1.1: 4-(N,N-dimethlyamino)pyridine; 4-methyl-morpholine; HATU / acetonitrile / 5.75 h / 20 - 50 °C 2.1: trifluoroacetic acid / dichloromethane / 0.75 h / 20 °C 3.1: sodium hydride / N,N-dimethyl-formamide / 1 h / 20 °C 3.2: 72 h 4.1: acetic acid / 4 h / 35 °C 4.2: 6 h / 60 °C View Scheme

Multi-step reaction with 4 steps 1: N-iodo-succinimide / acetonitrile / 0.83 h / 0 °C2: tris-(dibenzylideneacetone)dipalladium(0) / isobutyramide / 6 h / 60 °C / Inert atmosphere3: caesium carbonate / N,N-dimethyl-formamide / 1 h / 60 °C4: sodium hydroxide; water / ethanol / 3 h / 60 °C  

Multi-step reaction with 2 steps 1: caesium carbonate / N,N-dimethyl-formamide / 1 h / 60 °C2: sodium hydroxide; water / ethanol / 3 h / 60 °C