1: sodium hydroxide / water / 1 h / 20 °C 2: chlorosulfonic acid / 4 h / 5 - 130 °C 3: ammonia / water / 10 - 20 °C 4: palladium 10 on activated carbon; hydrogen / methanol / 4 h / 50 °C View Scheme
参考文献
Pan, Li; Jiang, Ying; Liu, Zhen; Liu, Xing-Hai; Liu, Zhuo; Wang, Gang; Li, Zheng-Ming; Wang, Di
European Journal of Medicinal Chemistry, 2012 , vol. 50, p. 18 - 26
1.1: N,N-dimethyl-formamide; thionyl chloride / 4 h / Reflux
2.1: ammonium hydroxide / toluene; water; tetrahydrofuran / 2 h / -10 °C / Reflux
2.2: pH 4
3.1: ammonium hydroxide; (NH4)2CO3; copper(II) sulfate / water / 72 h / 118 °C / Autoclave; Industry scale
4.1: hydrogen / 5 palladium on charcoal / ethanol; water / 8 h / 55 °C / Industry scale
5.1: pyridine / dichloromethane / 0 - 23 °C / Industry scale
6.1: tetrahydrofuran / 1 h / 0 - 23 °C / Industry scale
7.1: sodium hydroxide; water / 30 h / 23 °C / Industry scale
7.2: 0 °C / Industry scale
View Scheme
参考文献
ANADYS PHARMACEUTICALS, INC.
Patent: WO2008/124450 A1, 2008 ;
Elgersma
Recueil des Travaux Chimiques des Pays-Bas, 1929 , vol. 48, p. 766
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King
Journal of the Chemical Society, 1921 , vol. 119, p. 2115