Synthesis process of dexmedetomidine hydrochloride midbody

• Main Authors: DI CAIXIA, ZHANG AIPING, ZHENG YONG, SUN WENCHAO, GUO LIANG, YAO CHUNHU, HUANG JINYUAN, GE LAIBING
• Format: Patent
• Language: Chinese; English
• Published: 31.05.2017
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; METALLURGY; ORGANIC CHEMISTRY

The invention provides a synthesis process of a dexmedetomidine hydrochloride midbody. The process comprises the following steps: in the presence of titanium tetrachloride, carrying out reaction on 1-(1-chloroethyl)-2,3-dimethylbenzene and N-(trimethylsilyl)imidazole in a non-protonic solvent, so as to prepare medetomidine, wherein the mole ratio of 1-(1-chloroethyl)-2,3-dimethylbenzene to N-(trimethylsilyl)imidazole to titanium tetrachloride is (0.8-1.0): 2: (1.005-1.05). According to the process provided by the invention, the charge rates of the raw materials are initiatively adjusted, and the use amount of titanium tetrachloride is decreased while the use amount of N-(trimethylsilyl)imidazole is increased, so that the yield of the target product can be remarkably improved, the yield is 72.4% when an optimum raw material ratio is achieved, and the yield is much higher than the yield of 39.3% in the prior art. 本发明提供了种盐酸右美托咪定中间体的合成工艺，该工艺是在四氯化钛的存在下，1-(1-氯乙基)-2,3-二甲基苯与N-三甲基硅基咪唑在非质子性溶剂中发生反应，制得美托咪定，所述1-(1-氯乙基)-2,