Hydrochloric Acid → 5-Amino-2-(4-amino-3-fluorophenyl)-6,8-difluoro-4H-1-benzopyran-4-one
Reaction equation
[F:1][C:2]1[CH:3]=[C:4]([F:34])[C:5]2[O:10][C:9]([C:11]3[CH:16]=[CH:15][C:14]([NH:17]C(=O)C(C)(C)C)=[C:13]([F:24])[CH:12]=3)=[CH:8][C:7](=[O:25])[C:6]=2[C:26]=1[NH:27]C(=O)C(C)(C)C.Cl>O1CCOCC1>[NH2:27][C:26]1[C:6]2[C:7](=[O:25])[CH:8]=[C:9]([C:11]3[CH:16]=[CH:15][C:14]([NH2:17])=[C:13]([F:24])[CH:12]=3)[O:10][C:5]=2[C:4]([F:34])=[CH:3][C:2]=1[F:1]Participants
4
Procedure
3.90 g of Compound 25 was dissolved in 180 ml of dioxane, 180 ml of concentrated hydrochloric acid was added and the mixture was heated at reflux for 3 hours. The reaction solution was cooled on ice, and the precipitated crystals were collected by filtration and recrystallized from methanol/chloroform to give 1.31 g (52%) of Compound 26.