3-氧代-3-(3-吡啶基)丙酸乙酯合成路线 (共 29 条)
反应条件
1: [3H]-Nicotinic acid With carbonyl diimidazole in tetrahydrofuran T=5 - 20°C; 1 h; 2: malonic acid ethyl ester monopotassium salt With magnesium chloride in tetrahydrofuran T=20°C; 12 h; Mixture stirred previously for 4 h at 50 C;
参考文献
Bayer Healthcare AG
Patent: WO2004/29055 A1, 2004 ;
Location in patent: Page 52-53 ;
WO 2004/029055 A1
反应条件
lithium hexamethyldisilazane in tetrahydrofuran T=-40°C; Claisen condensation; 0.333333 h; Inert atmosphere;
参考文献
Venkat Ragavan; Vijayakumar; Rajesh; Palakshi Reddy; Karthikeyan; Suchetha Kumari
Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 12 p. 4193 - 4197
反应条件
1,1'-carbonyldiimidazole; magnesium chloride in tetrahydrofuran T=20°C; 16 h;
参考文献
Hoffmann-La Roche Inc.; Bhagirath, Niala; Brameld, Kenneth Albert; Kennedy-Smith, Joshua
Patent: US2013/90333 A1, 2013 ;
Location in patent: Paragraph 0130 ;
反应条件
sodium ethanolate 16 h; Heating / reflux;
参考文献
Li, Francine Feirong; Rehder, Kenneth S.; Campbell, Michael Gordon; Viscardi, Celeste Patrice; Strachan, Jon-Paul; Guo, Zhengming
Patent: US2004/116425 A1, 2004 ;
Location in patent: Page 86 ;
反应条件
1: malonic acid ethyl ester monopotassium salt With triethylamine; magnesium chloride in acetonitrile 2 h; Cooling with ice-salt bath; 2: 3-pyridinecarbonyl chloride in acetonitrile T=20°C; Cooling with ice-salt bath; 3: With hydrogenchloride in water; acetonitrile 1.5 h; Cooling with ice;
参考文献
WO2012/67664 A1, ;
Page/Page column 28-29 ;
反应条件
dichloro(cycloocta-1,5-diene)palladium(II); N,N-dicyclohexylmethylamine; triethylamine; 9,9-dimethyl-4,5-bis(diphenyl-phosphino)xanthene; magnesium chloride; [(t-Bu)3PH]BF4 in 1,4-dioxane T=80°C; 18 h; Inert atmosphereGlovebox;
参考文献
Korsager, Signe; Nielsen, Dennis U.; Taaning, Rolf H.; Skrydstrup, Troels
Angewandte Chemie - International Edition, 2013 , vol. 52, # 37 p. 9763 - 9766
Angew. Chem., 2013 , vol. 125, # 37 p. 9945 - 9948
反应条件
1: concentrated H2SO4 2: sodium ethylate; benzene View Scheme
参考文献
Journal of the American Chemical Society, , vol. 70, p. 2755,2757
参考文献
Pharmaceutical Bulletin, , vol. 3, p. 32
参考文献
Journal of the American Chemical Society, , vol. 49, p. 557