1: With 1H-imidazole in N,N-dimethyl-formamide
T=20°C;
2: With water; ammonium chloride in N,N-dimethyl-formamide
3: With hydrogenchloride in water; N,N-dimethyl-formamide
pH=~ 3;
参考文献
SCHERING CORPORATION
Patent: WO2009/143039 A2, 2009 ;
Location in patent: Page/Page column 124-125 ;
WO 2009/143039 A2
1.1: dichloromethane / 0.08 h / 22.2 °C / |Inert atmosphere
1.2: 0.08 h / |Inert atmosphere
1.3: 2.5 h / 25 °C / |Inert atmosphere
2.1: tetrahydrofuran; toluene / 0.5 h / 20 °C / |Inert atmosphere
2.2: -78 - -20 °C
View Scheme
参考文献
Magnus, Nicholas A.; Anzeveno, Peter B.; Coffey, D. Scott; Hay, David A.; Laurila, Michael E.; Schkeryantz, Jeffrey M.; Shaw, Bruce W.; Staszak, Michael A.
Organic Process Research and Development, 2007 , vol. 11, # 3 p. 560 - 567
1: 75 percent / 4-dimethylaminopyridin, triethylamin / CH2Cl2 / 23 h / Ambient temperature
2: 1.) sodium hydride 2.) HMPT / 1.) room temperature, THF 2.) room temperature for 16 h then 40 deg C for 2 h
View Scheme
参考文献
Schubert, Thomas; Kunisch, Franz; Welzel, Peter
Tetrahedron, 1983 , vol. 39, # 13 p. 2211 - 2217
Ha, Young Mi; Lee, Hye Jin; Park, Daeui; Jeong, Hyoung Oh; Park, Ji Young; Park, Yun Jung; Lee, Kyung Jin; Lee, Ji Yeon; Moon, Hyung Ryong; Chung, Hae Young
Biological and Pharmaceutical Bulletin, 2013 , vol. 36, # 1 p. 55 - 65
