Dichloromethane → HCID 86728246, compound

Participants

Reaction Conditions

Reaction Steps

To a solution of 2-chloro-6H-pyrido[2′,3′:5,6][1,3]oxazino[3,4-a]indole-11-carbaldehyde (31 mg, 0.11 mmol), 2-(4-fluorophenyl)-N-methyl-6-(N-methylmethylsulfonamido)-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzofuran-3-carboxamide (50 mg, 0.10 mmol) and K3PO4.3H2O (53 mg, 0.19 mmol) in 1,4-dioxane (1 mL) and water (0.2 mL) was added X-Phos (5 mg) and Pd2(dba)3 (5 mg) under nitrogen. The mixture was heated at 100° C. for 16 hours, and then filtered through the celite pad. The filtrate was extracted with EtOAc, then the combined organic phase was washed with brine, dried over Na2SO4 and concentrated in vacuo to provide the 2-(4-fluorophenyl)-5-(11-formyl-6H-pyrido[2′,3′:5,6][1,3]oxazino[3,4-a]indol-2-yl)-N-methyl-6-(N-methylmethylsulfonamido)benzofuran-3-carboxamide (50 mg, yield: 80%) by the prep-TLC (dichloromethane:MeOH=30:1). MS (M+H)+: 625.

Provenance & Evidence