1,4-Dioxane hydrochloride → (R)-1-(4-cyclopropyl-benzenesulfonyl)-piperazine-2-carboxylic acid 4-trifluoromethoxy-benzylamide
反応式
Cl.O1CCOCC1.C(OC([N:15]1[CH2:20][CH2:19][N:18]([S:21]([C:24]2[CH:29]=[CH:28][C:27]([CH:30]3[CH2:32][CH2:31]3)=[CH:26][CH:25]=2)(=[O:23])=[O:22])[C@@H:17]([C:33](=[O:47])[NH:34][CH2:35][C:36]2[CH:41]=[CH:40][C:39]([O:42][C:43]([F:46])([F:45])[F:44])=[CH:38][CH:37]=2)[CH2:16]1)=O)(C)(C)C>>[F:46][C:43]([F:44])([F:45])[O:42][C:39]1[CH:40]=[CH:41][C:36]([CH2:35][NH:34][C:33]([C@H:17]2[CH2:16][NH:15][CH2:20][CH2:19][N:18]2[S:21]([C:24]2[CH:29]=[CH:28][C:27]([CH:30]3[CH2:31][CH2:32]3)=[CH:26][CH:25]=2)(=[O:22])=[O:23])=[O:47])=[CH:37][CH:38]=1参加物
3
反応物 2
生成物 1
実験手順
4N Hydrogen chloride/1,4-dioxane solution (1.3 ml) was added to the compound (130 mg) obtained in Step 3, and the mixture was stirred at room temperature for 6 hr. The reaction mixture was concentrated under reduced pressure, and the residue was partitioned by adding ethyl acetate, saturated aqueous sodium hydrogen carbonate solution and water. The organic layer was dried over anhydrous magnesium sulfate, filtrated, and concentrated under reduced pressure. The residue was purified by thin layer silica gel chromatography (chloroform:methanol=9:1) to give the title compound (88 mg).