3-(6-Chloro-[1,2,4]triazolo[3,4-a]phthalazin-3-yl)-5-methylisoxazole → 6-[5-{1-(Azetidin-1-yl)ethyl}pyridin-2-ylmethyloxyl]-3-(5-methyl isoxazol-3-yl)-[1,2,4]triazolo[3,4-alpha]phthalazine

Participants

Reaction Steps

The reaction was carried out as described in Example 1, Step 4 using 6-chloro-3-(5-methylisoxazol-3-yl)-[1,2,4]triazolo[3,4-α]phthalazine (100 mg, 0.35 mmol) and [5-{1-(azetidin-1-yl)ethyl}pyridin-2-yl]methanol (67 mg, 0.35 mmol) to give, after column chromatography on silica, eluting with 2.5% MeOH/CH2Cl2 containing 1% NH3 solution, the amine (121 mg, 79%) which was recrystallised from CH2Cl2/hexane.

Provenance & Evidence