(5R)-3-(4-(1-benzyl-1,2,5,6-tetrahydropyridin-4-yl)-3,5-difluorophenyl)-5-hydroxymethyloxazolidin-2-one → (5R)-3-(4-(1-Benzyl-1,2,5,6-tetrahydropyridin-4-yl)-3,5-difluorophenyl)-5-(2-oxo-3H-1,3,4-thiadiazol-3-ylmethyl)oxazolidin-2-one
反応式
[CH2:1]([N:8]1[CH2:13][CH2:12][C:11]([C:14]2[C:19]([F:20])=[CH:18][C:17]([N:21]3[CH2:25][C@H:24]([CH2:26]O)[O:23][C:22]3=[O:28])=[CH:16][C:15]=2[F:29])=[CH:10][CH2:9]1)[C:2]1[CH:7]=[CH:6][CH:5]=[CH:4][CH:3]=1.[S:30]1[CH:34]=[N:33][NH:32][C:31]1=[O:35]>>[CH2:1]([N:8]1[CH2:13][CH2:12][C:11]([C:14]2[C:19]([F:20])=[CH:18][C:17]([N:21]3[CH2:25][C@H:24]([CH2:26][N:32]4[N:33]=[CH:34][S:30][C:31]4=[O:35])[O:23][C:22]3=[O:28])=[CH:16][C:15]=2[F:29])=[CH:10][CH2:9]1)[C:2]1[CH:3]=[CH:4][CH:5]=[CH:6][CH:7]=1参加物
3
反応物 2
生成物 1
実験手順
Essentially the procedure of Example 35 was used, but starting with (5R)-3-(4-(1-benzyl-1,2,5,6-tetrahydropyridin-4-yl)-3,5-difluorophenyl)-5-hydroxymethyloxazolidin-2-one (800 mg, 2 mM), and 3H-1,3,4-thiadiazol-2-one (214 mg, 2.2 mM, Helv. Chim. Acta, 1982, 65, 2606), and stirring the reaction for 18 hours. After elution from the SCX column, the gum after evaporation was triturated with diethyl ether to give the desired product (291 mg).