4-Bromo-2-fluoroaniline → Jtp-70902
반응식
[CH:1]1([N:4]2[C:9](=[O:10])[C:8]3[C:11](OS(C4C=CC(C)=CC=4)(=O)=O)=[CH:12][C:13](=[O:16])[N:14]([CH3:15])[C:7]=3[N:6]([C:28]3[CH:33]=[CH:32][CH:31]=[C:30]([NH:34][S:35]([CH3:38])(=[O:37])=[O:36])[CH:29]=3)[C:5]2=[O:39])[CH2:3][CH2:2]1.[F:40][C:41]1[CH:47]=[C:46]([Br:48])[CH:45]=[CH:44][C:42]=1[NH2:43]>>[Br:48][C:46]1[CH:45]=[CH:44][C:42]([NH:43][C:11]2[C:8]3[C:9](=[O:10])[N:4]([CH:1]4[CH2:3][CH2:2]4)[C:5](=[O:39])[N:6]([C:28]4[CH:29]=[C:30]([NH:34][S:35]([CH3:38])(=[O:37])=[O:36])[CH:31]=[CH:32][CH:33]=4)[C:7]=3[N:14]([CH3:15])[C:13](=[O:16])[CH:12]=2)=[C:41]([F:40])[CH:47]=1참가 물질
3
반응 조건
- 온도
- 135 °C
실험 절차
To toluene-4-sulfonic acid 3-cyclopropyl-1-(3-methanesulfonylaminophenyl)-8-methyl-2,4,7-trioxo-1,2,3,4,7,8-hexahydropyrido[2,3-d]pyrimidin-5-yl ester 15 (3.5 g) obtained in Step 8 was added 2-fluoro-4-bromoaniline 16 (23 g), and the mixture was stirred under heating at 135° C. for 3 hrs. The reaction mixture was purified by column chromatography (chloroform:acetone=9:1) to give N-{3-[5-(4-bromo-2-fluoro-phenylamino)-3-cyclopropyl-8-methyl-2,4,7-trioxo-3,4,7,8-tetrahydro-2H-pyrido[2,3-d]pyrimidin-1-yl]phenyl}-methanesulfonamide 17 (3.0 g, 83%) as a white solid.