1: 6-fluoro-3-(4-piperidinyl)-1,2-benzisoxazole monohydrochloride With potassium carbonate in acetonitrile T=25 - 60°C; 1.16667 h; 2: 3-(2-chloroethyl)-6,7,8,9-tetrahydro-2-methyl-9-hydroxy-4H-pyrido[1,2-a]pyrimidine-4-one palmitate ester With tetrabutylammomium bromide; potassium iodide T=20 - 75°C; 14 h;

1: With 4-(N,N-dimethlyamino)pyridine in toluene T=20 - 70°C; 3 h; 2: With tert-butyl methyl ether in toluene T=10°C; 1 h; Product distribution / selectivity;

4-(N,N-dimethlyamino)pyridine; pivaloyl chloride; triethylamine in tetrahydrofuran T=20°C; 24 h; Product distribution / selectivity;

1: 3-[2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]ethyl]-6,7,8,9-tetrahydro-9-hydroxy-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one With sodium hydride in N,N-dimethyl-formamide T=0°C; 2: n-hexadecanoyl chloride in N,N-dimethyl-formamide T=0°C; 5 h; Product distribution / selectivity;

in N,N-dimethyl-formamide T=20°C; 2 h;

1.1: 4-(N,N-dimethlyamino)pyridine; triethylamine / dichloromethane / 0.25 h / 25 - 30 °C 1.2: 2 h / 25 - 40 °C 2.1: potassium carbonate / acetonitrile / 1.17 h / 25 - 60 °C 2.2: 14 h / 20 - 75 °C View Scheme

1.1: 4-(N,N-dimethlyamino)pyridine; triethylamine / dichloromethane / 0.25 h / 25 - 30 °C 1.2: 2 h / 25 - 40 °C 2.1: potassium carbonate / acetonitrile / 1.17 h / 25 - 60 °C 2.2: 14 h / 20 - 75 °C View Scheme

1: With hydrogenchloride in water T=75 - 80°C; 2 h; 2: With sodium hydroxide in methanol; dichloromethane; water; isopropyl alcohol T=10 - 30°C; pH=10 - 12; 1 h; Reflux;

X-irradiation; Product distribution / selectivity;