Process for producing 2-acylpyridine derivative

摘要

PROBLEM TO BE SOLVED: To obtain the subject derivative useful as an intermediate for synthesizing fusaric acid having antibiosis and antihypertensive action in a high yield by an industrially advantageous method by acylating a specific cyanopyridine derivative. ;SOLUTION: A 2-sulfonylpyridine derivative of formula [R1 to R3 are each H or a (substituted) alkyl or a (substituted) aryl; R4 is H, an alkoxyl, an acyloxy or the like; R5 is a (substituted) alkyl, a cycloalkyl, an aryl or the like] (e.g. 2-benzenesulfonyl-5-ethylpyridine) is reacted with (B) a cyanating agent (e.g. sodium cyanide) in an amount of 1-10 times as much as mols of the component A to give (C) a 2-cyanopyridine derivative of formula II (e.g. 2-cyano-5- ethylpyridine), which is acylated with (D) an acylating agent in an amount of 1-5 times as much as the component C to give the objective derivative of formula III [R6 is a (substituted) alkyl or a (substituted) aryl] (e.g. 2-acetyl-5- ethylpyridine).;COPYRIGHT: (C)2000,JPO