阿奇沙坦沙坦中间体甲酯C3合成路线 （共 19 条）
反应条件
1: 2-methoxycarbonyl-6-nitrobenzoic acid; triethylamine With diphenyl phosphoryl azide in DMF (N,N-dimethyl-formamide) T=20 - 35°C; 3 h; Industry scale; 2: tert-butyl alcohol in DMF (N,N-dimethyl-formamide) T=85 - 90°C; 4 - 7 h; Heating / reflux;
参考文献
Takeda Chemical Industries, Ltd.
Patent: EP1420016 A1, 2004 ;
Location in patent: Page 31-32 ;
反应条件
1: 2-methoxycarbonyl-6-nitrobenzoic acid With diphenyl phosphoryl azide; triethylamine in N,N-dimethyl-formamide T=20 - 31°C; Inert atmosphere; 2: tert-butyl alcohol in N,N-dimethyl-formamide T=85 - 87°C; 9 h; 3: With methanol T=50 - 55°C; 3 h;
参考文献
MITSUBISHI TANABE PHARMA CORPORATION
Patent: US2012/232283 A1, 2012 ;
Location in patent: Page/Page column 43 ;
反应条件
1: acid chloride of 1-methylhydrogen-3-nitrophthalate; N,N-dimethyl-formamide With sodium azide; tetrabutylammomium bromide in toluene T=-10 - -5°C; 4 h; 2: tert-butyl alcohol in toluene T=80 - 85°C; 1 h;
参考文献
WO2011/145100 A1, ;
Page/Page column 5 ;
反应条件
1: SOCl2, DMF / toluene / 0.5 h / Heating 2: NaN3 / acetone; H2O / 1 h 3: 1.5 h / Heating View Scheme
参考文献
Journal of Medicinal Chemistry, , vol. 36, # 15 p. 2182 - 2195
反应条件
1: concd. H2SO4 / methanol 2: SOCl2, DMF / toluene / 0.5 h / Heating 3: NaN3 / acetone; H2O / 1 h 4: 1.5 h / Heating View Scheme
参考文献
Journal of Medicinal Chemistry, , vol. 36, # 15 p. 2182 - 2195
反应条件
1: NaN3 / acetone; H2O / 1 h 2: 1.5 h / Heating View Scheme
参考文献
Journal of Medicinal Chemistry, , vol. 36, # 15 p. 2182 - 2195
反应条件
1.5 h; Heating; Yield given;
参考文献
Journal of Medicinal Chemistry, , vol. 36, # 15 p. 2182 - 2195
反应条件
potassium carbonate in acetonitrile 4 h; Heating;
参考文献
Kubo, Keiji; Kohara, Yasuhisa; Imamiya, Eiko; Sugiura, Yoshihiro; Inada, Yoshiyuki; et al.
Journal of Medicinal Chemistry, 1993 , vol. 36, # 15 p. 2182 - 2195
反应条件
potassium carbonate in acetonitrile T=82°C; 5 h;
参考文献
Takeda Chemical Industries, Ltd.
Patent: EP1420016 A1, 2004 ;
Location in patent: Page 16-17 ;
反应条件
1: 85 percent / K2CO3 / acetonitrile / 4 h / Heating 2: 77 percent / 30percent ethanolic HCl / ethyl acetate / 1 h / Ambient temperature 3: 1.) FeCl3*6H2O, activated carbon, 2.) hydrazine monohydrate / 1.) MeOH, THF, reflux, 30 min, 2.) MeOH, THF, reflux, 14 h 4: 78 percent / ethanol / 1.5 h / Heating View Scheme
参考文献
Kubo, Keiji; Kohara, Yasuhisa; Imamiya, Eiko; Sugiura, Yoshihiro; Inada, Yoshiyuki; et al.
Journal of Medicinal Chemistry, 1993 , vol. 36, # 15 p. 2182 - 2195
