N-叔丁基氧基羰基-氨基-4,4-联苯-R-丙氨酸甲酯合成路线 (共 5 条)
反应条件
potassium carbonate; tetrakis(triphenylphosphine) palladium(0) in toluene T=80°C; 2 h;
参考文献
Ksander, Gary M.; Ghai, Raj D.; deJesus, Reynalda; Diefenbacher, Clive G.; Yuan, Andrew; et al.
Journal of Medicinal Chemistry, 1995 , vol. 38, # 10 p. 1689 - 1700
反应条件
nitrogen; potassium carbonate; tetrakis (triphenylphosphine) palladium (0) in toluene
参考文献
Ciba-Geigy Corporation
Patent: US5217996 A1, 1993 ;
US 5217996 A
反应条件
1: 96 percent / pyridine / CH2Cl2 / 0.08 h / -15 °C 2: 100 percent / potassium carbonate / tetrakis(triphenylphosphine)palladium(0) / toluene / 2 h / 80 °C View Scheme
参考文献
Ksander, Gary M.; Ghai, Raj D.; deJesus, Reynalda; Diefenbacher, Clive G.; Yuan, Andrew; et al.
Journal of Medicinal Chemistry, 1995 , vol. 38, # 10 p. 1689 - 1700
反应条件
[R,R-RhMe-Duphos]; hydrogen in methanol; ethyl acetate P=2068.65 Torr; 12 h;
参考文献
Blake, James F.; Kallan, Nicholas C.; Xiao, Dengming; Xu, Rui; Bencsik, Josef R.; Skelton, Nicholas J.; Spencer, Keith L.; Mitchell, Ian S.; Woessner, Richard D.; Gloor, Susan L.; Risom, Tyler; Gross, Stefan D.; Martinson, Matthew; Morales, Tony H.; Vigers, Guy P.A.; Brandhuber, Barbara J.
Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 19 p. 5607 - 5612
反应条件
1: 95 percent / 1 N aq. NaOH / tetrahydrofuran; methanol / Ambient temperature
2: 97 percent / triethylamine, 1-ethyl-3-<(dimethylamino)propyl>carbodiimide hydrochloride, hydroxybenzotriazole / CH2Cl2 / 16 h / Ambient temperature
3: 100 percent / LiAlH4 / diethyl ether / 0.33 h / 0 °C
4: 78 percent / CH2Cl2 / 16 h / Ambient temperature
5: 9.5 percent / H2 / 10percent Pd/C / ethanol / 6 h / 2585.7 Torr
6: 95 percent / HCl (gas) / CH2Cl2 / 5 h / Ambient temperature
7: pyridine / CH2Cl2 / 16 h / Ambient temperature
8: toluene / 1 h / 80 °C
9: HCl (gas) / CH2Cl2 / 16 h / Ambient temperature
View Scheme
参考文献
Ksander, Gary M.; Ghai, Raj D.; deJesus, Reynalda; Diefenbacher, Clive G.; Yuan, Andrew; et al.
Journal of Medicinal Chemistry, 1995 , vol. 38, # 10 p. 1689 - 1700