3-(2-氯乙基)-2-甲基-9-羟基-6, 7,8,9-四氢-4H-吡啶[1,2-A]嘧啶-4-酮盐酸盐合成路线 （共 9 条）
反应条件
1: 6-fluoro-3-(4-piperidinyl)-1,2-benzisoxazole monohydrochloride With potassium carbonate; potassium iodide in acetonitrile T=30 - 60°C; 2: (±)-3-(2-chloroethyl)-6,7,8,9-tetrahydro-9-hydroxy-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one monohydrochloride in acetonitrile T=60°C; 47 h;
参考文献
CADILA PHARMACEUTICALS LTD.; MODI, Indravadan, Ambalal; SODAGAR, Keval, Rameshchandra; VINEET, Malik; JAIN, Sudhir, Hukamchand; PARIKH, Sanjay, Natvarlal; SHARMA, Arun, Omprakash; BAPAT, Uday, Rajaram; KHAMAR, Bakulesh, Mafatlal
Patent: WO2010/64134 A2, 2010 ;
Location in patent: Page/Page column 7 ;
反应条件
1: 4-(6-fluoro-1,2-benzisoxazol-3-yl)-piperidine With potassium carbonate; potassium iodide in acetonitrile T=30 - 60°C; 2: (±)-3-(2-chloroethyl)-6,7,8,9-tetrahydro-9-hydroxy-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one monohydrochloride in acetonitrile 47 h;
参考文献
CADILA PHARMACEUTICALS LTD.; SODAGAR, Keval, Rameshchandra; MALIK, Vineet; DESAI, Bharat, Ramchandra; JAIN, Sudhir, Hukamchand; PARIKH, Sanjay, Natvarlal; SHARMA, Arun, Omprakash; BAPAT, Uday, Rajaram; KHAMAR, Bakulesh, Mafatlal
Patent: WO2010/82111 A1, 2010 ;
Location in patent: Page/Page column 8-9 ;
反应条件
1: triethylamine / dichloromethane / 6 h / 0 - 20 °C 2: tetra-(n-butyl)ammonium iodide; diisopropylamine / methanol / 48 h / 45 °C View Scheme
参考文献
Xu, Weichu; Wright, George E.; Yanachkova, Milka; Yanachkov, Ivan B.
Letters in Organic Chemistry, 2014 , vol. 11, # 6 p. 470 - 473
反应条件
palladium 10 on activated carbon; hydrogen; carbon in methanol
T=50°C; P=112.511 Torr; Reagent/catalystSolventTime;
参考文献
De Smet, Koen; Van Dun, Jan; Stokbroekx, Bard; Spittaels, Tom; Schroyen, Christine; Van Broeck, Peter; Lambrechts, Julien; Van Cleuvenbergen, Dirk; Smout, Guy; Dubois, Jeroen; Horvath, Andras; Verbraeken, Jurgen; Cuypers, Jef
Organic Process Research and Development, 2005 , vol. 9, # 3 p. 344 - 347
反应条件
hydrogenchloride in water; butanone
pH=2;
参考文献
INKE, S.A.
Patent: WO2009/144288 A1, 2009 ;
Location in patent: Page/Page column 12-13 ;
反应条件
palladium 10 on activated carbon; hydrogen; zinc(II) chloride in methanol
T=50°C; P=112.511 Torr; 24 h; PressureTemperatureReagent/catalystTime;
参考文献
De Smet, Koen; Van Dun, Jan; Stokbroekx, Bard; Spittaels, Tom; Schroyen, Christine; Van Broeck, Peter; Lambrechts, Julien; Van Cleuvenbergen, Dirk; Smout, Guy; Dubois, Jeroen; Horvath, Andras; Verbraeken, Jurgen; Cuypers, Jef
Organic Process Research and Development, 2005 , vol. 9, # 3 p. 344 - 347
反应条件
hydrogenchloride; palladium 10 on activated carbon; hydrogen in methanol
参考文献
Xu, Weichu; Wright, George E.; Yanachkova, Milka; Yanachkov, Ivan B.
Letters in Organic Chemistry, 2014 , vol. 11, # 6 p. 470 - 473
反应条件
1: trichlorophosphate / toluene
2: hydrogen; palladium 10 on activated carbon; hydrogenchloride / methanol
View Scheme
参考文献
Xu, Weichu; Wright, George E.; Yanachkova, Milka; Yanachkov, Ivan B.
Letters in Organic Chemistry, 2014 , vol. 11, # 6 p. 470 - 473
反应条件
1: trichlorophosphate / toluene
2: hydrogen; palladium 10 on activated carbon; hydrogenchloride / methanol
View Scheme
参考文献
Xu, Weichu; Wright, George E.; Yanachkova, Milka; Yanachkov, Ivan B.
Letters in Organic Chemistry, 2014 , vol. 11, # 6 p. 470 - 473
