4-羟基-3,4,5,6-四氢-2H-[2,4]联吡啶-1-羧酸叔丁酯合成路线 （共 8 条）
反应条件
trifluoroacetic acid in dichloromethane
参考文献
Abreo, Melwyn A.; Meng, Jerry J.; Agree, Charles S.
Patent: US2002/65292 A1, 2002 ;
反应条件
n-butyllithium
1.) Et2O, hexane, -50 deg C, 10 min, 2.) Et2O, hexane, -30 deg C, 1 h; Multistep reaction;
参考文献
Saari, Walfred S.; Halczenko, Wasyl; Huff, Joel R.; Guare, James P.; Hunt, Cecilia A.; et al.
Journal of Medicinal Chemistry, 1984 , vol. 27, # 9 p. 1182 - 1185
反应条件
triethylamine in dichloromethane
0.5 h;
参考文献
MERCK SHARP and DOHME CORP.; KUDUK, Scott, D.; BESHORE, Douglas, C.; DIMARCO, Christina, Ng; GRESHOCK, Thomas, J.
Patent: WO2011/84371 A1, 2011 ;
Location in patent: Page/Page column 50-51 ;
WO 2011/084371 A1
反应条件
1: 63 percent / Et3N / dimethylformamide / 18 h / Ambient temperature
2: 1.) n-BuLi / 1.) Et2O, hexane, -50 deg C, 10 min, 2.) Et2O, hexane, -30 deg C, 1 h
View Scheme
参考文献
Saari, Walfred S.; Halczenko, Wasyl; Huff, Joel R.; Guare, James P.; Hunt, Cecilia A.; et al.
Journal of Medicinal Chemistry, 1984 , vol. 27, # 9 p. 1182 - 1185
反应条件
1: 63 percent / Et3N / dimethylformamide / 18 h / Ambient temperature
2: 1.) n-BuLi / 1.) Et2O, hexane, -50 deg C, 10 min, 2.) Et2O, hexane, -30 deg C, 1 h
View Scheme
参考文献
Saari, Walfred S.; Halczenko, Wasyl; Huff, Joel R.; Guare, James P.; Hunt, Cecilia A.; et al.
Journal of Medicinal Chemistry, 1984 , vol. 27, # 9 p. 1182 - 1185
反应条件
[bis(2-methoxyethyl)amino]-sulfur trifluoride in dichloromethane
T=-78 - 20°C; 1 h;
参考文献
MERCK SHARP and DOHME CORP.; KUDUK, Scott, D.; BESHORE, Douglas, C.; DIMARCO, Christina, Ng; GRESHOCK, Thomas, J.
Patent: WO2011/84371 A1, 2011 ;
Location in patent: Page/Page column 51 ;
WO 2011/084371 A1
反应条件
pyridine; trichlorophosphate
参考文献
Kamei, Katsuhide; Maeda, Noriko; Nomura, Kayoko; Shibata, Makoto; Katsuragi-Ogino, Ryoko; Koyama, Makoto; Nakajima, Mika; Inoue, Teruyoshi; Ohno, Tomochika; Tatsuoka, Toshio
Bioorganic and Medicinal Chemistry, 2006 , vol. 14, # 6 p. 1978 - 1992
反应条件
1: 45 percent / methyl ester of (carboxysulfamoyl)triethylammonium hydroxide inner salt / benzene / 0.75 h / 50 °C
2: 92 percent / TFA / CH2Cl2 / 0.08 h / 0 °C
View Scheme
参考文献
Saari, Walfred S.; Halczenko, Wasyl; Huff, Joel R.; Guare, James P.; Hunt, Cecilia A.; et al.
Journal of Medicinal Chemistry, 1984 , vol. 27, # 9 p. 1182 - 1185
