反应详情

The process is carried out as in stage 3 of Example 3, but using 155.6 mg of 2-fluoro-4-[4-(6-fluoro-1H-benzimidazol-2-yl)-9H-carbazol-9-yl]benzonitrile, obtained according to stage 2 of Example 3, 153.4 mg of potassium carbonate, 1.033 g of 4-amino-2-methylbutan-2-ol hydrochloride and 0.749 g of triethylamine in 2 ml of dimethyl sulphoxide. 0.703 ml of a 1M aqueous solution of sodium hydroxide, 0.681 ml of a 30% aqueous solution of hydrogen peroxide and 4 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 (95/5 by volume), followed by crystallization from 5 ml of ethyl acetate, 185 mg of 4-[4-(6-fluoro-1H-benzimidazol-2-yl)-9H-carbazol-9-yl]-2-(3-hydroxy-3-methylbutylamino)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 (95/5 by volume)
5. customfollowed by crystallization from 5 ml of ethyl acetate, 185 mg of 4-[4-(6-fluoro-1H-benzimidazol-2-yl)-9H-carbazol-9-yl]-2-(3-hydroxy-3-methylbutylamino)benzamide
6. customare thus obtained in the form of a beige solid