1196551-99-1Relevant articles and documents
Synthesis method of R-2-(2, 5-difluorophenyl) pyrrolidine
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Page/Page column 8-12, (2020/04/29)
The invention relates to a synthesis method of R-2-(2, 5-difluorophenyl) pyrrolidine, and the method comprises the following steps: 1) reacting pyrrolidone serving as a raw material with di-tert-butylcarbonate in a polar or non-polar solvent in the presence of alkali to obtain tert-butyl pyrrolidone formate; 2) in an organic solvent, enabling the tert-butyl pyrrolidone formate to react with a Grignard reagent of 2, 5-difluorobromobenzene to obtain tert-butyl 2-(2, 5-difluorophenyl)-2-hydroxypyrrole-1-formate; 3) carrying out acid catalytic dehydration and deprotection on the tert-butyl 2-(2,5-difluorophenyl)-2-hydroxypyrrole-1-formate in an organic solvent to obtain 5-(2, 5-difluorophenyl)-3, 4-dihydro-2H-pyrrole; and 4) reducing the 5-(2, 5-difluorophenyl)-3, 4-dihydro-2H-pyrrole in anorganic solvent by using chiral acid and ammonia borane to obtain the R-2-(2, 5-difluorophenyl) pyrrolidine with high enantioselectivity. The synthesis method disclosed by the invention is simple, mild in condition, simple to operate and low in production cost, and can be used for industrial production.