反应详情

(S)-3-(2-amino-5-methylphenoxy)-2-(tert-butoxycarbonylamino)propanoic acid (3.85 g, 12.4 mmol, Eq: 1.00) and EDCI (2.38 g, 12.4 mmol, Eq: 1.00) were dissolved in DMF (50 mL) and the mixture was stirred at RT for 3 h. The mixture was diluted with EtOAc and washed with water, brine and the organic solution dried over Na2SO4. The mixture was filtered, concentrated and the residue was purified by silica gel chromatography to afford (S)-tert-butyl 8-methyl-4-oxo-2,3,4,5-tetrahydrobenzo[b][1,4]oxazepin-3-ylcarbamate (2.51 g, 69%) as an off white foam.

1. washwashed with water, brine
2. dry with materialthe organic solution dried over Na2SO4
3. filtrationThe mixture was filtered
4. concentrationconcentrated
5. customthe residue was purified by silica gel chromatography