2-丙氨基-5-甲氧基四嗪合成路线 （共 17 条）
反应条件
1: (CH3)3NBH3 / xylene 2: 48percent aq. HBr View Scheme
参考文献
van Vliet; Tepper; Dijkstra; Damsma; Wikstroem; Pugsley; Akunne; Heffner; Glase; Wise
Journal of medicinal chemistry, 1996 , vol. 39, # 21 p. 4233 - 4237
反应条件
1: methyltretrahydrofuran, 2- / 75 °C 2: hydrogenchloride / water; tetrahydrofuran / 0.25 h / 65 °C View Scheme
参考文献
UCB PHARMA GMBH; ATES, Celal; SCHULE, Arnaud; PALACIO, Magali; DEUTSCH, Paul; VASSELIN, David; CARLY, Nicolas; PHADTARE, Ganesh; YERANDE, Swapnil; DELATINNE, Jean-Pierre; ESCUDERO HERNANDEZ, Maria Luisa; PINILLA, Veronique
Patent: WO2011/161255 A2, 2011 ;
反应条件
1.1: acetonitrile; water / 2 h / 0 - 5 °C 2.1: potassium carbonate / toluene / 60 °C 3.1: hydrogen bromide / acetic acid / 3 h / Reflux 3.2: pH 12.5 3.3: pH 9 - 9.5 4.1: sodium hydrogencarbonate / acetonitrile / 9 h / Reflux 4.2: pH 1 - 2 4.3: pH 7 - 7.5 View Scheme
参考文献
Journal of medicinal chemistry, , vol. 39, # 21 p. 4233 - 4237
参考文献
Marquillas Olondriz, Francisco; Pomares Marco, Marta
Patent: US2011/152543 A1, 2011 ;
反应条件
1.1: methyltretrahydrofuran, 2- / 75 °C 2.1: hydrogenchloride / water; tetrahydrofuran / 0.25 h / 65 °C 3.1: sodium hydrogensulfite; water; hydrogen bromide; acetic acid / 2 h / Reflux 4.1: sodium carbonate / o-xylene; water / 70 - 80 °C 4.2: Reflux 4.3: 15 - 55 °C View Scheme
参考文献
UCB PHARMA GMBH; ATES, Celal; SCHULE, Arnaud; PALACIO, Magali; DEUTSCH, Paul; VASSELIN, David; CARLY, Nicolas; PHADTARE, Ganesh; YERANDE, Swapnil; DELATINNE, Jean-Pierre; ESCUDERO HERNANDEZ, Maria Luisa; PINILLA, Veronique
Patent: WO2011/161255 A2, 2011 ;
反应条件
potassium carbonate in 2-methyl tetrahydrofuran
Reflux; Product distribution / selectivity;
参考文献
UCB PHARMA GMBH; Ates, Celal; Schule, Arnaud; Palacio, Magali; Deutsch, Paul; Vasselin, David; Carly, Nicolas; Phadtare, Ganesh; Yerande, Swapnil; Delatinne, Jean-Pierre; Escudero Hernandez, Maria Luisa; Pinilla, Veronique
Patent: US2013/102794 A1, 2013 ;
Location in patent: Paragraph 0199-0201 ;
反应条件
1: With acetic acid in dichloromethane
0.5 h; Inert atmosphere;
2: With sodium cyanoborohydride in methanol; dichloromethane
T=0 - 20°C; Inert atmosphere;
参考文献
Johnson, Mark; Antonio, Tamara; Reith, Maarten E. A.; Dutta, Aloke K.
Journal of Medicinal Chemistry, 2012 , vol. 55, # 12 p. 5826 - 5840
反应条件
sodium tris(acetoxy)borohydride in 1,2-dichloro-ethane
T=20°C; Inert atmosphere;
参考文献
Soriano, Aroa; Ventura, Ruben; Molero, Anabel; Hoen, Rob; Casado, Vicent; Corte, Antoni; Fanelli, Francesca; Albericio, Fernando; Lluis, Carmen; Franco, Rafael; Royo, Miriam
Journal of Medicinal Chemistry, 2009 , vol. 52, # 18 p. 5590 - 5602
反应条件
sodium cyanoborohydride; acetic acid in methanol
参考文献
van Vliet; Tepper; Dijkstra; Damsma; Wikstroem; Pugsley; Akunne; Heffner; Glase; Wise
Journal of medicinal chemistry, 1996 , vol. 39, # 21 p. 4233 - 4237
