Morpholine → HCID 68313268, compound

Participants

Reaction Conditions

Reaction Steps

A mixture of 1-(1-{4-[1-(propan-2-yl)-1H-1,2,4-triazol-5-yl]-9-oxa-3,6-diazatricyclo[8.4.0.02,6]tetradeca1(14),2,4,10,12-pentaen-13-yl}ethyl)azetidin-3-yl methanesulfonate (70 mg, 0.15 mmol) and morpholine (20 mg, 1.5 mmol) in 1,4-dioxane (4 mL) was stirred at 80° C. for 16 h under nitrogen atmosphere. After concentration, the residue was purified by reverse phase Combiflash eluting with a 0-50% gradient of CH3CN in 0.3% NH4HCO3 to give 163. The enantiomers were separated by chiral HPLC (OD column, 10% EtOH (0.1% DEA) in n-hexane isocratic) to give: 24 mg of one enantiomer and 25 mg of the other (71% total yield)

Provenance & Evidence