公开(公告)号：BG107390A

公开(公告)日：2004-06-30

申请号：BG10739002

申请日：2002-12-16

Applicant: BALKANFARMA DUPNITSA AD

Inventor： STANEVA TINKA D ,  NACHEVA ELIZABET B ,  LAZAROV VLADIMIR K ,  BACHEVA BOJKA L ,  KATSARSKI DIMITAR E

IPC: A61K31/445 ,  C07D211/14

Abstract: The invention relates to a method for the preparation of 2-[4-[2-(1-piperidinyl)ethoxy] benzoyl] benzoic acid methyl ester hydrochloride having antispasmolytic activity and strong local anaesthetic effect and is used as antispasmolytic component in medicamentous compositions in combination with analgetics. By the method, a high purity and high yield product is turned out in reaction between phenol and dichlorethane, acylation of the phenyloxyethylchloride produced and subsequent amination with piperidine in aqueous-alkaline medium at 100 degrees C of an influx. After the water distillation the remainder is cooled to room temperature and is esterified with methanol and sulphuric acid at 65 to 75 degrees C. After the elimination of the methanol excess, the remainder of the reaction mixture is diluted in water and is neutralized to pH 7-8 at continuous cooling. The ester produced is extracted by dichlorethane, the extract is evaporated, and the residue is dissolved in acetone, hydrochloric acid is added, and the reaction mixture is cooled to 0-5 degrees C. The sediment produced is filtered, washed in acetone, is dried and purified in ethanol. The purified product crystallizes by the addition of acetone and cooling to 0-5 degrees C and is then dried. 2 claims