PURPOSE: To provide a method for profitably producing a 1,2-cis-2- fluorocyclopropanecarboxylic acid derivative useful as a raw material for producing a quinolone derivative which is an excellent antimicrobial agent.
CONSTITUTION: A compound of formula I or formula II (R is H, a 1-4C alkyl; X is Cl, Br) is subjected to a catalytic hydrocracking reaction in the presence of a base, preferably 1,2-diaminoethane, to obtain a compound of formula III. The catalytic hydrocracking reaction is carried out by treating a reaction substrate in the presence of a catalyst selected from various metal catalysts (preferably Raney nickel or PdC) in a solution under a hydrogen gas atmosphere having a hydrogen gas pressure of 1-50atm. The reaction advances a dehalogenation reaction in a steric configuration-holding state, thus enabling to obtain 1,2-cis-fluorocyclopropanecarboxylic acid derivative in a good yield.
IKETANI TAKANOBU
KAWANISHI HIROFUMI
YUKIMOTO YUSUKE
KANBARA SHINJI
EHATA TSUTOMU