반응 #1964682

반응 방정식

2-fluoro-4-[4-(6-fluoro-1H-benzimidazol-2-yl)-9H-carbazol-9-yl]benzonitrile

sodium hydroxide

hydrogen peroxide

potassium carbonate

1-(aminomethyl)cyclopropan-1-ol

→

4-[4-(6-fluoro-1H-benzimidazol-2-yl)-9H-carbazol-9-yl]-2-[(1-hydroxycyclopropan-1-yl)methylamino]benzamide

용매

ethanol

dimethyl sulphoxide

반응 조건

후처리

1. 1
   기타obtained
2. 2
   기타After treatment as in stage 3 of Example 3, and then purification by flash chromatography
3. 3
   세척on silica gel, elution
4. 4
   workup.ADDITIONbeing carried out with a mixture of dichloromethane and methanol (95/5 by volume), 26 mg of 4-[4-(6-fluoro-1H-benzimidazol-2-yl)-9H-carbazol-9-yl]-2-[(1-hydroxycyclopropan-1-yl)methylamino]benzamide
5. 5
   기타are thus obtained in the form of a pale yellow powder

실험 절차

The process is carried out as in stage 3 of Example 3, but using 168.2 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, 165.8 mg of potassium carbonate and 279 mg of 1-(aminomethyl)cyclopropan-1-ol in 1.7 ml of dimethyl sulphoxide, in a microwave for 1 hour and 30 minutes at 115° C. 0.76 ml of a 1M aqueous solution of sodium hydroxide, 0.735 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 methanol (95/5 by volume), 26 mg of 4-[4-(6-fluoro-1H-benzimidazol-2-yl)-9H-carbazol-9-yl]-2-[(1-hydroxycyclopropan-1-yl)methylamino]benzamide are thus obtained in the form of a pale yellow powder, the characteristics of which are the following:

출처