Triethylamine → HCID 22711097、化合物

反応式

FC(F)(F)C(O)=O.[Cl:8][C:9]1[CH:10]=[C:11]2[C:15](=[CH:16][CH:17]=1)[NH:14][C:13]([S:18]([N:21]1[CH2:26][CH2:25][N:24]([C:27]([C:29]3[S:30][C:31]4[CH2:32][NH:33][CH2:34][CH2:35][C:36]=4[N:37]=3)=[O:28])[CH:23]([CH2:38][C:39]([NH:41][S:42]([CH3:45])(=[O:44])=[O:43])=[O:40])[CH2:22]1)(=[O:20])=[O:19])=[CH:12]2.C(N(CC)CC)C.[C:53](=O)([O:61]C1C=CC([N+]([O-])=O)=CC=1)[O:54][CH:55]([O:57][C:58](=[O:60])[CH3:59])[CH3:56]>C(O)C>[C:58]([O:57][CH:55]([O:54][C:53]([CH:34]1[NH:33][CH2:32][C:31]2[S:30][C:29]([C:27]([N:24]3[CH2:25][CH2:26][N:21]([S:18]([C:13]4[NH:14][C:15]5[C:11]([CH:12]=4)=[CH:10][C:9]([Cl:8])=[CH:17][CH:16]=5)(=[O:20])=[O:19])[CH2:22][CH:23]3[CH2:38][C:39]([NH:41][S:42]([CH3:45])(=[O:44])=[O:43])=[O:40])=[O:28])=[N:37][C:36]=2[CH2:35]1)=[O:61])[CH3:56])(=[O:60])[CH3:59]

参加物

実験手順

In ethanol (2 ml) was dissolved N-[[4-[(5-chloroindol-2-yl)sulfonyl]-1-[(4,5,6,7-tetrahydrothiazolo[5,4-c]pyridin-2-yl)carbonyl]piperazin-2-yl]acetyl]methanesulfonamide trifluoroacetate (97 mg), followed by the addition of triethylamine (0.63 ml) and 1-acetoxyethyl p-nitrophenyl carbonate (110 mg). The resulting mixture was stirred at room temperature for 4 hours. The reaction mixture was concentrated under reduced pressure. Methylene chloride was added to the residue. The resulting mixture was washed with water, dried over anhydrous sodium sulfate and distilled to remove the solvent. The residue was purified by chromatography on a silica gel column (methylene chloride:methanol=50:1), whereby the title compound (50 mg) was obtained as a colorless foam.