2-丙氨基-5-甲氧基四嗪合成路线 （共 17 条）
反应条件
1.1: sodium acetate; acetic acid; sodium tris(acetoxy)borohydride / tetrahydrofuran / 0 - 10 °C
1.2: 0.5 h / 0 - 20 °C
1.3: 1.33 h / 10 - 50 °C
2.1: potassium carbonate / 2-methyl tetrahydrofuran / Reflux
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: acetic acid; methanol; tetrahydrofuran
2: Mol. sieves; sodium cyanoborohydride
View Scheme
参考文献
Mukherjee, Jogeshwar; Yang, Zhi-Ying; Brown, Terry; Jiang, Meiying; Kapp, Oscar; et al.
Medicinal Chemistry Research, 1995 , vol. 5, # 2/3 p. 174 - 192
反应条件
1.1: lauryl mercaptan / ethyl acetate / Inert atmosphere; Reflux
1.2: 0.58 h / Inert atmosphere; Reflux
1.3: 0.08 h / Reflux
2.1: potassium carbonate / 2-methyl tetrahydrofuran / Reflux
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
View Scheme
参考文献
Marquillas Olondriz, Francisco; Pomares Marco, Marta
Patent: US2011/152543 A1, 2011 ;
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
boron tribromide in dichloromethane
T=-40 - 20°C;
参考文献
Biswas, Swati; Zhang, Suhong; Fernandez, Fernando; Ghosh, Balaram; Zhen, Juan; Kuzhikandathil, Eldo; Reith, Maarten E. A.; Dutta, Aloke K.
Journal of Medicinal Chemistry, 2008 , vol. 51, # 1 p. 101 - 117
反应条件
hydrogenchloride in diethyl ether; ethyl acetate
参考文献
Ghoshs, Balaram; Antonio, Tamara; Reith, Maarten E. A.; Dutta, Aloke K.
Journal of Medicinal Chemistry, 2010 , vol. 53, # 5 p. 2114 - 2125
Title/Abstract Full Text View citing articles Show Details
Ghosh, Balaram; Antonio, Tamara; Gopishetty, Bhaskar; Reith, Maarten; Dutta, Aloke
Bioorganic and Medicinal Chemistry, 2010 , vol. 18, # 15 p. 5661 - 5674
