Ethyl oxoacetate → HCID 86728306, compound

Participants

Reaction Conditions

Reaction Steps

A mixture of 5-(11-fluoro-6H-pyrido[2′,3′:5,6][1,3]oxazino[3,4-a]indol-2-yl)-2-(4-fluorophenyl)-N-methyl-6-(N-methylmethylsulfonamido)benzofuran-3-carboxamide (500 mg, 0.814 mmol) and ethyl glyoxalate (323 μl, 1.627 mmol) was heated at 115° C. for 3 hours in a sealed tube. The reaction mixture was cooled to room temperature, concentrated under vacuum then applied onto 2-EP column (30 mm×250 mm) eluted with 30% IPA/CO2. This resulted in 108 mg (18.5%) of ethyl 2-(11-fluoro-2-(2-(4-fluorophenyl)-3-(methylcarbamoyl)-6-(N-methylmethylsulfonamido)benzofuran-5-yl)-6H-pyrido[2′,3′:5,6][1,3]oxazino[3,4-a]indol-12-yl)-2-hydroxyacetate (Compound 206) as a white solid. LC-MS (ES, m/z) C36H30F2N4O8S: 716. Found: 717 [M+H]+.

Provenance & Evidence