3-Aminoazetidine, 3-BOC protected → tert-Butyl (1-(5-(thiophen-2-yl)-[1,2,4]triazolo[4,3-a]pyrazin-8-yl)azetidin-3-yl)carbamate

Participants

Reaction Steps

A 50 mL round bottom flask was charged with 8-chloro-5-(thiophen-2-yl)-[1,2,4]triazolo[4,3-a]pyrazine (0.25 g, 1.1 mmol), tert-butyl azetidin-3-ylcarbamate (540 mg, 3.1 mmol) and ethanol (5 mL). The resulting solution was refluxed overnight. Work-up: the solvent was evaporated. The residue was purified by flash column chromatography on silica gel with a 1:2 EtOAc/petroleum ether and then a 1:50 methanol/dichloromethane, to afford 130 mg (33%) of the product as a white solid. MS m/z: 373 (M+H+).

Provenance & Evidence