反应详情

A mixture of (2S,3S)-3-hydroxy-pyrrolidine-1,2-dicarboxylic acid 1-tert-butyl ester (6 g), EDAC (6 g, 1.2 eq.), HOBt (4.2 g, 1.2 eq.), TEA (9 mL, 2.5 eq.) and cyclopropylamine (2.2 mL, 1.2 eq.) in DMF (30 mL) was stirred at rt for over the weekend. The insolubles were filtered off, the filtrate was concentrated, redissolved in ethyl acetate, washed with sodium bicarbonate and brine, dried and concentrated to give 5.6 g of (2S,3S)-2-cyclopropylcarbamoyl-3-hydroxy-pyrrolidine-1-carboxylic acid tert-butyl ester as a white solid.

1. filtrationThe insolubles were filtered off
2. concentrationthe filtrate was concentrated
3. dissolutionredissolved in ethyl acetate
4. washwashed with sodium bicarbonate and brine
5. customdried
6. concentrationconcentrated