81579-50-2

Upstream product

• 100-46-9 benzylamine 
• 73866-23-6 5-(2-bromoacetyl)-2-hydroxybenzamide 
• 143097-80-7 2-bromo-4-phenylbutane 
• 116199-39-4 4-phenylbutan-2-yl 4-methylbenzene-1-sulfonate 
• 2344-70-9 1-phenyl-3-butanol 
• 68164-04-5 N-benzyl-1-methyl-3-phenylpropylamine 

Downstream Products

• 36894-69-6 labetaol 

Relevant academic research and scientific papers

Preparation method of labetalol hydrochloride

The invention provides a preparation method of labetalol hydrochloride, and belongs to the technical field of medicines. The invention provides a preparation method. The method comprises the following steps: carrying out nucleophilic substitution reaction on 5-halogenated acetyl salicylamide serving as an initial raw material and benzylamine, and then carrying out nucleophilic substitution reaction on the obtained product and 3-halogenated butylbenzene (or carrying out amine-ester exchange reaction on the obtained product and an esterification reaction product of 3-hydroxybutylbenzene and p-toluenesulfonyl chloride); and carrying out catalytic hydrogenation reaction and salifying to obtain the labeolol hydrochloride. According to the preparation method provided by the invention, benzylamine is adopted to replace dibenzylamine, so that the raw materials are high in atom utilization rate and environment-friendly, and atom economy of green chemistry is embodied; wherein the amine-ester exchange reaction is high in selectivity, and the obtained product is directly used for the next-step reaction. The one-step method is adopted to remove the protective agent and reduce carbonyl, so that the process route is shortened; meanwhile, the preparation method is simple and convenient to operate, high in stability and controllability, high in production cost, high in yield and suitable for industrial production.