| 摘要 |
<P>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. <P>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<SP POS="POST">1</SP>, R<SP POS="POST">2</SP>, R<SP POS="POST">3</SP>, and R<SP POS="POST">4</SP>each independently represent a hydrogen atom, a 1-5C alkyl group, a 3-10C cyclic hydrocarbon group, or a 2-6C acyloxy group, provided that R<SP POS="POST">1</SP>and R<SP POS="POST">2</SP>, R<SP POS="POST">3</SP>and R<SP POS="POST">4</SP>may 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 R<SP POS="POST">2</SP>and R<SP POS="POST">3</SP>may 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 R<SP POS="POST">1</SP>and R<SP POS="POST">2</SP>, R<SP POS="POST">3</SP>and R<SP POS="POST">4</SP>, or R<SP POS="POST">2</SP>and R<SP POS="POST">3</SP>, may contain a substituent; R<SP POS="POST">5</SP>represents a hydrogen atom, a halogen atom, or a 1-6C hydrocarbon group; and X<SP POS="POST">2</SP>each independently represents a halogen atom). <P>COPYRIGHT: (C)2012,JPO&INPIT |
