[F:1][C:2]1[CH:38]=[CH:37][C:5]([CH2:6][NH:7][C:8]([C:10]2[C:18]3[C:13](=[CH:14][C:15]([C:19]([NH:21][CH2:22][C:23]([OH:26])([CH3:25])[CH3:24])=O)=[CH:16][CH:17]=3)[N:12]([CH2:27][C:28]3[CH:33]=[CH:32][CH:31]=[CH:30][N:29]=3)[C:11]=2[CH:34]([CH3:36])[CH3:35])=[O:9])=[CH:4][CH:3]=1.C(N1C2C(=CC=C(C(NCC(O)(C)C)=O)C=2)C(C(NCC2C=CC(F)=C(F)C=2)=O)=C1C(C)C)C1C=CC=CC=1.O=P12OP3(OP(OP(O3)(O1)=O)(=O)O2)=O>C1C=CC=CC=1>[CH3:25][C:23]1([CH3:24])[O:26][C:19]([C:15]2[CH:14]=[C:13]3[C:18]([C:10]([C:8]([NH:7][CH2:6][C:5]4[CH:4]=[CH:3][C:2]([F:1])=[CH:38][CH:37]=4)=[O:9])=[C:11]([CH:34]([CH3:36])[CH3:35])[N:12]3[CH2:27][C:28]3[CH:33]=[CH:32][CH:31]=[CH:30][N:29]=3)=[CH:17][CH:16]=2)=[N:21][CH2:22]1To a solution of N3-(4-fluorobenzyl)-N6-(2-hydroxy-2-methylpropyl)-2-isopropyl-1-(pyridin-2-ylmethyl)-1H-indole-3,6-dicarboxamide (Compound 68, 23 mg, 0.043 mmol) in benzene (6 ml) at 25° C. was added P2O5 (120 mg, 0.86 mmol). The mixture was stirred at 50° C. for 4 h, quenched with 6N NaOH (1 ml), extracted several times with EtOAc, washed with H2O, brine, dried over Na2SO4, concentrated in vacuo. The residue was purified by chromatography on silica gel (100% EtOAc) to yield the title compound as yellow oil.
読み込み中…