Dimethylformamide → HCID 44430466, compound

Participants

Reaction Conditions

Reaction Steps

A mixture of methanesulfonic acid 1-(6-azepan-1-yl-2-cyclopropyl-5-methyl-pyrimidin-4-yl)-azetidin-3-yl ester 190 (0.3 g, 0.8 mmol) and sodium cyanide (0.047 g, 1.0 mmol) in N,N-dimethylformamide (5 ml) is heated at 120° C. for 24 hours. The mixture is then cooled and concentrated in vacuo. The mixture is diluted with dichloromethane and washed two times with water. The combined organic layers are dried over magnesium sulfate and concentrated in vacuo to afford 0.4 g of a crude mixture, which is purified by column chromatography (dichloromethane/ethanol 98/2). 0.10 g (60%) of 1-(6-azepan-1-yl-2-cyclopropyl-5-methyl-pyrimidin-4-yl]-azetidine-3-carbonitrile 183 is obtained.

Provenance & Evidence