反应详情

Pyrrolidine-1,2-dicarboxylic acid 1-tert-butyl ester (24.0 g) was dissolved in acetonitrile (330 mL), and triethylamine (15.6 mL) was added. A solution of 2-bromo-1-(6-bromonaphthalen-2-yl)-ethanone (33.0 g) in acetonitrile (170 mL) were added. Reaction mixture was stirred over 3 days and evaporated under vacuum. Oil was dissolved in dichloromethane (100 mL), extracted with water (50 mL) and with NaHCO3 solution (50 mL), and evaporated under vacuum to a concentrated liquid. Solution was purified by chromatography (0-30% ethyl acetate:hexane) and evaporated under vacuum, giving pyrrolidine-1,2-dicarboxylic acid 2-[2-(6-bromo-naphthalen-2-yl)-2-oxo-ethyl]ester 1-tert-butyl ester (39.2 g, 84%) as a tan solid.

1. customReaction mixture
2. customevaporated under vacuum
3. dissolutionOil was dissolved in dichloromethane (100 mL)
4. extractionextracted with water (50 mL) and with NaHCO3 solution (50 mL)
5. customevaporated under vacuum to a concentrated liquid
6. customSolution was purified by chromatography (0-30% ethyl acetate:hexane)
7. customevaporated under vacuum