| 摘要 |
PROBLEM TO BE SOLVED: To produce a new compound comprising a piperidine derivative and useful as an antihistaminic agent, an antiallergic agent and a bronchodilator. SOLUTION: This compound is represented by formula I or II (R1 is H or OH; R2 is a halogen; R3 is COOH or COOR4; R4 is a 1-6C alkyl; A, B and D are each H, a halogen or the like), e.g. 4- 4-[4-(hydroxydiphenylemthyl)-1- piperidinyl]-1-hydroxybutyl)-α,α-dimethylbenzeneacetic acid. The compound represented by formula I or II is produced by opening the ring and halogenating a position isomer represented by formula III and reacting the resultant compound with a piperidine compound represented by formula IV in the presence of a base (e.g. sodium hydrogencarbonate) and, as desired, potassium iodide in a catalytic amount preferably in a solvent (e.g. methanol) at about 70 deg.C to the refluxing temperature of the solvent for about 4-120 h. |
