反应详情

(R)-3-Cyano-pyrrolidine-1-carboxylic acid tert-butyl ester (1.02 g, 5.2 mmol), hydroxylamine hydrochloride (396 mg, 5.7 mmol) and NaHCO3 (487 mg, 5.8 mmol) were added to MeOH (12 mL) and the solution was heated to reflux. After 4 h, the reaction was concentrated in vacuo. The residue was partitioned between EtOAc and brine. The layers were separated and the organic layer was dried over Na2SO4, filtered and concentrated to yield 927 mg of crude (R)-3-(N-hydroxycarbamimidoyl)-pyrrolidine-1-carboxylic acid tert-butyl ester as a yellow foam.

1. temperaturethe solution was heated to reflux
2. concentrationthe reaction was concentrated in vacuo
3. customThe residue was partitioned between EtOAc and brine
4. customThe layers were separated
5. dry with materialthe organic layer was dried over Na2SO4
6. filtrationfiltered
7. concentrationconcentrated