Cesium carbonate → HCID 11563567, compound

Participants

Reaction Conditions

Reaction Steps

8.99 g 7-bromo-1-methyl-1H-indole-2-carboxylic acid-(5-tert-butyl-3-methanesulphonylamino-2-methoxy-phenyl)-amide and 5.95 g potassium ((4-(tert.-butoxycarbonyl)-piperazin-1-yl)-methyl)-trifluoroborate (for preparation see Org. Lett. 2007, 9, 1597-1600) are dissolved in 150 ml of tetrahydrofuran and 15 ml of water, combined with 17.3 g caesium carbonate and argon is piped through the resulting solution for 10 minutes. Then 120 mg palladium-II-acetate and 1.23 g 2-dicyclohexylphosphino-2′,4′,6′-triisopropyl-1,1′-biphenyl (XPhos) are added and the mixture is heated to 80° C. for 12 hours. Then it is divided between water and ethyl acetate and the organic phase is washed with saturated aqueous sodium chloride solution. After drying with magnesium sulphate the solvents are eliminated in vacuo. The crude product is further reacted directly.

Provenance & Evidence