Pyrazole → 2-Pyrazol-1-yl-quinazolin-8-ol

反応式

Cl[C:2]1[N:11]=[CH:10][C:9]2[C:4](=[C:5]([O:12]C)[CH:6]=[CH:7][CH:8]=2)[N:3]=1.[NH:14]1[CH:18]=[CH:17][CH:16]=[N:15]1.B(Br)(Br)Br>>[N:14]1([C:2]2[N:11]=[CH:10][C:9]3[C:4](=[C:5]([OH:12])[CH:6]=[CH:7][CH:8]=3)[N:3]=2)[CH:18]=[CH:17][CH:16]=[N:15]1

参加物

反応物 3

HCID 1048Pyrazole

HCID 25134Boron tribromide

HCID 199886952-Chloro-8-methoxyquinazoline

生成物 1

HCID 685622682-Pyrazol-1-yl-quinazolin-8-ol

実験手順

A mixture of the 2-chloride 113 (0.5 mmol) and pyrazole (2.5 mmol) was heated at 175° C. in a steel autoclave for 48 h. The crude product was then treated with BBr3 according to the procedure described in Example 6. Subsequent purification by column chromatography gave 2-pyrazol-1-yl-quinazolin-8-ol (A131).