4-羟基-4-(3-羟基丙基)-1-哌啶羧酸 1,1-二甲基乙酯合成路线 (共 7 条)
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
反应条件
hydrogen; palladium on activated charcoal in ethanol; water; acetic acid
P=2068.65 Torr; 20 h;
参考文献
MERCK SHARP and DOHME LIMITED
Patent: WO2004/78750 A1, 2004 ;
Location in patent: Page 77-78 ;
WO 2004/078750 A1
反应条件
tetrabutyl ammonium fluoride
参考文献
Astellas Pharma Inc.
Patent: WO2009/131246 A1, 2009 ;
Location in patent: Page/Page column 87 ;
反应条件
diisobutylaluminium hydride in dichloromethane
T=-78 - 0°C; 5 h;
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: n-BuLi / tetrahydrofuran / -78 °C
1.2: tetrahydrofuran / 1 h / -78 °C
2.1: H2 / Pd/C / ethanol
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: H2 / Pd/C / ethanol
2: p-TsOH / toluene / 3 h / Heating
3: 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