Morpholine → HCID 86689191, compound

Participants

Reaction Conditions

Reaction Steps

A mixture of ethyl 3-{[(5-bromo-3-methyl-1-benzothiophen-2-yl)sulfonyl]amino}benzoate (Intermediate 18) (23 mg, 0.05 mmol), morpholine (9 mg, 0.10 mmol), PdOAc2 (0.6 mg, 0.0025 mmol), 2-(di-tbutylphosphino)biphenyl (1 mg, 0.0035 mmol) and Cs2CO3 (66 mg, 0.25 mmol) in dioxane (200 μL) was heated at 110° C. for 20 h giving the intermediate ethyl 3-{[(3-methyl-5-morpholin-4-yl-1-benzothiophen-2-yl)sulfonyl]amino}benzoate. The intermediate ester was hydrolyzed using LiOH in aqueous THF (1 mL, 1:1 water/THF) giving the title compound. MS (ESI+) calcd mass for C20H20N2O5S2 432.081363, found 432.081153.

Provenance & Evidence