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Method for synthesizing novel intermediate, and method for synthesizing 3'-azido-3'-deoxythymidine and analog using the intermediate

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

摘要

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.
机译:PCT号PCT / FR89 / 00018第371日期1990年5月4日102(e)1990年5月4日的PCT申请,1989年1月19日提交。本发明涉及一种制备式(I)化合物的方法,其中R 1为氢,烷基或烷氧基,羟烷基R3为N3或CN基,其特征在于,式(II)的化合物: II与膦衍生物,偶氮二羧酸二酯和羧酸R2-COOH在溶剂相容的条件下反应。在反应条件下,形成式(III)的化合物: III,其在需要时分离后,在叠氮化物或氰化物的存在下,在与反应条件相容的溶剂中打开,以及然后在5′-位脱保护后,从反应介质中分离出式(I)。

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