, comprising the salification with primary or secondary amine and acidification to ph ranging from 2 to 4.
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