tert-butyl (2R)-2-(ethylcarbamoyl)pyrrolidine-1-carboxylate

反应条件: temp:0.00; pressure:0.00; stir:; See reaction.notes.procedure_details.

实验步骤: To tert-butyl (2R)-2-(ethylcarbamoyl)pyrrolidine-1-carboxylate (561 mg, 2.3 mmol) was added hydrogen chloride (580 μL of 4 M, 2.3 mmol) in dioxane at room temperature under an atmosphere of nitrogen. The reaction mixture was stirred for 3 h. The solvent was removed under reduced pressure to obtain (2R)-N-ethylpyrrolidine-2-carboxamide (225 mg, 54%). LC/MS m/z 143.2 [M+H]+. The solvent was removed under reduced pressure

反应条件: temp:0.00; pressure:0.00; stir:; See reaction.notes.procedure_details.

实验步骤: To a solution of (2R)-1-tert-butoxycarbonylpyrrolidine-2-carboxylic acid (810 mg, 3.8 mmol) and HATU (1.40 g, 3.8 mmol) in DMF (7.5 mL) was added ethanamine (3.8 mL of 2 M, 7.5 mmol) followed by DIEA (1.0 g, 1.4 mL, 8.0 mmol) at room temperature. The reaction mixture was stirred at room temperature for 16 h. The reaction mixture was diluted with EtOAc and washed sequentially with 1M HCl, saturated NaHCO3 and brine solution. The organic layer was dried (Na2SO4) filtered and concentrated under reduced pressure to obtain tert-butyl (2R)-2-(ethylcarbamoyl)pyrrolidine-1-carboxylate (624 mg, 68%). LC/MS m/z 243.4 [M+H]+. washed sequentially with 1M HCl, saturated NaHCO3 and brine solution The organic layer was dried (Na2SO4) filtered concentrated under reduced pressure