Trifluoroacetic acid → 3-(1-azetidin-3-ylmethyl-1H-pyrazol-4-yl)-6-(6-methyl-[1,2,4]triazolo[4,3-b]pyridazin-3-ylmethyl)-quinoline

Participants

Reaction Steps

To 3-{4-[6-(6-methyl-[1,2,4]triazolo[4,3-b]pyridazin-3-ylmethyl)-quinolin-3-yl]-pyrazol-1-ylmethyl}-azetidine-1-carboxylic acid tert-butyl ester (189 mg) was added 6 mL of TFA:dichloromethane/1:1 solution. The mixture was allowed to sit for 2 hours. The volatiles were removed by rotary evaporation and then Methanol (6 mL) and MP-carbonate (400 mg, 3.18 mmol/g) were added. The resin was filtered and the volatiles were removed in vacuo to obtain a quantitative yield of 3-(1-azetidin-3-ylmethyl-1H-pyrazol-4-yl)-6-(6-methyl-[1,2,4]triazolo[4,3-b]pyridazin-3-ylmethyl)-quinoline. Analytical data presented in Table 2.

Provenance & Evidence