THE REGENTS OF THE UNIVERSITY OF CALIFORNIA; VERKMAN, Alan S.; PHUAN, Puay-Wah; KURTH, Mark J.; KNAPP, John
Patent: WO2012/166654 A1, 2012 ;
Location in patent: Page/Page column 88 ;
WO 2012/166654 A1
Knapp, John M.; Wood, Alex B.; Phuan, Puay-Wah; Lodewyk, Michael W.; Tantillo, Dean J.; Verkman; Kurth, Mark J.
Journal of Medicinal Chemistry, 2012 , vol. 55, # 3 p. 1242 - 1251
1.1: trichlorophosphate / 2 h / Inert atmosphere; Reflux
1.2: 3 h / 20 °C / Inert atmosphere
2.1: hydroxylamine hydrochloride; triethylamine / ethanol / 3 h / Reflux
3.1: thionyl chloride / benzene / 4 h / Inert atmosphere; Reflux
4.1: 1,4-dioxane / Reflux
View Scheme
参考文献
Knapp, John M.; Wood, Alex B.; Phuan, Puay-Wah; Lodewyk, Michael W.; Tantillo, Dean J.; Verkman; Kurth, Mark J.
Journal of Medicinal Chemistry, 2012 , vol. 55, # 3 p. 1242 - 1251
1.1: tetrahydrofuran / 0 - 20 °C / Inert atmosphere
2.1: trichlorophosphate / 2 h / Inert atmosphere; Reflux
2.2: 3 h / 20 °C / Inert atmosphere
3.1: hydroxylamine hydrochloride; triethylamine / ethanol / 3 h / Reflux
4.1: thionyl chloride / benzene / 4 h / Inert atmosphere; Reflux
5.1: 1,4-dioxane / Reflux
View Scheme
参考文献
Knapp, John M.; Wood, Alex B.; Phuan, Puay-Wah; Lodewyk, Michael W.; Tantillo, Dean J.; Verkman; Kurth, Mark J.
Journal of Medicinal Chemistry, 2012 , vol. 55, # 3 p. 1242 - 1251
Knapp, John M.; Wood, Alex B.; Phuan, Puay-Wah; Lodewyk, Michael W.; Tantillo, Dean J.; Verkman; Kurth, Mark J.
Journal of Medicinal Chemistry, 2012 , vol. 55, # 3 p. 1242 - 1251
1: 3-methoxy-benzoic acid With 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; triethylamine in dichloromethane; N,N-dimethyl-formamide
T=20°C; 0.5 h;
2: 2-((2-aminoethyl)amino)-5,7-dimethylquinoline-3-carbonitrile in dichloromethane; N,N-dimethyl-formamide
参考文献
THE REGENTS OF THE UNIVERSITY OF CALIFORNIA; VERKMAN, Alan S.; PHUAN, Puay-Wah; KURTH, Mark J.; KNAPP, John
Patent: WO2012/166654 A1, 2012 ;
Location in patent: Page/Page column 88-89 ;
WO 2012/166654 A1