4-Bromo-1-methyl-1H-pyrazole-3-carbonyl chloride → 4-bromo-N-[3-fluoro-4-[[6-methoxy-7-(3-morpholinopropoxy)-4-quinolyl]oxy]phenyl]-1-methyl-pyrazole-3-carboxamide

HRID 1465198

反応式

HRID 1465198 の反応式
[F:1][C:2]1[CH:3]=[C:4]([CH:6]=[CH:7][C:8]=1[O:9][C:10]1[C:19]2[C:14](=[CH:15][C:16]([O:22][CH2:23][CH2:24][CH2:25][N:26]3[CH2:31][CH2:30][O:29][CH2:28][CH2:27]3)=[C:17]([O:20][CH3:21])[CH:18]=2)[N:13]=[CH:12][CH:11]=1)[NH2:5].[Br:32][C:33]1[C:34]([C:39](Cl)=[O:40])=[N:35][N:36]([CH3:38])[CH:37]=1>>[Br:32][C:33]1[C:34]([C:39]([NH:5][C:4]2[CH:6]=[CH:7][C:8]([O:9][C:10]3[C:19]4[C:14](=[CH:15][C:16]([O:22][CH2:23][CH2:24][CH2:25][N:26]5[CH2:31][CH2:30][O:29][CH2:28][CH2:27]5)=[C:17]([O:20][CH3:21])[CH:18]=4)[N:13]=[CH:12][CH:11]=3)=[C:2]([F:1])[CH:3]=2)=[O:40])=[N:35][N:36]([CH3:38])[CH:37]=1

参加物

3

反応物 2

HCID 6051064-Bromo-1-methyl-1H-pyrazole-3-carbonyl chlorideHCID 469280403-Fluoro-4-(6-methoxy-7-(3-morpholinopropoxy)quinolin-4-yloxy)aniline

生成物 1

HCID 568467384-bromo-N-[3-fluoro-4-[[6-methoxy-7-(3-morpholinopropoxy)-4-quinolyl]oxy]phenyl]-1-methyl-pyrazole-3-carboxamide

実験手順

Q2 was prepared from 3-fluoro-4-[[6-methoxy-7-(3-morpholinopropoxy)-4-quinolyl]oxy]aniline and 4-bromo-1-methyl-1H-pyrazole-3-carbonyl chloride following the general procedure reported in Preparative Example 1 Step 3. 1H NMR (400 MHz, d4-MeOD, 300K) δ 2.20 (m, 2H), 2.73 (m, 4H), 2.81 (t, J=7.4 Hz, 2H), 3.80 (t, J=4.7 Hz, 4H), 4.02 (s, 3H), 4.05 (s, 3H), 4.29 (t, J=6.1 Hz, 2H), 6.54 (dd, J=5.4 Hz, J=1.0 Hz, 1H), 7.37 (t, J=9.0 Hz, 1H), 7.38 (s, 1H), 7.61 (d, J=8.8 Hz, 1H), 7.68 (s, 1H), 7.86 (s, 1H), 7.95 (dd, J=12.9 Hz, J=2.4 Hz, 1H), 8.45 (d, J=5.4 Hz, 1H). MS (ES) C28H29BrFN5O5 requires: 614. Found: 614/616 (M+H)+.

出典と根拠

ORDレコード
ord-1a725304f2cd46b1ac73a6c64a0791b0
出典データセット
uspto-grants-2015_04
特許番号
US08999982B2

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