反应详情

The process is carried out as in stage 3 of Example 3, but using 150 mg of 2-fluoro-4-[4-(6-fluoro-1H-benzimidazol-2-yl)carbazol-9-yl]benzonitrile, obtained according to stage 2 of Example 3, 148 mg of potassium carbonate, 1.314 g of 2-(1H-imidazol-1-yl)ethylamine dihydrochloride and 1.445 g of triethylamine in 2 ml of dimethyl sulphoxide. 0.678 ml of a 1M aqueous solution of sodium hydroxide, 0.656 ml of a 30% aqueous solution of hydrogen peroxide and 3 ml of ethanol are then added to the reaction medium. After treatment as in stage 3 of Example 3, and then purification by flash chromatography on silica gel, elution being carried out with a mixture of dichloromethane and ethanol (90/10 by volume), followed by crystallization from 2 ml of ethyl acetate, 130 mg of 4-[4-(6-fluoro-1H-benzimidazol-2-yl)-9H-carbazol-9-yl]-2-[2-(1H-imidazol-1-yl)ethylamino]benzamide are thus obtained in the form of a beige solid, the characteristics of which are the following:

1. customobtained
2. customAfter treatment as in stage 3 of Example 3, and then purification by flash chromatography
3. washon silica gel, elution
4. additionbeing carried out with a mixture of dichloromethane and ethanol (90/10 by volume)
5. customfollowed by crystallization from 2 ml of ethyl acetate, 130 mg of 4-[4-(6-fluoro-1H-benzimidazol-2-yl)-9H-carbazol-9-yl]-2-[2-(1H-imidazol-1-yl)ethylamino]benzamide
6. customare thus obtained in the form of a beige solid