Ethyl orthoformate → Tert-butyl 4-(5-bromo-[1,2,4]triazolo[4,3-a]pyrazin-8-yl)piperazine-1-carboxylate

Participants

Reaction Conditions

Reaction Steps

A 50 mL round bottom flask was charged with tert-butyl 4-(5-bromo-3-hydrazinylpyrazin-2-yl)piperazine-1-carboxylate (5.8 g, 20 mmol) and triethyl orthoformate (60 mL). The resulting solution was heated at 130° C. for 3 h. TLC indicated a complete conversion. The solvent was evaporated and the residue was purified by flash column chromatography on silica gel with 2% methanol in dichloromethane, to afford 5.3 g (69%) of the product as a yellow solid. MS m/z: 383 (M+H+).

Provenance & Evidence