6-氨基-1,4-苯并二氧杂环合成路线 （共 38 条）
反应条件
1: 2,5-dioxopyrrolidin-1-yl 2-(diisopropoxyphosphoryl)acetate; 2,3-dihydro-1,4-benzodioxin-6-amine in dichloromethane T=20°C; 4 h; 2: (carboxymethyl)trimethylammonium chloride hydrazide in methanol; dichloromethane
参考文献
ACS Combinatorial Science, , vol. 15, # 4 p. 208 - 215
反应条件
1: 2,5-dioxopyrrolidin-1-yl 2-(diisopropoxyphosphoryl)propanoate; 2,3-dihydro-1,4-benzodioxin-6-amine in dichloromethane T=20°C; 4 h; 2: (carboxymethyl)trimethylammonium chloride hydrazide in methanol; dichloromethane
参考文献
ACS Combinatorial Science, , vol. 15, # 4 p. 208 - 215
反应条件
1: 1.) NaNO2, H2SO4 / 1.) H2O, 0 deg C, 2.) 80 deg C 2: 69 percent / concd. H2SO4 / 2 h / 0 °C View Scheme
参考文献
Guillaumet, Gerald; Hretani, Mohamed; Coudert, Gerard; Averbeck, Dietrich; Averbeck, Simone
European Journal of Medicinal Chemistry, 1990 , vol. 25, # 1 p. 45 - 51
反应条件
1: 3 h / 20 °C 2: nitric acid; acetic acid / 3 h / 0 - 20 °C 3: sulfuric acid / 6 h / Reflux 4: hydrogen / palladium 10 on activated carbon / methanol / 18 h 5: methanol / 5 h View Scheme
参考文献
Xuanzhu Pharma Co., Ltd.
Patent: EP2532665 A1, 2012 ;
反应条件
1: 1.) NaNO2, H2SO4 / 1.) H2O, 0 deg C, 2.) 80 deg C 2: 75 percent / concd. H2SO4 / 2.5 h / 0 °C 3: 62 percent / 10percent Pd/C / diphenyl ether / 2.5 h / Heating 4: N-bromosuccinimide, AIBN / CCl4 / 6.5 h / Heating 5: NaI / acetone / 6 h / Heating View Scheme
参考文献
Guillaumet, Gerald; Hretani, Mohamed; Coudert, Gerard; Averbeck, Dietrich; Averbeck, Simone
European Journal of Medicinal Chemistry, 1990 , vol. 25, # 1 p. 45 - 51
反应条件
1: acetone View Scheme
参考文献
Renzi et al.
Gazzetta Chimica Italiana, 1956 , vol. 86, p. 1362,1364
反应条件
sulfuric acid; sodium nitrite in water 1.) 0-5 deg C, 0.5 h; 2.) reflux, 0.5 h;
参考文献
Chapleo, Christopher B.; Doxey, John C.; Myers, Peter L.; Myers, Malcolm; Smith, Colin F. C.; Stillings, Michael R.
European Journal of Medicinal Chemistry, 1989 , vol. 24, p. 619 - 622
反应条件
in toluene 6 h; Heating;
参考文献
Novo Nordisk A/S
Patent: US5378714 A1, 1995 ;
US 5378714 A
反应条件
triethylamine in toluene
参考文献
Novo Nordisk A/S
Patent: US5246935 A1, 1993 ;
US 5246935 A
反应条件
1: in ethanol Reflux; 2: With hydrogenchloride in ethanol 6 h; Reflux;
参考文献
Minegishi, Hidemitsu; Fukashiro, Shinji; Ban, Hyun Seung; Nakamura, Hiroyuki
ACS Medicinal Chemistry Letters, 2013 , vol. 4, # 2 p. 297 - 301
