Triphosgene → 1-[4-(4-Methyl-piperazin-1-ylmethyl)-3-trifluoromethyl-phenyl]-3-[3-(1-methyl-1H-pyrazolo[3,4-c]pyridin-4-ylethynyl)-phenyl]-urea

Participants

Reaction Steps

124 mg of 3-(1-methyl-1H-pyrazolo[3,4-c]pyridin-4-ylethynyl)-phenylamine (Intermediate 3.1, 0.5 mmol, 1 eq.) were dissolved in 9 mL acetonitrile and treated with 163 mg of 4-(4-methyl-piperazin-1-ylmethyl)-3-trifluoromethyl-phenylamine (0.6 mmol, 1 eq.) and 59 mg of triphosgene (0.2 mmol). The reaction mixture was stirred at rt for 4 h after which the same amounts of triphosgene and 4-(4-methyl-piperazin-1-ylmethyl)-3-trifluoromethyl-phenylamine were added once more and stirring at rt was continued for 16 h. Extractive work-up followed by HPLC purification provided the pure target compound.

Provenance & Evidence