反应详情

Boc-N-Me-Ala-OH (107.91 mg, 0.532 mmol), DIPEA (0.251 mL, 1.45 mmol) and HATU (220.37 mg, 0.58 mmol) were added to a solution of (S)-3-amino-1-(5-bromo-2-methoxy-naphthalen-1-ylmethyl)-1,3,4,5-tetrahydro-benzo[b][1,4]diazepin-2-one trifluoroacetate (260 mg) in DMF (4 mL) at 0° C. After 3 h the mixture was diluted with water and extracted with ethyl acetate. The extracts were washed with 1 M aqueous citric acid solution, brine, saturated aqueous sodium carbonate solution, dried and concentrated. The residue was purified by silica gel chromatography to afford the title compound (282 mg, 51%) as an off white solid. LC-MS: 613.2 (M+H).

1. extractionextracted with ethyl acetate
2. washThe extracts were washed with 1 M aqueous citric acid solution, brine, saturated aqueous sodium carbonate solution
3. customdried
4. concentrationconcentrated
5. customThe residue was purified by silica gel chromatography