Studies on Fluorinated Pyrimidines. I. A New Method of Synthesizing 5-Fluorouracil and Its Derivatives
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概要
- 論文の詳細を見る
A series of 5-fluoro-6-substituted-5,6-dihydrouracil-5-carboxylic esters (13), -5-carboxamides (15,16), and -5-carbonitriles (18,19) was prepared by direct fluorination of the corresponding uracil-5-carboxylic esters (6), -5-carboxamide (14), and -5-carbonitrile (17) with fluorine or trifluoromethyl hypofluorite (CF_3OF) in the presence of water, methanol and/or acetic acid. Hydrolysis of the above-mentioned products under mild conditions gave 5-fluorouracil (1a) in high yield. Some applications of the present method for the synthesis of 1-(2-tetrahydrofuryl)-5-fluorouracil (1b) were also described.
- 公益社団法人日本薬学会の論文
- 1981-11-25
著者
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橋本 直人
Central Research Division Takeda Chemical Industries Ltd.
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宮下 修
Central Research Division, Takeda Chemical Industries, Ltd.
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松村 興一
Central Research Division, Takeda Chemical Industries, Ltd.
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島津 浩
Central Research Division, Takeda Chemical Industries, Ltd.
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島津 浩
Pharmaceutical Research Division Pharmaceutical Research Laboratories Iii Takeda Chemical Industires
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宮下 修
Central Research Division Takeda Chemical Industries Ltd.
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松村 興一
Central Research Division Takeda Chemical Industries Ltd.
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