1: With 4-(N,N-dimethlyamino)pyridine; dicyclohexyl-carbodiimide in dichloromethane T=0 - 20°C; 2 h; 2: With toluene-4-sulfonic acid in ethanol Heating / reflux;
参考文献
BAYER AKTIENGESELLSCHAFT
Patent: WO2003/106450 A1, 2003 ;
Location in patent: Page column 39,40 ;
WO 03/106450 A1
1: malonic acid ethyl ester monopotassium salt With magnesium chloride in tetrahydrofuran T=50°C; 2: isonicotinic acid With 1,1'-carbonyldiimidazole in tetrahydrofuran 18 h;
参考文献
Alam, Muzaffar; Du Bois, Daisy Joe; Hawley, Ronald Charles; Kennedy-Smith, Joshua; Minatti, Ana Elena; Palmer, Wylie Solang; Silva, Tania; Wilhelm, Robert Stephen
Patent: US2011/71150 A1, 2011 ;
Location in patent: Page/Page column 27 ;
1: malonic acid ethyl ester monopotassium salt With triethylamine; magnesium chloride in acetonitrile 2 h; Cooling with ice-salt bath; 2: 4-pyridinecarboxylic acid 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
GLAXO GROUP LIMITED; JOHNS, Brian Alvin; SHOTWELL, John Brad
Patent: WO2012/67664 A1, 2012 ;
Location in patent: Page/Page column 31 ;