反应详情

The process is carried out as in stage 2 of Example 3, but using 300 mg of 2-fluoro-4-[4-(quinolin-3-yl)-9H-carbazol-9-yl]benzonitrile, obtained according to stage 1 of Example 32, 301 mg of potassium carbonate and 1.50 g of 4-amino-2(R,S)-methylbutanol in 3 ml of dimethyl sulphoxide. 1.38 ml of a 1M aqueous solution of sodium hydroxide, 1.336 ml of a 30% aqueous solution of hydrogen peroxide and 7 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, 225 mg of 4-[4-(quinolin-3-yl)-9H-carbazol-9-yl]-2-(4-hydroxy-3(R,S)-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, 225 mg of 4-[4-(quinolin-3-yl)-9H-carbazol-9-yl]-2-(4-hydroxy-3(R,S)-methylbutylamino)benzamide
6. customare thus obtained in the form of a beige solid