N-(2-吡嗪基羰基)-L-苯丙氨酸合成路线 (共 12 条)
反应条件
1: With sodium carbonate in water; toluene T=10 - 25°C; 3 h; 2: With hydrogenchloride in methanol; water T=15 - 20°C; pH=3;
参考文献
WO2011/87822 A1, ;
Page/Page column 120-121 ;
WO 2011/087822 A1
反应条件
sodium hydroxide in 1,4-dioxane; methanol 1 h;
参考文献
Organic and Biomolecular Chemistry, , vol. 5, # 9 p. 1416 - 1426
反应条件
1: in dichloromethane T=-40 - 20°C; 19.5 h; 2: With water; citric acid in dichloromethane
参考文献
Tetrahedron, , vol. 65, # 34 p. 7105 - 7108
反应条件
1.1: BOP; DiPEA / dimethylformamide / 0.25 h 1.2: 70 percent / dimethylformamide / 1 h 2.1: 69 percent / aq. NaOH / dioxane; methanol / 1 h View Scheme
参考文献
Organic and Biomolecular Chemistry, , vol. 5, # 9 p. 1416 - 1426
反应条件
1: 2-carboxypyrazine With chloroformic acid ethyl ester; triethylamine in acetone T=-5 - 30°C; 3.5 h; 2: L-Phe sodium salt in water; acetone T=0 - 30°C; 18 h; Product distribution / selectivity;
参考文献
WO2009/36281 A2, ;
Page/Page column 38-39 ;
反应条件
1.1: BOP; DiPEA / dimethylformamide / 0.25 h 1.2: 70 percent / dimethylformamide / 1 h 2.1: 69 percent / aq. NaOH / dioxane; methanol / 1 h View Scheme
参考文献
Organic and Biomolecular Chemistry, , vol. 5, # 9 p. 1416 - 1426
反应条件
1: benzotriazol-1-ol; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; N-ethyl-N,N-diisopropylamine / N,N-dimethyl-formamide / 0 - 20 °C / Inert atmosphere 2: lithium hydroxide hydrate / tetrahydrofuran; water / 3 h / 0 °C View Scheme
参考文献
Journal of Medicinal Chemistry, , vol. 54, # 13 p. 4365 - 4377
反应条件
hydrogenchloride; oxygen in dimethyl sulfoxide T=70°C; Oxidation; hydrolysis; pH=1.0; 250 h; KineticsProduct distribution;
参考文献
Journal of Pharmaceutical Sciences, , vol. 89, # 6 p. 758 - 765
反应条件
sodium hydroxide; oxygen in dimethyl sulfoxide T=70°C; Oxidation; hydrolysis; pH=12.0; 250 h; KineticsProduct distribution;
参考文献
Journal of Pharmaceutical Sciences, , vol. 89, # 6 p. 758 - 765
反应条件
dihydrogen peroxide in water T=20°C; Oxidation; hydrolysis; 1 h; KineticsProduct distribution; Further Variations:Solvents;
参考文献
Journal of Pharmaceutical Sciences, , vol. 89, # 6 p. 758 - 765