2-Morpholinoethylamine → Methyl 2-(2-morpholinoethylamino)-3-fluorobenzoate

Participants

Reaction Conditions

Reaction Steps

Methyl 2,3-difluorobenzoate (817 mg, 4.746 mmol) and 2-morpholinoethanamine (2.5 mL, 19.20 mmol) were dissolved in DMF (15 mL) and heated in a microwave for 30 mins at 100° C. The crude material was purified by silica gel column chromatography with EtOAc/Hexanes to yield 943 mg (70%) of desired methyl 2-(2-morpholinoethylamino)-3-fluorobenzoate. LC/MS: 283.15 (M+1) Rt=1.48 min (10-90% 3/5 min (grad/run) with formic acid).

Provenance & Evidence