Reaction #41575

Reaction equation

1H-pyrazole-3-carboxaldehyde

4-(2-fluoro-phenoxy)-5-(6-methanesulfonyl-pyridin-3-yloxy)-benzene-1,2-diamine

→

compound

5-(2-Fluoro-phenoxy)-2-(1H-pyrazol-3-yl)-6-(6-methanesulfonyl-pyridin-3-yloxy)-1H-benzimidazole

Solvents

dimethylformamide

Conditions

Workup

1. 1
   Otherthe reaction liquid
2. 2
   OtherThe solvent was evaporated away under reduced pressure
3. 3
   Otherthe resulting residue was purified
4. 4
   Otherthrough partitioning thin-layer chromatography (Kieselgel™ 60F254, Art 5744 (by Merck), chloroform/methanol=9/1)

Procedure

3.9 mg of 1H-pyrazole-3-carboxaldehyde was added to a dimethylformamide (0.5 ml) solution of 15 mg of 4-(2-fluoro-phenoxy)-5-(6-methanesulfonyl-pyridin-3-yloxy)-benzene-1,2-diamine obtained in Example 200, and the reaction liquid was stirred at 90° C. for 30 minutes. The solvent was evaporated away under reduced pressure, and the resulting residue was purified through partitioning thin-layer chromatography (Kieselgel™ 60F254, Art 5744 (by Merck), chloroform/methanol=9/1) to obtain the entitled compound as a white solid.

Source