Cyclopropanecarbonyl chloride → methyl 2-(2-{(cyclopropylcarbonyl)[3-(1H-pyrazol-1-yl)phenyl]amino}ethyl)-1-oxo-1,2-dihydroisoquinoline-7-carboxylate

Participants

Reaction Steps

To a solution of methyl 1-oxo-2-(2-{[3-(1H-pyrazol-1-yl)phenyl]amino}ethyl)-1,2-dihydroisoquinoline-7-carboxylate (77 mg, 0.20 mmol) dissolved in methylene chloride (1.5 mL) was added N,N-diisopropylethylamine (69 μL, 0.4 mmol) and cyclopropanecarbonyl chloride (27 μL, 0.30 mmol). The reaction mixture was stirred at rt for 1 h. The mixture was then concentrated to dryness and the residue was purified by flash silica gel chromatography (30% to 100% EtOAc/hexanes) to afford methyl 2-(2-{(cyclopropylcarbonyl)[3-(1H-pyrazol-1-yl)phenyl]amino}ethyl)-1-oxo-1,2-dihydroisoquinoline-7-carboxylate (77 mg, 85%). LC-MS: (FA) ES+ 457.

Provenance & Evidence