N−(α−ハロアシル)−β−ラクタム誘導体の製造方法

METHOD OF PRODUCING N-(α-HALOACYL)-β-LACTAM DERIVATIVE

Abstract

【課題】取り扱い容易な原料を用いて、温和な条件で収率良くN−(α−ハロアシル)−β−ラクタム誘導体を製造する方法を提供する。 【解決手段】特定のβ−ラクタム誘導体に対して、特定のα−ハロカルボン酸ハロゲン化物及び塩基を、系内に添加した塩基の総モル数が、系内に添加したα−ハロカルボン酸ハロゲン化物の総モル数を常に上回るようにして、塩基とα−ハロカルボン酸ハロゲン化物をそれぞれ独立して同時に添加することを特徴とする、下記一般式(III) 【化3】 (式中、R 1 、R 2 、R 3 、R 4 、R 5 およびX 2 は、明細書に記載のとおりである。) で示されるN−(α−ハロアシル)−β−ラクタム誘導体の製造方法。 【選択図】なし
PROBLEM TO BE SOLVED: To provide a method of producing N-(α-haloacyl)-β-lactam derivative using an easily handleable raw material under a mild condition at a high yield.SOLUTION: The method of producing N-(α-haloacyl)-β-lactam derivative represented by formula (III) is characterized by independently and simultaneously adding an alkali and a specific α-halocarboxylic acid halide respectively into a specific β-lactam derivative in a manner of always keeping the total mole number of the alkali added into the reaction system greater than that of α-halocarboxylic acid halide added thereinto (in the formula, R, R, R, and Reach independently represent a hydrogen atom, a 1-5C alkyl group, a 3-10C cyclic hydrocarbon group, or a 2-6C acyloxy group, provided that Rand R, Rand Rmay respectively bind to each other to form a ring of the number of ring forming atoms of 3-10, together with a carbon atom binding thereto respectively, which ring may contain an oxygen atom at an optional position, or Rand Rmay bind to each other to form a ring of the number of ring forming atoms of 4-10, together with a carbon atom binding thereto respectively, which ring may contain an oxygen atom at an optional position, or a ring that may be formed by the binding of Rand R, Rand R, or Rand R, may contain a substituent; Rrepresents a hydrogen atom, a halogen atom, or a 1-6C hydrocarbon group; and Xeach independently represents a halogen atom).

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