1-(4-甲氧基苯基)-1-氢-[1,2,3]三氮唑-4-甲酸合成路线 （共 5 条）
反应条件
1: With sodium hydroxide in methanol; water
T=20°C; Inert atmosphere;
2: With hydrogenchloride in water
pH=5 - Ca. 6; Inert atmosphere;
参考文献
Bai, Suping; Li, Shihong; Xu, Jinbin; Peng, Xin; Sai, Kiran; Chu, Wenhua; Tu, Zhude; Zeng, Chenbo; Mach, Robert H.
Journal of Medicinal Chemistry, 2014 , vol. 57, # 10 p. 4239 - 4251
反应条件
sodium azide; sodium carbonate; sodium L-ascorbate; copper(II) sulfate; DL-proline in dimethyl sulfoxide
T=65°C;
参考文献
Aufort, Marie; Herscovici, Jean; Bouhours, Pascale; Moreau, Nicole; Girard, Christian
Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 3 p. 1195 - 1198
反应条件
1: acetylenecarboxylic acid With 2-nitrobenzeneboronic acid in 1,2-dichloro-ethane
T=25°C; 0.166667 h; Inert atmosphere;
2: 4-Methoxyphenylazide in 1,2-dichloro-ethane
T=25°C; Huisgen cycloaddition; 24 h; Inert atmosphere; regioselective reaction;
参考文献
Zheng, Hongchao; McDonald, Robert; Hall, Dennis G.
Chemistry - A European Journal, 2010 , vol. 16, # 18 p. 5454 - 5460
反应条件
1.1: hydrogenchloride; sodium nitrite / water / 0 °C / |Inert atmosphere
1.2: 0 - 20 °C / pH 7 -Ca. 8 / |Inert atmosphere
2.1: copper(II) sulfate; sodium L-ascorbate; BPDS / water; N,N-dimethyl-formamide / 0 - 20 °C / |Inert atmosphere
3.1: sodium hydroxide / water; methanol / 20 °C / |Inert atmosphere
3.2: pH 5 - Ca. 6 / |Inert atmosphere
View Scheme
参考文献
Bai, Suping; Li, Shihong; Xu, Jinbin; Peng, Xin; Sai, Kiran; Chu, Wenhua; Tu, Zhude; Zeng, Chenbo; Mach, Robert H.
Journal of Medicinal Chemistry, 2014 , vol. 57, # 10 p. 4239 - 4251
反应条件
1.1: copper(II) sulfate; sodium L-ascorbate; BPDS / water; N,N-dimethyl-formamide / 0 - 20 °C / |Inert atmosphere
2.1: sodium hydroxide / water; methanol / 20 °C / |Inert atmosphere
2.2: pH 5 - Ca. 6 / |Inert atmosphere
View Scheme
参考文献
Bai, Suping; Li, Shihong; Xu, Jinbin; Peng, Xin; Sai, Kiran; Chu, Wenhua; Tu, Zhude; Zeng, Chenbo; Mach, Robert H.
Journal of Medicinal Chemistry, 2014 , vol. 57, # 10 p. 4239 - 4251
