Morpholine → N-(8-morpholino-2,3-dihydrobenzo[b][1,4]dioxin-5-yl)acetamide

Participants

Reaction Conditions

Reaction Steps

To a solution of N-(8-bromo-2,3-dihydrobenzo[b][1,4]dioxin-5-yl)acetamide (5 g, 18.4 mmol) in toluene (50 mL) was added morpholine (1.9 g, 22 mmol), Pd2(dba)3 (1.68 g, 1.84 mmol), X-Phos (1.75 g, 3.68 mmol) and potassium tert-butoxide (4.1 g, 36.8 mmol) in a sealed tube. The mixture was heated at 130° C. for overnight. After cooled to room temperature, the mixture was filtered and the filtrate was evaporated to give a crude product, which was purified by silica gel column chromatography (petroleum ether/ethyl acetate 4/1) to afford the product N-(8-morpholino-2,3-dihydrobenzo[b][1,4]dioxin-5-yl)acetamide (2 g, yield 40%).

Provenance & Evidence