The invention relates to a practical synthesis method of 3-benzyl-3-aza-bicyclo[2,1,0]
hexane. The method comprises the following synthesis processes of: condensing dimethyl itaconate, serving as a
raw material, with
benzylamine to obtain ester, and reducing to obtain
alcohol; reacting the ester with
methanesulfonyl chloride to generate methanesulfonyl ester; reacting the methanesulfonyl ester with
lithium hexamethyl disilazide to obtain corresponding 3-benzyl-3-aza-bicyclo[2,1,0]
hexane-2-one; and reducing by
lithium aluminum hydride to obtain the 3-benzyl-3-aza-bicyclo[2,1,0]
hexane. Due to the adoption of the method, the defects of low yield, complexity in operation, difficulty in post-treatment and amplification and the like in the conventional document process are overcome. The practical synthesis method of the 3-benzyl-3-aza-bicyclo[2,1,0]hexane provided by the invention has the advantages of simple synthesis
route, reasonable
process selection, low cost of the
raw material, easiness in obtaining of the
raw material, convenience for operation and post-treatment, high total yield, easiness in amplification, and application to large-scale production. In the method, the dimethyl itaconate serves as the raw material.