反应详情

To a solution of (R)-3-(3-amino-6-methyl-pyridin-2-ylamino)-3-phenyl-propionic acid ethyl ester (390 mg, 1.30 mmol) in THF (10 mL) was added CDI (317 mg, 1.95 mmol). The reaction mixture was stirred at room temperature for 2 hours and then heated to 60° C. for another 2 hours. The reaction mixture was diluted with ethyl acetate and washed with water. The organic phase was dried over Na2SO4 and concentrated. The resulting residue was purified by silica gel prep TLC using 95:5 CH2Cl2:MeOH as an eluent to afford 250 mg (59%) of the title compound as a light brown foamy residue. LCMS, M++1, m/z: 326.43

1. temperatureheated to 60° C. for another 2 hours
2. washwashed with water
3. dry with materialThe organic phase was dried over Na2SO4
4. concentrationconcentrated
5. customThe resulting residue was purified by silica gel prep TLC