反应详情

A mixture of 2-{2,6-dichloro-3-[(2,2-dimethyl-propionylamino)-methyl]-phenylamino}-6-[3,3-difluoro-pyrrolidinyl]-1-methyl-1H-benzimidazole-5-carboxylic acid (50 mg, 0.090 mmol), (1-chloro-2-methyl-propenyl)-dimethylamine (0.026 mL, 0.20 mmol) and DCM (2 mL) is stirred for 30 min. This mixture is added to 4-trifluoromethoxyaniline (0.100 mmol) and pyridine (25 μL, 0.32 mmol) in MeCN (1 mL) and it is stirred for 2 h at 40° C. and overnight at 60° C. The mixture is concentrated and the residue diluted with DMF/water 19/1 (2 mL) and purified via reverse phase HPLC.

1. stirringis stirred for 2 h at 40° C. and overnight at 60° C
2. concentrationThe mixture is concentrated
3. additionthe residue diluted with DMF/water 19/1 (2 mL)
4. custompurified via reverse phase HPLC