反应详情

Pyrrolidine-1,2-dicarboxylic acid 1-tert-butyl ester (4.85 g) was dissolved in acetonitrile (65 mL), and triethylamine (3.09 mL) was added. A solution of 2-bromo-1-(4-bromonaphthalen-1-yl)-ethanone (6.60 g) in acetonitrile (35 mL) was added. Reaction mixture was stirred 90 minutes and evaporated under vacuum. Oil was dissolved in DCM (50 mL), extracted once with water (20 mL) and once with NaHCO3 solution (20 mL), and evaporated under vacuum to a concentrated liquid. Solution was purified by chromatography (0-50% ethyl acetate:hexane) and evaporated under vacuum, giving pyrrolidine-1,2-dicarboxylic acid 2-[2-(4-bromonaphthalen-1-yl)-2-oxo-ethyl]ester 1-tert-butyl ester (8.95 g, 95%) as a tan solid.

1. customReaction mixture
2. customevaporated under vacuum
3. dissolutionOil was dissolved in DCM (50 mL)
4. extractionextracted once with water (20 mL) and once with NaHCO3 solution (20 mL)
5. customevaporated under vacuum to a concentrated liquid
6. customSolution was purified by chromatography (0-50% ethyl acetate:hexane)
7. customevaporated under vacuum