Preparation method of 1-cyclohexyl-1-phenyl-3-piperidinepropanol hydrochloride

Abstract

The invention discloses a preparation method of 1-cyclohexyl-1-phenyl-3-piperidinepropanol hydrochloride. The preparation method comprises the following steps of: dropwise adding chlorocyclohexane and diethyl ether mixed liquid into a magnesium and diethyl ether mixture; keeping warm, and carrying out refluxing reaction for 3 hours to obtain Grignard reaction liquid; and dropwise adding acetophenone into piperidine hydrochloride, anhydrous methanol and formaldehyde mixed liquid at room temperature to react for 30 minutes; cooling and filtering in vacuum to obtain a solid mixture; mixing the solid mixture and diethyl ether, and dropwise adding the Grignard reaction liquid; cooling and then dropwise adding 5% diluted hydrochloric acid; separating; and drying to obtain a product. By using the preparation method of 1-cyclohexyl-1-phenyl-3-piperidinepropanol hydrochloride disclosed by the invention, the yield of a product can reach more than 95%, the production cycle of the product is shortened, the productivity is improved, the labor amount in a production process is reduced, the production cost is reduced, and the market competitiveness is improved.

Description

technical field [0001] The invention relates to the field of synthesis of pharmaceutical intermediates, in particular to a production method of 1-cyclohexyl-1-phenyl-3-piperidine propanol hydrochloride. Background technique [0002] 1-cyclohexyl-1-phenyl-3-piperidine propanol hydrochloride, commonly known as benzhexol hydrochloride, molecular weight 337.93, molecular formula C 20 h 32 ClNO, the structural formula is . It can be used as a pharmaceutical intermediate, and it is also a central anticholinergic anti-Parkinson's disease drug. Its function is to selectively block the cholinergic nerve pathway of the striatum, and has little effect on the periphery, which is beneficial to the recovery of Parkinson's disease patients. The balance of dopamine and acetylcholine in the brain improves the symptoms of Parkinson's disease in patients. [0003] The preparation technology of existing 1-cyclohexyl-1-phenyl-3-piperidine propanol hydrochloride mainly adopts to prepare inte...

AI Technical Summary

Problems solved by technology

However, the general reaction process is carried out under high temperature and high pressure. The operating environment is dangerous to people. The production cycle of the product is long and the yield is low, which greatly increases the production cost. At the same time, a large amount of waste water and waste gas will be generated during the production process, polluting the environment.