Water → HCID 57713871, compound

Participants

Reaction Conditions

Reaction Steps

A solution of methanesulfonyl chloride (0.63 ml, 7.6 mmol) in dichloromethane (10 ml) is added dropwise to a solution of 1-(6-azepan-1-yl-2-cyclopropyl-5-methyl-pyrimidin-4-yl)-azetidin-3-ol 189 (1.90 g, 6.3 mmol) and triethylamine (1.74 ml, 13 mmol) in dichloromethane (90 ml) at 0° C. The mixture is stirred 1 hour at 0° C. and 1 hour at room temperature. Water (40 ml) is added and the mixture is extracted three times with dichloromethane. The combined organic layers are dried over magnesium sulfate and concentrated in vacuo to afford pure methanesulfonic acid 1-(6-azepan-1-yl-2-cyclopropyl-5-methyl-pyrimidin-4-yl)-azetidin-3-yl ester 190 (2.66 g, 100%).

Provenance & Evidence