2-乙酰氨基-4-溴苯酚合成路线 （共 17 条）
参考文献
Raiford; Linsk
Journal of the American Chemical Society, 1945 , vol. 67, p. 878
反应条件
hydrogenchloride; water in ethanol 4 h; Reflux;
参考文献
Armitage, Mark; Bret, Guillaume; Choudary, Bernie M.; Kingswood, Mike; Loft, Mike; Moore, Steve; Smith, Steve; Urquhart, Michael W. J.
Organic Process Research and Development, 2012 , vol. 16, # 10 p. 1626 - 1634
反应条件
1: hydrogenchloride; water / ethanol / 4 h / |Reflux 2: sodium hydrogencarbonate / tetrahydrofuran / 0.67 h / 5 - 8 °C / |Inert atmosphere 3: potassium carbonate / tetrahydrofuran / 17 h / 20 °C / |Reflux; |Inert atmosphere View Scheme
参考文献
Organic Process Research and Development, , vol. 16, # 10 p. 1626 - 1634
反应条件
1: 90 percent / NaOH, Aliquat 336 / CH2Cl2; acetonitrile / 18 h / Ambient temperature 2: aq. KOH / methanol / 0.5 h / 55 °C View Scheme
参考文献
Journal of Medicinal Chemistry, , vol. 40, # 10 p. 1465 - 1474
反应条件
1.1: potassium carbonate / N,N-dimethyl-formamide / 0.5 h / 70 °C 1.2: 16 h / 60 °C 2.1: potassium acetate / triphenylphosphine; bis(dibenzylideneacetone)-palladium(0) / ethylene glycol dimethyl ether / 150 °C View Scheme
参考文献
HEPTARES THERAPEUTICS LIMITED; CONGREVE, Miles Stuart; ANDREWS, Stephen Philippe; MASON, Jonathan Stephen; RICHARDSON, Christine Mary; BROWN, Giles Albert
Patent: WO2011/95625 A1, 2011 ;
WO 2011/095625 A1
反应条件
1: N-acetyl-2-amino-4-bromophenol With potassium carbonate in N,N-dimethyl-formamide
T=70°C; 0.5 h;
2: methyl iodide in N,N-dimethyl-formamide
T=60°C; 16 h;
参考文献
HEPTARES THERAPEUTICS LIMITED; CONGREVE, Miles Stuart; ANDREWS, Stephen Philippe; MASON, Jonathan Stephen; RICHARDSON, Christine Mary; BROWN, Giles Albert
Patent: WO2011/95625 A1, 2011 ;
Location in patent: Page/Page column 202 ;
WO 2011/095625 A1
反应条件
1.1: hydrogenchloride; water / ethanol / 4 h / |Reflux
2.1: sodium hydrogencarbonate / tetrahydrofuran / 0.67 h / 5 - 8 °C / |Inert atmosphere
3.1: potassium carbonate / tetrahydrofuran / 17 h / 20 °C / |Reflux; |Inert atmosphere
4.1: n-butyllithium / tetrahydrofuran; hexane / 0.83 h / -70 - -60 °C / |Inert atmosphere
4.2: 1.25 h / -70 °C / |Inert atmosphere
5.1: acetic acid; palladium 10 on activated carbon; hydrogen / 6 h / 70 °C / 2068.65 Torr
6.1: sodium hydrogencarbonate / ethylene glycol dimethyl ether / 85 °C / |Inert atmosphere
View Scheme
参考文献
Armitage, Mark; Bret, Guillaume; Choudary, Bernie M.; Kingswood, Mike; Loft, Mike; Moore, Steve; Smith, Steve; Urquhart, Michael W. J.
Organic Process Research and Development, 2012 , vol. 16, # 10 p. 1626 - 1634
