Cl.[O:2]=[C:3]1[CH:7]([CH2:8][CH2:9][C:10]2[CH:19]=[CH:18][C:17]3[CH2:16][CH2:15][CH2:14][NH:13][C:12]=3[N:11]=2)[CH2:6][CH2:5][N:4]1[CH2:20][C:21]([OH:23])=O.CN1CCOCC1.CC#N.F[P-](F)(F)(F)(F)F.[N:41]1(O[P+](N(C)C)(N(C)C)N(C)C)[C:45]2C=CC=[CH:49][C:44]=2N=N1.[CH3:61][CH2:62][O:63][C:64]([CH3:66])=[O:65]>>[CH2:62]([O:63][C:64](=[O:65])[CH2:66][C@@H:45]([C:44]#[CH:49])[NH:41][C:21](=[O:23])[CH2:20][N:4]1[CH2:5][CH2:6][CH:7]([CH2:8][CH2:9][C:10]2[CH:19]=[CH:18][C:17]3[CH2:16][CH2:15][CH2:14][NH:13][C:12]=3[N:11]=2)[C:3]1=[O:2])[CH3:61]To a stirred solution of 2-8 (50 mg, 0.15 mmol), 2-9 (29 mg, 0.17 mmol) (Zablocki et al., J. Med Chem., 1995, 38, 2378), NMM (83 μL, 0.75 mmol), and CH3CN (1 mL) was added BOP (74 mg, 0.17 mmol). After 20 h, the reaction mixture was diluted with EtOAc and then washed with sat. NaHCO3, H2O and brine, dried (MgSO4), and concentrated to give 2-11 as a yellow oil.
読み込み中…