4-氯甲基-N-[4-甲基-3-[[4-(吡啶-3-基)嘧啶-2-基]氨基]苯基]苯甲酰胺合成路线 （共 12 条）
反应条件
potassium carbonate in tetrahydrofuran T=0 - 20°C; 1.16667 - 4.25 h; Conversion of starting material;
参考文献
INSTYTUT FARMACEUTYCZNY
Patent: WO2006/71130 A2, 2006 ;
Location in patent: Page/Page column 25-27 ;
反应条件
1: 4-(chloromethyl)benzoic acid With thionyl chloride in 1,4-dioxane; N,N-dimethyl-formamide T=65 - 70°C; 10 - 12 h; 2: N-(5-amino-2-methylphenyl)-4-(pyridin-3-yl)-2-pyrimidine-amine With pyridine in tetrahydrofuran; 1,4-dioxane; N,N-dimethyl-formamide T=-5 - 5°C; 1 - 1.5 h;
参考文献
ACTAVIS GROUP PTC EHF; KHUNT, Mayur, Devjibhai; PATIL, Nilesh, Sudhir; PAGIRE, Haushabhau, Shivaji; PRADHAN, Nitin, Sharadchandra
Patent: WO2011/95835 A1, 2011 ;
Location in patent: Page/Page column 32 ;
反应条件
1: 8.9 g / SnCl2; aq. HCl / 0.5 h 2: 61 percent / dimethylformamide / 2 h / 0 °C View Scheme
参考文献
Heo, Yumi; Hyun, Dajung; Kumar, Manian Rajesh; Jung, Hyun Min; Lee, Sunwoo
Tetrahedron Letters, 2012 , vol. 53, # 49 p. 6657 - 6661
反应条件
1: HNO3 / ethanol / Heating 2: NaOH / propan-2-ol / 24 h / Heating 3: 8.9 g / SnCl2; aq. HCl / 0.5 h 4: 61 percent / dimethylformamide / 2 h / 0 °C View Scheme
参考文献
Ingham, Richard J.; Riva, Elena; Nikbin, Nikzad; Baxendale, Ian R.; Ley, Steven V.
Organic Letters, 2012 , vol. 14, # 15 p. 3920 - 3923
反应条件
1: ethanol / Heating 2: NaOH / propan-2-ol / 24 h / Heating 3: 8.9 g / SnCl2; aq. HCl / 0.5 h 4: 61 percent / dimethylformamide / 2 h / 0 °C View Scheme
参考文献
Liu, Yi-Feng; Wang, Cui-Ling; Bai, Ya-Jun; Han, Ning; Jiao, Jun-Ping; Qi, Xiao-Li
Organic Process Research and Development, 2008 , vol. 12, # 3 p. 490 - 495
反应条件
1: NaOH / propan-2-ol / 24 h / Heating 2: 8.9 g / SnCl2; aq. HCl / 0.5 h 3: 61 percent / dimethylformamide / 2 h / 0 °C View Scheme
参考文献
Liu, Yi-Feng; Wang, Cui-Ling; Bai, Ya-Jun; Han, Ning; Jiao, Jun-Ping; Qi, Xiao-Li
Organic Process Research and Development, 2008 , vol. 12, # 3 p. 490 - 495
反应条件
1: potassium tert-butylate / dimethyl sulfoxide / 12 h / 120 °C 2: tin(ll) chloride; hydrogenchloride / methanol / 10 h / 50 °C 3: triethylamine / tetrahydrofuran / 7 h / 0 - 20 °C View Scheme
参考文献
Liu, Yi-Feng; Wang, Cui-Ling; Bai, Ya-Jun; Han, Ning; Jiao, Jun-Ping; Qi, Xiao-Li
Organic Process Research and Development, 2008 , vol. 12, # 3 p. 490 - 495
反应条件
1: 1-(2,6-diisopropylphenyl)-3-(2-oxo-2-(2,4,6-tri-tert-butylphenylamino)ethyl)-1H-imidazol-3-ium bromide; palladium diacetate; sodium hydroxide / dimethyl sulfoxide; water / 10 h / 100 °C 2: potassium tert-butylate / dimethyl sulfoxide / 12 h / 120 °C 3: tin(ll) chloride; hydrogenchloride / methanol / 10 h / 50 °C 4: triethylamine / tetrahydrofuran / 7 h / 0 - 20 °C View Scheme
参考文献
Heo, Yumi; Hyun, Dajung; Kumar, Manian Rajesh; Jung, Hyun Min; Lee, Sunwoo
Tetrahedron Letters, 2012 , vol. 53, # 49 p. 6657 - 6661
反应条件
1.1: bromine; iron / 1.5 h / 80 °C / |Inert atmosphere; |Schlenk technique 2.1: copper(l) iodide; potassium carbonate; N-methyl-2-(methylamino)ethylamine / 1,4-dioxane / 20 h / 20 - 100 °C / |Inert atmosphere; |Schlenk technique 3.1: hydrazine hydrate; anhydrous iron chloride; carbon / water / 80 °C / |Inert atmosphere; |Schlenk technique 4.1: triethylamine / tetrahydrofuran / 0.17 h / 0 °C / |Inert atmosphere; |Schlenk technique 4.2: 3.17 h / 0 °C / |Inert atmosphere; |Schlenk technique View Scheme
参考文献
Liu, Yi-Feng; Wang, Cui-Ling; Bai, Ya-Jun; Han, Ning; Jiao, Jun-Ping; Qi, Xiao-Li
Organic Process Research and Development, 2008 , vol. 12, # 3 p. 490 - 495
反应条件
1.1: copper(l) iodide; potassium carbonate; N-methyl-2-(methylamino)ethylamine / 1,4-dioxane / 20 h / 20 - 100 °C / |Inert atmosphere; |Schlenk technique 2.1: hydrazine hydrate; anhydrous iron chloride; carbon / water / 80 °C / |Inert atmosphere; |Schlenk technique 3.1: triethylamine / tetrahydrofuran / 0.17 h / 0 °C / |Inert atmosphere; |Schlenk technique 3.2: 3.17 h / 0 °C / |Inert atmosphere; |Schlenk technique View Scheme
参考文献
Liu, Yi-Feng; Wang, Cui-Ling; Bai, Ya-Jun; Han, Ning; Jiao, Jun-Ping; Qi, Xiao-Li
Organic Process Research and Development, 2008 , vol. 12, # 3 p. 490 - 495
