反应详情

16 mg of imidazole and 40.5 mg of methylphenylphosphinic chloride are added to a solution of 27 mg of 3-[1-tert-butoxycarbonyl-5-(2-morpholin-4-yl-ethoxy)-1H-indol-2-yl]-5-hydroxyindazole-1-carboxylic acid tert-butyl ester in 2 ml of dichloromethane. The solution obtained is stirred at ambient temperature. After stirring for 15 hours, a further 16 mg of imidazole and 40.5 mg of methylphenylphosphinic chloride are added and the mixture is stirred at ambient temperature for another 3½ hours in order for the reaction to be complete. The reaction mixture is then filtered and evaporated under reduced pressure in a rotary evaporator. The residue obtained is purified by LC/MS to obtain 10.5 mg of 3-[1-tert-butoxycarbonyl-5-(2-morpholin-4-ylethoxy)-1H-indol-2-yl]-5-(methylphenylphosphinoyloxy)indazole-1-carboxylic acid tert-butyl ester.

1. customThe solution obtained
2. stirringAfter stirring for 15 hours
3. stirringthe mixture is stirred at ambient temperature for another 3½ hours in order for the reaction
4. filtrationThe reaction mixture is then filtered
5. customevaporated under reduced pressure in a rotary evaporator
6. customThe residue obtained
7. customis purified by LC/MS