4-(2-羟基乙基)-4-(羟基甲基)-1-哌啶羧酸 1,1-二甲基乙酯合成路线 （共 10 条）
反应条件
1: With diisobutylaluminium hydride in dichloromethane T=-78 - 0°C; 5 h; 2: With water in dichloromethane T=0 - 20°C;
参考文献
Castro Pineiro, Jose Luis; Dinnell, Kevin; Elliott, Jason Matthew; Hollingworth, Gregory John; Shaw, Duncan Edward; Swain, Christopher John
Patent: US2003/236250 A1, 2003 ;
Location in patent: Page 30 ;
反应条件
1: With sodium tetrahydroborate in ethanol T=0 - 20°C; Heating / reflux; 2: With hydrogenchloride in ethanol; water pH=5 - 6;
参考文献
ASTRAZENECA AB
Patent: WO2007/30061 A1, 2007 ;
Location in patent: Page/Page column 86; 87 ;
WO 2007/030061 A1
反应条件
sodium borohydride in methanol; acetone
参考文献
Banyu Pharmaceutical Co Ltd
Patent: US6140333 A1, 2000 ;
US 6140333 A
反应条件
1.1: KHMDS / tetrahydrofuran / -78 °C 1.2: tetrahydrofuran / 1 h / -78 °C 2.1: O3 / methanol; CH2Cl2 / -78 °C 2.2: NaBH4 / 3 h / -78 - 20 °C 3.1: p-TsOH / toluene / 3 h / Heating 4.1: DIBAL-H / CH2Cl2 / 5 h / -78 - 0 °C View Scheme
参考文献
Cooper, Laura C.; Carlson, Emma J.; Castro, Jose L.; Chicchi, Gary G.; Dinnell, Kevin; Di Salvo, Jerry; Elliott, Jason M.; Hollingworth, Gregory J.; Kurtz, Marc M.; Ridgill, Mark P.; Rycroft, Wayne; Tsao, Kwei-Lan; Swain, Christopher J.
Bioorganic and Medicinal Chemistry Letters, 2002 , vol. 12, # 13 p. 1759 - 1762
反应条件
1.1: O3 / methanol; CH2Cl2 / -78 °C 1.2: NaBH4 / 3 h / -78 - 20 °C 2.1: p-TsOH / toluene / 3 h / Heating 3.1: DIBAL-H / CH2Cl2 / 5 h / -78 - 0 °C View Scheme
参考文献
Cooper, Laura C.; Carlson, Emma J.; Castro, Jose L.; Chicchi, Gary G.; Dinnell, Kevin; Di Salvo, Jerry; Elliott, Jason M.; Hollingworth, Gregory J.; Kurtz, Marc M.; Ridgill, Mark P.; Rycroft, Wayne; Tsao, Kwei-Lan; Swain, Christopher J.
Bioorganic and Medicinal Chemistry Letters, 2002 , vol. 12, # 13 p. 1759 - 1762
反应条件
1: p-TsOH / toluene / 3 h / Heating 2: DIBAL-H / CH2Cl2 / 5 h / -78 - 0 °C View Scheme
参考文献
Cooper, Laura C.; Carlson, Emma J.; Castro, Jose L.; Chicchi, Gary G.; Dinnell, Kevin; Di Salvo, Jerry; Elliott, Jason M.; Hollingworth, Gregory J.; Kurtz, Marc M.; Ridgill, Mark P.; Rycroft, Wayne; Tsao, Kwei-Lan; Swain, Christopher J.
Bioorganic and Medicinal Chemistry Letters, 2002 , vol. 12, # 13 p. 1759 - 1762
反应条件
1: PPh3; diethyl azodicarboxylate / tetrahydrofuran / 16 h / 0 - 20 °C 2: AcCl; MeOH / 16 h / 0 - 20 °C View Scheme
参考文献
Cooper, Laura C.; Carlson, Emma J.; Castro, Jose L.; Chicchi, Gary G.; Dinnell, Kevin; Di Salvo, Jerry; Elliott, Jason M.; Hollingworth, Gregory J.; Kurtz, Marc M.; Ridgill, Mark P.; Rycroft, Wayne; Tsao, Kwei-Lan; Swain, Christopher J.
Bioorganic and Medicinal Chemistry Letters, 2002 , vol. 12, # 13 p. 1759 - 1762
参考文献
Banyu Pharmaceutical Co Ltd
Patent: US6140333 A1, 2000 ;
US 6140333 A
反应条件
triphenylphosphine; diethylazodicarboxylate in tetrahydrofuran
T=0 - 20°C;
参考文献
Castro Pineiro, Jose Luis; Dinnell, Kevin; Elliott, Jason Matthew; Hollingworth, Gregory John; Shaw, Duncan Edward; Swain, Christopher John
Patent: US2003/236250 A1, 2003 ;
Location in patent: Page 30 ;
反应条件
triethylamine in dichloromethane
T=0°C; 2 h;
参考文献
ASTRAZENECA AB
Patent: WO2007/30061 A1, 2007 ;
Location in patent: Page/Page column 86; 87 ;
WO 2007/030061 A1
