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Method for synthesizing novel intermediate, and method for synthesizing 3'-azido-3'-deoxythymidine and analog using the intermediate
Method for synthesizing novel intermediate, and method for synthesizing 3'-azido-3'-deoxythymidine and analog using the intermediate
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机译:新型中间体的合成方法以及使用该中间体的3'-叠氮基-3'-脱氧胸苷和类似物的合成方法
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PCT No. PCT/FR89/00018 Sec. 371 Date May 4, 1990 Sec. 102(e) Date May 4, 1990 PCT Filed Jan. 19, 1989.The invention relates to a process for preparing a compound of formula (I) IMAGE I in which R1 is H, an alkyl radical or an alkoxy, hydroxyalkyl or halogen radical, and R3 is N3 or a CN radical, characterized in that a compound of formula (II): IMAGE II is reacted with a phosphine derivative and an azodicarboxylic acid diester and a carboxylic acid R2-COOH in a solvent compatible with the reaction conditions, to form the compound of formula (III): IMAGE III which, after separation if required, is opened in the presence of an azide or a cyanide in a solvent compatible with the reaction conditions, and the compound of formula (I) is then isolated from the reaction medium after deprotection of the 5'-position.
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