6-Aminoquinoline → 2-chloro-5-fluoro-N4-(quinolin-6-yl)-4-pyrimidineamine

HRID 76419

反応式

HRID 76419 の反応式
[Cl:1][C:2]1[N:7]=[C:6](Cl)[C:5]([F:9])=[CH:4][N:3]=1.[NH2:10][C:11]1[CH:12]=[C:13]2[C:18](=[CH:19][CH:20]=1)[N:17]=[CH:16][CH:15]=[CH:14]2>>[Cl:1][C:2]1[N:7]=[C:6]([NH:10][C:11]2[CH:12]=[C:13]3[C:18](=[CH:19][CH:20]=2)[N:17]=[CH:16][CH:15]=[CH:14]3)[C:5]([F:9])=[CH:4][N:3]=1

参加物

3

反応物 2

HCID 113736-AminoquinolineHCID 2507052,4-Dichloro-5-fluoropyrimidine

生成物 1

HCID 220605312-chloro-5-fluoro-N4-(quinolin-6-yl)-4-pyrimidineamine

実験手順

In like manner to the preparation of 2-chloro-5-fluoro-N4-[3-(1H-tetrazol-5-yl)phenyl]-4-pyrimidineamine the reaction of 2,4-dichloro-5-fluoropyrimidine with 6-aminoquinoline gave 2-chloro-5-fluoro-N4-(quinolin-6-yl)-4-pyrimidineamine. 1H NMR (CDCl3): δ 8.02 (dd, 1H, J=2.7 Hz), 8.00 (dd, 1H, J=2.4 Hz), 7.73 (d, 1H, J=9 Hz), 7.68 (dd, 1H, J=2.4 and 8.7 Hz), 7.28 (t, 1H, J=10.5 Hz), 6.42 (d, 1H, J=9.3 Hz); 19F NMR (CDCl3): −44344; LCMS: purity: 91%; MS (m/e): 292 (M+).

後処理

  1. customIn like manner to the preparation of 2-chloro-5-fluoro-N4-[3-(1H-tetrazol-5-yl)phenyl]-4-pyrimidineamine

出典と根拠

ORDレコード
ord-8b5d7dfa977d4169a2a8593b326e69c8
出典データセット
uspto-grants-2014_09
特許番号
US08835430B2

関連ノート

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