1-Boc-4-(4-甲氧基-4-氧基-2-丁稀)哌啶合成路线 （共 9 条）
反应条件
1: dimethyl methoxycarbonylmethanephosphonate With lithium hexamethyldisilazane in tetrahydrofuran T=-78°C; 0.333333 h; 2: 4-(2-oxo-ethyl)-piperidine-1-carboxylic acid tert-butyl ester in tetrahydrofuran T=-78°C; 0.75 h; 3: With triethylamine more than 3 stages;
参考文献
JANSSEN PHARMACEUTICA N.V.
Patent: WO2004/20435 A1, 2004 ;
Location in patent: Page 113 ;
反应条件
1: 87 percent / H2 / PtO2 / H2O; acetic acid / 72 h / 2844.3 Torr 2: Et3N / H2O; dioxane / 96 h 3: 99 percent / BH3 / tetrahydrofuran / 1 h 4: 1.) oxalyl chloride, DMSO, 2.) Et3N / 1.) CH2Cl2, -78 deg C, 20 min, 2.) CH2Cl2, from -78 deg C to RT, 1.5 h 5: CH2Cl2 / Ambient temperature View Scheme
参考文献
Egbertson, Melissa S.; Chang, Charles T.-C.; Duggan, Mark E.; Gould, Robert J.; Halczenko, Wasyl; et al.
Journal of Medicinal Chemistry, 1994 , vol. 37, # 16 p. 2537 - 2551
反应条件
1: 1.) oxalyl chloride, DMSO, 2.) Et3N / 1.) CH2Cl2, -78 deg C, 20 min, 2.) CH2Cl2, from -78 deg C to RT, 1.5 h 2: CH2Cl2 / Ambient temperature View Scheme
参考文献
Egbertson, Melissa S.; Chang, Charles T.-C.; Duggan, Mark E.; Gould, Robert J.; Halczenko, Wasyl; et al.
Journal of Medicinal Chemistry, 1994 , vol. 37, # 16 p. 2537 - 2551
反应条件
1: 99 percent / BH3 / tetrahydrofuran / 1 h 2: 1.) oxalyl chloride, DMSO, 2.) Et3N / 1.) CH2Cl2, -78 deg C, 20 min, 2.) CH2Cl2, from -78 deg C to RT, 1.5 h 3: CH2Cl2 / Ambient temperature View Scheme
参考文献
Egbertson, Melissa S.; Chang, Charles T.-C.; Duggan, Mark E.; Gould, Robert J.; Halczenko, Wasyl; et al.
Journal of Medicinal Chemistry, 1994 , vol. 37, # 16 p. 2537 - 2551
反应条件
1: Et3N / H2O; dioxane / 96 h 2: 99 percent / BH3 / tetrahydrofuran / 1 h 3: 1.) oxalyl chloride, DMSO, 2.) Et3N / 1.) CH2Cl2, -78 deg C, 20 min, 2.) CH2Cl2, from -78 deg C to RT, 1.5 h 4: CH2Cl2 / Ambient temperature View Scheme
参考文献
Egbertson, Melissa S.; Chang, Charles T.-C.; Duggan, Mark E.; Gould, Robert J.; Halczenko, Wasyl; et al.
Journal of Medicinal Chemistry, 1994 , vol. 37, # 16 p. 2537 - 2551
反应条件
in dichloromethane Ambient temperature; Yield given;
参考文献
Egbertson, Melissa S.; Chang, Charles T.-C.; Duggan, Mark E.; Gould, Robert J.; Halczenko, Wasyl; et al.
Journal of Medicinal Chemistry, 1994 , vol. 37, # 16 p. 2537 - 2551
反应条件
1: 90 percent / H2 / 10percent Pd/C / ethyl acetate 2: 97 percent / NaOH / methanol 3: 98 percent / BH3 / tetrahydrofuran / 1 h 4: 85 percent / Ph3P, CBr4 / tetrahydrofuran; acetonitrile / 24 h View Scheme
参考文献
Egbertson, Melissa S.; Chang, Charles T.-C.; Duggan, Mark E.; Gould, Robert J.; Halczenko, Wasyl; et al.
Journal of Medicinal Chemistry, 1994 , vol. 37, # 16 p. 2537 - 2551
反应条件
1: 90 percent / H2 / 10percent Pd/C / ethyl acetate 2: 97 percent / NaOH / methanol 3: 98 percent / BH3 / tetrahydrofuran / 1 h View Scheme
参考文献
Egbertson, Melissa S.; Chang, Charles T.-C.; Duggan, Mark E.; Gould, Robert J.; Halczenko, Wasyl; et al.
Journal of Medicinal Chemistry, 1994 , vol. 37, # 16 p. 2537 - 2551
反应条件
1: 90 percent / H2 / 10percent Pd/C / ethyl acetate 2: 97 percent / NaOH / methanol View Scheme
参考文献
Egbertson, Melissa S.; Chang, Charles T.-C.; Duggan, Mark E.; Gould, Robert J.; Halczenko, Wasyl; et al.
Journal of Medicinal Chemistry, 1994 , vol. 37, # 16 p. 2537 - 2551
