2-氰基-5-羟基甲基吡啶合成路线 （共 9 条）
参考文献
Nihon Tokushu Noyaku Seizo K.K.
Patent: US4772620 A1, 1988 ;
反应条件
1: With oxalyl dichloride; dimethyl sulfoxide in dichloromethane T=-78°C; 0.333333 h; 2: 5-(hydroxymethyl)pyridine-2-carbonitrile in dichloromethane T=-78°C; 2 h; 3: With triethylamine in dichloromethane T=20°C;
参考文献
BAYER HEALTHCARE AG
Patent: WO2005/82863 A2, 2005 ;
Location in patent: Page/Page column 29-30 ;
WO 2005/082863 A2
反应条件
1: oxalyl dichloride With dimethyl sulfoxide in dichloromethane T=-78°C; 0.333333 h; 2: 5-(hydroxymethyl)pyridine-2-carbonitrile in dichloromethane T=-78°C; 2 h; 3: With triethylamine in dichloromethane
参考文献
BAYER HEALTHCARE AG
Patent: WO2004/20410 A2, 2004 ;
Location in patent: Page 82 ;
WO 2004/020410 A2
反应条件
1: With N-bromosuccinmide; dibenzoyl peroxide in tetrachloromethane
3 h; Heating / reflux;
2: With calcium carbonate in 1,4-dioxane; water
2 h; Heating / reflux;
参考文献
BAYER HEALTHCARE AG
Patent: WO2005/82863 A2, 2005 ;
Location in patent: Page/Page column 29 ;
WO 2005/082863 A2
反应条件
1: With chloroformic acid ethyl ester; triethylamine in tetrahydrofuran
T=0°C; 0.25 h;
2: With sodium tetrahydroborate in tetrahydrofuran
T=0 - 20°C;
参考文献
ASTRAZENECA AB
Patent: WO2003/101956 A1, 2003 ;
Location in patent: Page 114 ;
WO 03/101956 A1
反应条件
1: With chloroformic acid ethyl ester; triethylamine in tetrahydrofuran
T=0°C; 0.25 h;
2: With sodium tetrahydroborate in tetrahydrofuran
T=20°C;
3: With water in tetrahydrofuran
参考文献
Inghardt, Tord; Johansson, Anders; Svensson, Arne
Patent: US2004/19033 A1, 2004 ;
Location in patent: Page/Page column 41 ;
反应条件
methanol; sodium tetrahydroborate in tetrahydrofuran
T=20°C; Cooling with ice;
参考文献
Mitsubishi Tanabe Pharma Corporation
Patent: EP2154135 A1, 2010 ;
Location in patent: Page/Page column 20; 21 ;
反应条件
potassium carbonate in methanol
2.5 h;
参考文献
Ashimori; Ono; Uchida; Ohtaki; Fukaya; Watanabe; Yokoyama
Chemical and Pharmaceutical Bulletin, 1990 , vol. 38, # 9 p. 2446 - 2458
反应条件
1: benzoyl chloride / H2O; CHCl3 / 7 h / 4 °C
2: 53 percent / K2CO3 / methanol / 2.5 h
View Scheme
参考文献
Ashimori; Ono; Uchida; Ohtaki; Fukaya; Watanabe; Yokoyama
Chemical and Pharmaceutical Bulletin, 1990 , vol. 38, # 9 p. 2446 - 2458
