1,2,3,6-四氢-4-苯基吡啶盐酸盐合成路线 （共 15 条）
反应条件
1.1: iodine; magnesium / tetrahydrofuran / Inert atmosphere; Reflux 1.2: 3 h / 20 °C / Inert atmosphere; Cooling with ice 2.1: methanesulfonic acid / toluene / 4 h / Reflux 3.1: 1,2-dichloro-ethane / Cooling with ice; Reflux 4.1: methanol / 2.5 h / Reflux View Scheme
参考文献
Conway, Richard J.; Valant, Celine; Christopoulos, Arthur; Robertson, Alan D.; Capuano, Ben; Crosby, Ian T.
Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 7 p. 2560 - 2564
反应条件
1.1: iodine; magnesium / tetrahydrofuran / Inert atmosphere; Reflux 1.2: 3 h / 20 °C / Inert atmosphere; Cooling with ice 2.1: methanesulfonic acid / toluene / 4 h / Reflux 3.1: 1,2-dichloro-ethane / Cooling with ice; Reflux 4.1: methanol / 2.5 h / Reflux View Scheme
参考文献
Conway, Richard J.; Valant, Celine; Christopoulos, Arthur; Robertson, Alan D.; Capuano, Ben; Crosby, Ian T.
Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 7 p. 2560 - 2564
反应条件
1: 1,2-dichloro-ethane / Cooling with ice; Reflux 2: methanol / 2.5 h / Reflux View Scheme
参考文献
Conway, Richard J.; Valant, Celine; Christopoulos, Arthur; Robertson, Alan D.; Capuano, Ben; Crosby, Ian T.
Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 7 p. 2560 - 2564
反应条件
1: methanesulfonic acid / toluene / 4 h / Reflux 2: 1,2-dichloro-ethane / Cooling with ice; Reflux 3: methanol / 2.5 h / Reflux View Scheme
参考文献
Conway, Richard J.; Valant, Celine; Christopoulos, Arthur; Robertson, Alan D.; Capuano, Ben; Crosby, Ian T.
Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 7 p. 2560 - 2564
反应条件
1: 1.) N,N'-carbonyldiimidazole / 1.) THF, RT, 1 h, 2.) THF, RT, overnight 2: dihydrobis(methoxyethanato-O,O')aluminate sodium / tetrahydrofuran / 2 h / Ambient temperature 3: diisobutylaluminium hydride (DIBAH) / toluene / 1.5 h / Heating View Scheme
参考文献
Bottcher; Barnickel; Hausberg; Haase; Seyfried; Eiermann
Journal of Medicinal Chemistry, 1992 , vol. 35, # 22 p. 4020 - 4026
参考文献
Welstead Jr.; Helsley; Taylor; Turnbull; DaVanzo; Funderburk; Alphin
Journal of Medicinal Chemistry, 1973 , vol. 16, # 10 p. 1129 - 1132
反应条件
sodium hydrogencarbonate in Sec-butyl alcohol Heating;
参考文献
Welstead Jr.; Helsley; Taylor; Turnbull; DaVanzo; Funderburk; Alphin
Journal of Medicinal Chemistry, 1973 , vol. 16, # 10 p. 1129 - 1132
反应条件
potassium carbonate in N-methyl-acetamide; water
参考文献
Hoffmann-La Roche Inc.
Patent: US5688798 A1, 1997 ;
反应条件
1: With hydrogen; palladium 10 on activated carbon in ethanol; water 2: With sodium hydroxide in diethyl ether T=0°C;
参考文献
MERCK and CO., INC.
Patent: WO2003/101381 A2, 2003 ;
Location in patent: Page 74 ;
WO 03/101381 A2
反应条件
sodium hydroxide in water
参考文献
WO2004/113275 A2, ;
Page 171 ;
