A Reagent, Ethyl 2-(2-tert-Butyl-2H-tetrazol-5-yl)-3-(dimethylamino)acrylate (DMTE), for Facile Synthesis of 2,3-(Ring Fused)-5-(5-tetratzolyl)-4H-pyrimidin-4-one Derivatives
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概要
- 論文の詳細を見る
A method for synthesizing 2,3-(ring fused)-5-(5-tetrazolyl)-4H-pyrimidin-4-one derivative from ethyl 2-(2-tert-butyl-2H-tetrazol-5-yl)-3-(dimethylamino)acrylate (DMTE) (4a) and amino-heterocycles is described. The structure of DMTE, which was prepared from ethyl (2-tert-butyl-2H-tetrazol-5-yl)acetate (3a) with dimethylformamide diethylacetal, was determined by X-ray analysis to be Z form. The reaction of 2-amino-5-methyloxazole (6) with DMTE in acetic acid gave the oxazolo[3,2-a]pyrimidine derivative (8), heating of which in concentrated sulfuric acid afforded the desired tetrazole derivative (20). Pyrimido[2,1-b]benzothiazole (21), pyrazolo[1,5-a]pyrimidine (22 and 23) and [1,2,4]triazolo[1,5-a]pyrimidine (24) derivatives were prepared in a similar manner.
- 公益社団法人日本薬学会の論文
- 1991-05-25
著者
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磯田 純郎
Exploratory Research Laboratories Iii Daiichi Pharmaceutical Co. Ltd.
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菅野 英幸
Research Institute, Daiichi Pharmaceutical Co., Ltd.,
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菅野 英幸
Exploratory Research Laboratories Iii Daiichi Pharmaceutical Co. Ltd.
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山口 等
Research Institute, Daiichi Pharmaceutical Co., Ltd.,
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市川 喜文
Research Institute, Daiichi Pharmaceutical Co., Ltd.,
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磯田 純郎
Research Institute, Daiichi Pharmaceutical Co., Ltd.,
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山口 等
Research Institute Daiichi Pharmaceutical Co. Ltd.
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磯田 純郎
Research Institute Daiichi Seiyaku Co. Ltd.
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市川 喜文
Research Institute Daiichi Pharmaceutical Co. Ltd.
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