N-[3-氟-4-[(甲基氨基)羰基]苯基]-2-甲基-丙氨酸甲酯合成路线 (共 5 条)
反应条件
1: 2-(3-fluoro-4-methylcarbamoyl-phenylamino)-2-methyl-propionic acid With potassium carbonate in water; N,N-dimethyl-formamide T=30°C; 2: methyl iodide in water; N,N-dimethyl-formamide T=32 - 40°C; 1.08333 h;
参考文献
MEDIVATION PROSTATE THERAPEUTICS, INC.; JAIN, Rajendra, Parasmal; ANGELAUD, Remy; THOMPSON, Andrew; LAMBERSON, Carol; GREENFIELD, Scott
Patent: WO2011/106570 A1, 2011 ;
Location in patent: Page/Page column 44 ;
反应条件
1.1: thionyl chloride / N,N-dimethyl-formamide; isopropanol acetate / 4.58 h / 21 - 72 °C / Inert atmosphere; Industry scale 2.1: water; isopropanol acetate / 1.08 h / 2 - 35 °C / Inert atmosphere; Industry scale 3.1: potassium carbonate / copper(l) chloride / N,N-dimethyl-formamide; water / 30 °C 3.2: 105 °C / Inert atmosphere 3.3: pH 4 4.1: potassium carbonate / N,N-dimethyl-formamide; water / 30 °C 4.2: 1.08 h / 32 - 40 °C View Scheme
参考文献
MEDIVATION PROSTATE THERAPEUTICS, INC.; JAIN, Rajendra, Parasmal; ANGELAUD, Remy; THOMPSON, Andrew; LAMBERSON, Carol; GREENFIELD, Scott
Patent: WO2011/106570 A1, 2011 ;
反应条件
1.1: water; isopropanol acetate / 1.08 h / 2 - 35 °C / Inert atmosphere; Industry scale 2.1: potassium carbonate / copper(l) chloride / N,N-dimethyl-formamide; water / 30 °C 2.2: 105 °C / Inert atmosphere 2.3: pH 4 3.1: potassium carbonate / N,N-dimethyl-formamide; water / 30 °C 3.2: 1.08 h / 32 - 40 °C View Scheme
参考文献
MEDIVATION PROSTATE THERAPEUTICS, INC.; JAIN, Rajendra, Parasmal; ANGELAUD, Remy; THOMPSON, Andrew; LAMBERSON, Carol; GREENFIELD, Scott
Patent: WO2011/106570 A1, 2011 ;
反应条件
1.1: potassium carbonate / copper(l) chloride / N,N-dimethyl-formamide; water / 30 °C 1.2: 105 °C / Inert atmosphere 1.3: pH 4 2.1: potassium carbonate / N,N-dimethyl-formamide; water / 30 °C 2.2: 1.08 h / 32 - 40 °C View Scheme
参考文献
MEDIVATION PROSTATE THERAPEUTICS, INC.; JAIN, Rajendra, Parasmal; ANGELAUD, Remy; THOMPSON, Andrew; LAMBERSON, Carol; GREENFIELD, Scott
Patent: WO2011/106570 A1, 2011 ;
反应条件
in isopropanol acetate; dimethyl sulfoxide T=83 - 84°C; 17.5 h;
参考文献
MEDIVATION PROSTATE THERAPEUTICS, INC.; JAIN, Rajendra, Parasmal; ANGELAUD, Remy; THOMPSON, Andrew; LAMBERSON, Carol; GREENFIELD, Scott
Patent: WO2011/106570 A1, 2011 ;
Location in patent: Page/Page column 46 ;