反应详情

温度

45 °C

A mixture of 5-bromo-1H-pyrazolo[3,4-b]pyridine-3-carboxylic acid Compound 1c (200 mg, 0.826 mmol), 4-methoxy-benzene-1,2-diamine Compound 19a (114 mg, 0.826 mmol), HATU (314 mg, 0.826 mmol) and DIPEA (213 mg, 1.652 mmol) in DMF (10 mL) was stirred and heated to 45° C. overnight. The mixture was diluted with AcOEt (60 mL) and washed with water. The organic layer was separated, dried and evaporated to give a brown solid residue. The residue was recrystallized with AcOEt/hexane mixture to give 5-bromo-1H-pyrazolo[3,4-b]pyridine-3-carboxylic acid (2-amino-5-methoxy-phenyl)-amide Compound 19b (221 mg, 74% yield) as a light brown powder. MS m/z 362 (M+).

1. washwashed with water
2. customThe organic layer was separated
3. customdried
4. customevaporated
5. customto give a brown solid residue
6. customThe residue was recrystallized with AcOEt/hexane mixture