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4 - acyloxy - 2 - manufacturing method null of azetidinone

机译:4-酰氧基-2-氮杂环丁酮的制备方法无效

摘要

PURPOSE:To obtain a compound useful as a synthetic intermediate for penem or carbapenem compounds without using mercury salts causing environmental pollution by reacting a 2-azetidinone derivative with a copper compound in the presence of an organic carboxylic acid. CONSTITUTION:A 2-azetidinone derivative expressed by formula I (OR is protected OH; X is alkyl or aromatic group) is reacted with a copper compound. In the process, a free or salt type organic carboxylic acid as an acyl group supply source is contained in the reaction mixture to carry out the reaction and afford the objective substance expressed by formula II (Y is acyl). The organic carboxylic acid is an aliphatic or aromatic carboxylic acid. The copper compound which is a copper salt (cupric acetate) of the organic carboxylic acid serves also as the acyl group supply source. The copper compound is used in an amount of =0.5 equiv. based on the compound expressed by formula I.
机译:目的:通过在有机羧酸的存在下,使2-氮杂环丁酮衍生物与铜化合物反应,而无需使用会造成环境污染的汞盐,而获得可用作青霉素或碳青霉烯化合物的合成中间体的化合物。组成:由式I表示的2-氮杂环丁酮衍生物(OR为受保护的OH; X为烷基或芳基)与铜化合物反应。在该方法中,在反应混合物中包含游离的或盐类的有机羧酸作为酰基供应源以进行反应并提供由式II表示的目标物质(Y为酰基)。有机羧酸是脂族或芳族羧酸。作为有机羧酸的铜盐(乙酸铜)的铜化合物也用作酰基供给源。铜化合物的使用量≥0.5当量。基于式I表示的化合物。

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