Benzenesulfonyl chloride → HCID 18674042、化合物

反応式

[C:1]1([S:7](Cl)(=[O:9])=[O:8])[CH:6]=[CH:5][CH:4]=[CH:3][CH:2]=1.O1CCCC1.[NH2:16][C:17]1[C:21]([C:22]2[CH:27]=[CH:26][N:25]=[CH:24][CH:23]=2)=[C:20]([C:28]2[CH:33]=[CH:32][C:31]([F:34])=[CH:30][CH:29]=2)[NH:19][N:18]=1>C(N(CC)CC)C>[F:34][C:31]1[CH:30]=[CH:29][C:28]([C:20]2[NH:19][N:18]=[C:17]([NH:16][S:7]([C:1]3[CH:6]=[CH:5][CH:4]=[CH:3][CH:2]=3)(=[O:9])=[O:8])[C:21]=2[C:22]2[CH:27]=[CH:26][N:25]=[CH:24][CH:23]=2)=[CH:33][CH:32]=1

参加物

実験手順

Under a stream of argon gas, 333 mg of benzenesulfonyl chloride was added dropwise to 4 ml of a tetrahydrofuran solution containing 150 mg of 3-amino-5-(4-fluorophenyl)-4-(4-pyridyl)pyrazole and 191 mg of triethylamine, followed by stirring at room temperature for 1.5 hours. After the reaction mixture was concentrated under reduced pressure, the resulting residue was purified by column chromatography using 20 g of silica gel [with an elution solvent comprising chloroform-methanol (100:1)]. Thus, 35 mg (15% yield) of the title compound was obtained as a pale-yellow powder.