反应详情

Using essentially the method for the intermediate of Example 12, starting from 3-(4-(3(S)-aminopyrrolidin-1-yl)-3-fluorophenyl)-5(R)-(N-(2,2,2-trichloroethyloxycarbonyl)isoxazol-3-ylaminomethyl)oxazolidin-2-one hydrochloride salt (400 mg, 0.74 mM) and methanesulfonyl chloride gave the desired product (361 mg ). NMR (DMSO-d6) δ: 1.87 (hextet, 1H); 2.19 (hextet, 1H); 2.97 (s, 3H); 3.20 (m, 1H); 3.30 (m, 1H); 3.37 (m, 1H); 3.54 (m overlapped by H2O, ˜1H); 3.83 (dd, 1H); 3.97 (dd, 1H); 4.13 (dd overlapping m, 2H); 4.36 (dd, 1H); 4.97 (d, 1H); 5.02 (m, 1H); 5.07 (d, 1H); 6.74 (t, 1H); 6.88 (d, 1H); 7.09 (dd, 1H); 7.36 (dd overlapping br, 2H); 8.89 (d, 1H). MS (ESP): 578 (MH+) for C21H23Cl3FN5O7S