PIPERIDINOPHENYLCARBOXYLIC ACID DERIVATIVE AND ITS PREPARATION

摘要

NEW MATERIAL:A piperidinophenylcarboxylic acid derivative shown by the formulaI(Z is a group shown by the formula II or III. EXAMPLE:alpha-Hydroxy-alpha-(chloro-piperidinophenyl)-propionic acid. USE:A raw material for preparing a-(3-chloro-4-piperidino phenyl)propionic acid having improved antiphlogistic and analgesic action. PROCESS:3-Chloro-4-piperidinoacetophenone shown by the formula IV is reacted with a halaform shown by the formula V (X<1> is Cl or Br) preferably in a nonproton polar solvent in the presence of a catalyst transferring between phases, to bive a compound shown by the formulaI. The compound shown by the formula IV is synthesized by reacting 4-aminoacetophenone with 1,5-dihalopentane shown by the formula VI (X<2> and X<3> are halogen) in the presence of a base to give 4- piperidionoacetophenone, which is chlorinated in an organic solvent.