4-[1-[(2,4-二氨基-6-蝶啶基)甲基]-3-丁炔基]苯甲酸合成路线 （共 7 条）
反应条件
in dimethyl sulfoxide T=120°C; 0.5 h;
参考文献
Vaidya, Chitra M.; Wright, Joel E.; Rosowsky, Andre
Journal of Medicinal Chemistry, 2002 , vol. 45, # 8 p. 1690 - 1696
反应条件
N-ethyl-N,N-diisopropylamine in 1-methyl-pyrrolidin-2-one T=120°C; 0.5 h; Reagent/catalyst;
参考文献
PLUS CHEMICALS S.A.; TEVA PHARMACEUTICALS USA, INC.; TISENI, Paolo, Simone; GALLUZZO, Christian; CANAVESI, Augusto; BILJAN, Tomislav
Patent: WO2013/96800 A1, 2013 ;
Location in patent: Page/Page column 17; 18 ;
反应条件
1: 720 mg / aq. NaOH / 2-methoxy-ethanol / 24 h / 20 °C 2: 60 percent / dimethylsulfoxide / 0.5 h / 120 °C View Scheme
参考文献
ALLOS THERAPEUTICS, INC.
Patent: US2011/190305 A1, 2011 ;
参考文献
AVRA LABORATORIES PRIVATE LIMITED; ALLA, Rama Rao Venkata; RAMARAO, Chandrashekar; MICHEL, Patrick Thomas; NITLIKAR, Lakshmikant Hanumanthrao; KALAM, Bhupathi Reddy; DUDUKA, Ramprasad
Patent: WO2013/164856 A1, 2013 ;
Location in patent: Page/Page column 21; 22 ;
反应条件
1: 720 mg / aq. NaOH / 2-methoxy-ethanol / 24 h / 20 °C 2: 60 percent / dimethylsulfoxide / 0.5 h / 120 °C View Scheme
参考文献
Vaidya, Chitra M.; Wright, Joel E.; Rosowsky, Andre
Journal of Medicinal Chemistry, 2002 , vol. 45, # 8 p. 1690 - 1696
反应条件
1.1: water; sodium hydroxide / 15 - 20 °C 2.1: sodium methylate / methanol 2.2: 3 h / 90 °C 3.1: sodium hydroxide / water / 2 h / 100 °C / |Reflux 3.2: 0 °C 4.1: sulfuric acid / |Reflux 5.1: water; acetone / 5 h / |Reflux 6.1: phosphorus trichoride / toluene / 0.5 h / 120 °C / |Reflux 7.1: toluene / 4 h / 120 °C / |Reflux 8.1: dihydrogen peroxide; potassium carbonate / methanol; water / 0 - 20 °C 9.1: trifluoroacetic acid; NsNHNH2 / 2 h / 20 °C 10.1: potassium hydroxide; water / 0 - 20 °C 10.2: 6 h / 0 - 25 °C 11.1: methanol / |Reflux View Scheme
参考文献
AVRA LABORATORIES PRIVATE LIMITED; ALLA, Rama Rao Venkata; RAMARAO, Chandrashekar; MICHEL, Patrick Thomas; NITLIKAR, Lakshmikant Hanumanthrao; KALAM, Bhupathi Reddy; DUDUKA, Ramprasad
Patent: WO2013/164856 A1, 2013 ;
反应条件
1.1: sodium methylate / methanol 1.2: 3 h / 90 °C 2.1: sodium hydroxide / water / 2 h / 100 °C / |Reflux 2.2: 0 °C 3.1: sulfuric acid / |Reflux 4.1: water; acetone / 5 h / |Reflux 5.1: phosphorus trichoride / toluene / 0.5 h / 120 °C / |Reflux 6.1: toluene / 4 h / 120 °C / |Reflux 7.1: dihydrogen peroxide; potassium carbonate / methanol; water / 0 - 20 °C 8.1: trifluoroacetic acid; NsNHNH2 / 2 h / 20 °C 9.1: potassium hydroxide; water / 0 - 20 °C 9.2: 6 h / 0 - 25 °C 10.1: methanol / |Reflux View Scheme
参考文献
AVRA LABORATORIES PRIVATE LIMITED; ALLA, Rama Rao Venkata; RAMARAO, Chandrashekar; MICHEL, Patrick Thomas; NITLIKAR, Lakshmikant Hanumanthrao; KALAM, Bhupathi Reddy; DUDUKA, Ramprasad
Patent: WO2013/164856 A1, 2013 ;
