반응식
Br[C:2]1[CH:3]=[C:4]2[C:13](=[CH:14][C:15]=1[F:16])[CH:12]1[CH2:17][CH:10]([CH2:11]1)[N:9]1[C:5]2=[N:6][C:7]([C:22]([NH2:24])=[O:23])=[C:8]1[C:18]([NH:20][CH3:21])=[O:19].[CH3:25][C:26]1[O:30][N:29]=[C:28]([C@:31]([OH:35])([C:33]#[CH:34])[CH3:32])[N:27]=1>>[F:16][C:15]1[CH:14]=[C:13]2[C:4]([C:5]3[N:9]([CH:10]4[CH2:17][CH:12]2[CH2:11]4)[C:8]([C:18]([NH:20][CH3:21])=[O:19])=[C:7]([C:22]([NH2:24])=[O:23])[N:6]=3)=[CH:3][C:2]=1[C:34]#[C:33][C@@:31]([OH:35])([C:28]1[N:27]=[C:26]([CH3:25])[O:30][N:29]=1)[CH3:32]참가 물질
반응물 2
생성물 1
실험 절차
9-Bromo-10-fluoro-3-N-methyl-2,5-diazatetracyclo[11.1.1.0[2,6].0[7,12]]pentadeca-3,5,7,9,11-pentaene-3,4-dicarboxamide (125 mg) was reacted with (2R)-2-(5-methyl-1,2,4-oxadiazol-3-yl)but-3-yn-2-ol similar to as described in General Procedure G to afford 14.5 mg of 10-fluoro-9-[(3R)-3-hydroxy-3-(5-methyl-1,2,4-oxadiazol-3-yl)but-1-yn-1-yl]-3-N-methyl-2,5-diazatetracyclo[11.1.1.0[2,6].0[7,12]]pentadeca-3,5,7,9,11-pentaene-3,4-dicarboxamide following reverse phase hplc purification. MS (Q1) 465 (M)+. 1H NMR (400 MHz, DMSO) δ 10.58 (q, J=4.1 Hz, 1H), 8.86 (d, J=7.5 Hz, 1H), 8.28 (s, 1H), 7.74 (s, 1H), 7.33 (d, J=10.0 Hz, 1H), 6.79 (s, 1H), 6.13-6.05 (m, 1H), 3.74-3.63 (m, 1H), 3.18-3.05 (m, 2H), 2.78 (d, J=4.6 Hz, 2H), 2.62 (s, 3H), 1.87 (s, 3H), 1.68 (d, J=12.3 Hz, 2H).
출처 및 근거
- ORD 기록
- ord-f2ae9515a649472f868c3a1dd309a142
- 출처 데이터셋
- uspto-grants-2015_05
- 특허 번호
- US09034866B2
연결된 노트
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