Dimethylbarbituric acid → HCID 68312858, compound

Participants

Reaction Steps

To a solution of (R)-3-(1-allylazetidin-2-yl)piperidine-1-carboxylic acid benzyl ester (163 mg, 0.518 mmol) in DCM (10 mL) was added 1,3-dimethylbarbituric acid (243 mg, 1.56 mmol) and Pd(PPh3)4 (60 mg, 0.052 mmol). The mixture was stirred at RT for 64 h, then diluted with MeOH and loaded onto an Isolute® SCX-2 cartridge. The cartridge was washed with MeOH and the product eluted with 0.5M NH3/MeOH. Further purification by column chromatography (Si-PCC, gradient 3-15% 2M NH3/MeOH in DCM) afforded the title compound (126.5 mg, 89%) as a colourless oil. LCMS (Method B): RT1.99 & 2.07 min [M+H]+ 275.

Provenance & Evidence