Benzyl Bromide → 1-Benzyl-5-[2-(pyridin-3-yloxymethyl)pyrrolidin-1-yl]sulfonylindole-2,3-dione
反応式
CN1[C:10]2[C:5](=[CH:6][C:7](S(N3CCC[C@H]3COC3C=CC=CC=3)(=O)=O)=[CH:8][CH:9]=2)[C:4](=O)C1=O.[N:29]1[CH:34]=[CH:33][CH:32]=[C:31]([O:35][CH2:36][CH:37]2[CH2:41][CH2:40][CH2:39][N:38]2[S:42]([C:45]2[CH:46]=[C:47]3[C:51](=[CH:52][CH:53]=2)[NH:50][C:49](=[O:54])[C:48]3=[O:55])(=[O:44])=[O:43])[CH:30]=1.C(Br)C1C=CC=CC=1>>[CH2:4]([N:50]1[C:51]2[C:47](=[CH:46][C:45]([S:42]([N:38]3[CH2:39][CH2:40][CH2:41][CH:37]3[CH2:36][O:35][C:31]3[CH:30]=[N:29][CH:34]=[CH:33][CH:32]=3)(=[O:44])=[O:43])=[CH:53][CH:52]=2)[C:48](=[O:55])[C:49]1=[O:54])[C:5]1[CH:10]=[CH:9][CH:8]=[CH:7][CH:6]=1参加物
4
実験手順
1-Benzyl-5-(2-(pyridin-3-yl-oxymethyl)-pyrrolidine-1-sulfonyl)-1H-indole-2,3-dione (21b) was prepared according to the same procedure for compound 11a, except using compound 20 and benzyl bromide, and the crude product was purified with ether to afford 61 mg (51%) of 21b as a yellow solid, mp 79.6-80.7° C. 1H NMR (300 MHz, CDCl3) δ 8.25 (s, 1H), 8.22 (t, J=2.7 Hz, 1H), 8.04 (d, J=2.1 Hz, 1H), 7.98 (dd, J=8.4 Hz, J=2.1 Hz, 1H), 7.36 (m, 5H), 7.22 (m, 2H), 6.91 (d, J=8.8 Hz, 1H), 4.97 (s, 2H), 4.25 (m, 1H), 3.99-3.94 (m, 2H), 3.55-3.48 (m, 1H), 3.21-3.15 (m, 1H), 2.10-1.97 (m, 2H), 1.84-1.75 (m, 2H). LRMS (FAB) m/e: 484.1 (M+Li, 100); HRMS (FAB) m/e calcd for C25H23N3O5SLi (M+Li) 484.1518, found 484.1539.