1: With palladium diacetate; potassium carbonate; 2-(dicyclohexylphosphino)-2',4',6'-tri-i-propyl-1,1’-biphenyl in N,N-dimethyl acetamide T=80°C; 2 h; Inert atmosphere; 2: With toluene-4-sulfonic acid in dichloromethane T=20°C; 2 h; Inert atmosphere;

sulfuric acid in ethanol 3 h; Heating;

1,4-dioxane; hydrogenchloride; water T=70°C; Inert atmosphere;

1: 52 percent / Cs2CO3; CuI; N,N-dimethylglycine hydrochloride / dioxane / 70 - 80 °C 2: 70 percent / n-Bu4NHSO4; NaHCO3; 4 Angstrom molecular sieves / Pd(OAc)2 / dimethylformamide / 100 °C View Scheme

1: 52 percent / Cs2CO3; CuI; N,N-dimethylglycine hydrochloride / dioxane / 70 - 80 °C 2: 70 percent / n-Bu4NHSO4; NaHCO3; 4 Angstrom molecular sieves / Pd(OAc)2 / dimethylformamide / 100 °C View Scheme