反应详情

Essentially the technique for the appropriate intermediate of Example 22 was used, but substituting 2-(t-butoxycarbonylamino)pyrimidine (293 mg, 1.5 mM) for the pyrazine analogue. To complete the reaction, heating at 80° for 1 hour was necessary, and the chromatography was carried out with a gradient from 0% to 50% ethyl acetate in dichloromethane containing 2% triethylamine. Relevant fractions were combined to give the desired product (427 mg). NMR (DMSO-d6) δ: 1.32 (s, 3H); 1.34 (s, 3H); 1.41 (s, 9H); 2.30 (br, 1H); 2.38 (br, 1H); 3.67 (t, 1H); 3.75 (m, 1H); 3.87 (dd, 1H); 4.00-4.33 (overlapping m, 7H); 4.90 (dd, 1H); 5.01 (m, 1H); 5.87 (s, 1H); 7.27 (t, 1H); 7.31 (d, 2H); 8.73 (d, 2H). MS (ESP): 616 (MH+) for C30H35F2N5O7

1. customthe reaction
2. temperatureheating at 80° for 1 hour