A Facile and Practical Synthesis of 9-Methyl-3-(1H-tetrazol-5-yl)-4H-pyrido[1,2-α]pyrimidin-4-one

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概要

• 論文の詳細を見る

• A facile and practical synthesis of 9-methyl-3-(1H-tetrazol-5-yl)-4H-pyrido[1,2-α]pyrimidin-4-one (4), the potassium salt of which is used clinically as an anti-asthma agent, is described. Treatment of a key intermediate (6b), prepared from 2-amino-3-methylpyridine (1) and 2-ethoxymethylene-1,3-propanedinitrile, with sodium azide in N, N-dimethylformamide gave predominantly the cyanotetrazole (7a), while in acetic acid it gave exclusively the iminotetrazole (7b), which was easily converted into 4 by acid hydrolysis. A one-pot process starting from 6b to give 4,avoiding the use of explosive aluminum azide, was established.

• 公益社団法人日本薬学会の論文
• 1995-04-15

著者

• 吉原 潤

  Tokyo Research Laboratories Wako Pure Chemical Industires Ltd.

• 佐野 淳典

  Tokyo Research Laboratories Wako Pure Chemical Industires Ltd.

• 石原 正巳

  Tokyo Research Laboratories, Wako Pure Chemical Industires, Ltd.,

• 角野 元重

  Tokyo Research Laboratories, Wako Pure Chemical Industires, Ltd.,

• 名和 裕美

  Tokyo Research Laboratories, Wako Pure Chemical Industires, Ltd.,

• 角野 元重

  Tokyo Research Laboratories Wako Pure Chemical Industires Ltd.

• 石原 正巳

  Tokyo Research Laboratories Wako Pure Chemical Industires Ltd.

• 名和 裕美

  Tokyo Research Laboratories Wako Pure Chemical Industires Ltd.

• Sumino Motoshige

  Tokyo Research Laboratories Wako Pure Chemical Industries Ltd.

関連論文

• Studies on Synthesis of 10,11-Dihydro-5H-dibenzo[a, d]cycloheptene Derivatives. IV. : Photoreactions of 5-Substituted-5H-dibenzo[a, d]cycloheptenes with 1,2-Substituted Olefins and the Stereostructures of the Cycloaddition Products
• A Facile and Practical Synthesis of 9-Methyl-3-(1H-tetrazol-5-yl)-4H-pyrido[1,2-α]pyrimidin-4-one

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