Triethyloxonium tetrafluoroborate → 2-(7-{[2-Chloro-3-(trifluoromethyl)phenyl]carbonyl}-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyrazin-3-yl)-3-pyridinol

関与物質

反応手順

Triethyloxonium tetrafluoroborate (204 mg, 1.076 mmol) was added to a solution of the 4-{[2-chloro-3-(trifluoromethyl)phenyl]carbonyl}-2-piperazinone (I1)(300 mg, 0.978 mmol) in Dichloromethane (DCM) (6 mL) and the reaction was stirred for 1 h. To this was added the 3-hydroxy-2-pyridinecarbohydrazide (I93) (180 mg, 1.174 mmol) and the reaction was stirred for 2 hrs. The solvent was evaporated and 1-butanol (6.00 mL) was added. The mixture was heated at reflux for 3 h. After cooling the solvent was evaporated and the residue was partitioned between water/EtOAc. The organic layer was passed through a phase sep. cartridge and the solvent evaporated to afford an amber oil. This was purified by MDAP to afford a colourless solid of desired material in 90 mg.

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