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利斯的明作为氨基甲酸酯类乙酰胆碱酯酶抑制剂在60多个国家被批准用于治疗老年痴呆症,是临床最重要的治疗药物之一.从3-乙基苯酚出发,以3步反应高效实用地合成了利斯的明消旋体.关键步骤是以NBS为试剂的N-甲基-N-乙基胺基甲酸-3-乙基苯酯的苄位溴代反应.目标分子能够以71%的总产率得到,并且整个实验不需要传统的柱层析或者重结晶分离.整个合成包括酯化、苄位溴代和取代3种反应.
Lysine as carbamate acetylcholinesterase inhibitors approved in more than 60 countries for the treatment of Alzheimer’s disease is one of the most clinically important drugs for the treatment of starting from 3-ethyl phenol, three-step reaction Efficient and practical synthesis of leracetas racemate The key step is the N-methyl-N-ethyl-N-ethylcarbamate N-methyl-N-ethyl benzyl ester bromination with NBS The target molecule can Obtained in 71% of the total yield, and the whole experiment does not require the traditional column chromatography or recrystallization separation.The entire synthesis includes esterification, benzyl bromide and substitution of three kinds of reactions.