1,1-环丙基二甲酸单甲酯合成路线 （共 8 条）
反应条件
sodium hydroxide in methanol
参考文献
Charton, Yves; Guillonneau, Claude; Lockhart, Brian; Lestage, Pierre; Goldstein, Solo
Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 6 p. 2188 - 2193
反应条件
potassium hydroxide T=0 - 20°C; 2 h;
参考文献
ARDELYX, INC.; LEWIS, Jason, G.; REICH, Nicholas; CHEN, Tao; JACOBS, Jeffrey W.; CHARMOT, Dominique; NAVRE, Marc; FINN, Patricia; CARRERAS, Christopher; SPENCER, Andrew
Patent: WO2013/96771 A1, 2013 ;
Location in patent: Page/Page column 229 ;
反应条件
sodium hydroxide in water T=40°C; 2 h;
参考文献
Organic Process Research and Development, , vol. 11, # 2 p. 200 - 205
反应条件
1.1: N-ethyl-N,N-diisopropylamine; O-(benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium tetrafluoroborate / N,N-dimethyl-formamide / 15 h / 20 °C 2.1: water; lithium hydroxide hydrate / tetrahydrofuran / 0.5 h / 20 °C 2.2: pH 5 / Cooling with ice View Scheme
参考文献
ADVENCHEN LABORATORIES, LLC
Patent: WO2012/34055 A2, 2012 ;
WO 2012/034055 A2
反应条件
in N,N-dimethyl-formamide T=20°C; 1 h;
参考文献
Krief, A.; Trabelsi, M.
Tetrahedron Letters, 1987 , vol. 28, # 36 p. 4225 - 4228
反应条件
1.1: triethylamine; isobutyl chloroformate / tetrahydrofuran / 1 h / -10 °C
1.2: 2.5 h / Cooling with ice
2.1: trichloroisocyanuric acid / 2,2,6,6-tetramethyl-1-piperidinyloxy, free radical / dichloromethane / 0.67 h / -5 - 20 °C
View Scheme
参考文献
ELI LILLY AND COMPANY; COATES, David, Andrew; GILMOUR, Raymond; MARTIN, Jose, Alfredo; MARTIN DE LA NAVA, Eva, Maria
Patent: WO2012/74761 A1, 2012 ;
反应条件
1: With triethylamine; isobutyl chloroformate in tetrahydrofuran
T=-10°C; 1 h;
2: With sodium tetrahydroborate in tetrahydrofuran; water
2.5 h; Cooling with ice;
参考文献
ELI LILLY AND COMPANY; COATES, David, Andrew; GILMOUR, Raymond; MARTIN, Jose, Alfredo; MARTIN DE LA NAVA, Eva, Maria
Patent: WO2012/74761 A1, 2012 ;
Location in patent: Page/Page column 21 ;
反应条件
sodium borohydride; sodium chloride; triethylamine; citric acid in tetrahydrofuran; tetrahydrofuran (100 ml)-water
参考文献
DAIICHI PHARMACEUTICAL CO., LTD.
Patent: US2005/20645 A1, 2005 ;
