2-Dimethylaminopyridine → HCID 68914455、化合物

反応式

[C:1]([O:5][C:6](=[O:22])[N:7]([C@H:11]1[CH2:20][CH2:19][C:18]2[C:13](=[CH:14][CH:15]=[C:16]([NH2:21])[CH:17]=2)[CH2:12]1)[CH2:8][CH2:9][CH3:10])([CH3:4])([CH3:3])[CH3:2].CN(C1C=CC=CN=1)C.[F:32][C:33]([F:46])([F:45])[CH2:34][C:35]1[CH:40]=[CH:39][C:38]([S:41](Cl)(=[O:43])=[O:42])=[CH:37][CH:36]=1>O1CCCC1>[C:1]([O:5][C:6](=[O:22])[N:7]([CH2:8][CH2:9][CH3:10])[C@H:11]1[CH2:20][CH2:19][C:18]2[C:13](=[CH:14][CH:15]=[C:16]([NH:21][S:41]([C:38]3[CH:37]=[CH:36][C:35]([CH2:34][C:33]([F:32])([F:45])[F:46])=[CH:40][CH:39]=3)(=[O:43])=[O:42])[CH:17]=2)[CH2:12]1)([CH3:2])([CH3:3])[CH3:4]

参加物

実験手順

((S)-6-Amino-1,2,3,4-tetrahydro-naphthalen-2-yl)-propyl-carbamic acid tert-butyl ester (720 mg, 2.37 mmol) was dissolved in tetrahydrofurane (50 ml). Then, dimethylamino pyridine (100 mg, 0.82 mmol) and 4-(2,2,2-trifluoro-ethyl)benzenesulfonyl chloride (761 mg, 2.37 mmol) were added and the reaction mixture was stirred for 30 minutes at room temperature. The solvent was evaporated under reduced pressure, the residue treated with water and diethyl ether. The organic layer was dried over magnesium sulfate, filtered, and the solvent evaporated under reduced pressure to give the crude product (1.22 g, 95% purity, 93% yield).