Boronic acid, 3-thienyl-, bis(1-methylethyl) ester → HCID 22478420、化合物
反応式
Cl.Br[C:3]1[CH:4]=[C:5]2[C:10](=[CH:11][CH:12]=1)[N:9]=[CH:8][N:7]=[C:6]2[NH:13][C:14]1[CH:19]=[CH:18][C:17]([F:20])=[C:16]([Cl:21])[CH:15]=1.[S:22]1[CH:26]=[CH:25][C:24](B(OC(C)C)OC(C)C)=[CH:23]1>>[Cl:21][C:16]1[CH:15]=[C:14]([CH:19]=[CH:18][C:17]=1[F:20])[NH:13][C:6]1[C:5]2[C:10](=[CH:11][CH:12]=[C:3]([C:24]3[CH:25]=[CH:26][S:22][CH:23]=3)[CH:4]=2)[N:9]=[CH:8][N:7]=1参加物
3
実験手順
Using an analogous procedure to that described in Example 5 except that the reaction mixture was heated to reflux for 2 hours, 6-bromo4-(3-chloro-4-fluoroanilino)quinazoline hydrochloride salt was reacted with di-isopropyl 3-thienylboronate to give 4-(3-chloro-4-fluoroanilino)-6-(3-thienyl)quinazoline in 51% yield, m.p. 195-197° C.; NMR Spectrum: 7.5 (t, 1H), 7.7-7.9 (m, 4H), 8.05 (m, 1H), 8.2 (m, 1H), 8.25 (m, 1H), 8.6 (s, 1H), 8.8 (d, 1H), 9.9 (broad s, 1H); Elemental Analysis: Found C, 57.8; H, 3.3; N, 10.6; C18H11ClFN3S 1.15H2O requires C, 57.4; H, 3.6; N, 11.2%.
後処理
- temperaturewas heated