7-氯-1-[2-甲基-4-[(2-甲基苯甲酰)氨基]苯甲酰基]-5-氧代-2,3,4,5-四氢-1H-1-苯并氮杂卓合成路线 （共 16 条）
反应条件
1,8-diazabicyclo[5.4.0]undec-7-ene; triphenylphosphine; palladium diacetate in N,N-dimethyl-formamide T=125°C; 3 h;
参考文献
OTSUKA PHARMACEUTICAL CO., LTD.
Patent: WO2007/26971 A2, 2007 ;
Location in patent: Page/Page column 32-33 ;
反应条件
triethylamine in dichloromethane T=20°C; Acylation; 1.5 h;
参考文献
Kondo, Kazumi; Ogawa, Hidenori; Yamashita, Hiroshi; Miyamoto, Hisashi; Tanaka, Michinori; Nakaya, Kenji; Kitano, Kazuyoshi; Yamamura, Yoshitaka; Nakamura, Shigeki; Onogawa, Toshiyuki; Mori, Toyoki; Tominaga, Michiaki
Bioorganic and Medicinal Chemistry, 1999 , vol. 7, # 8 p. 1743 - 1754
反应条件
manganese(IV) oxide in dichloromethane 7 h; Reflux;
参考文献
EP2495236 A1, ;
Page/Page column 7 ;
反应条件
caesium acetate; 1,8-diazabicyclo[5.4.0]undec-7-ene; triphenylphosphine; palladium diacetate in N,N-dimethyl-formamide Heating;
参考文献
Torisawa, Yasuhiro; Furuta, Takuya; Nishi, Takao; Aki, Shinji; Minamikawa, Jun-ichi
Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 23 p. 6455 - 6458
反应条件
1: 32 percent / Et3N / CH2Cl2 / 2 h / 20 °C 2: 39 percent / SnCl2*2H2O; conc. HCl / ethanol / 20 °C 3: 53 percent / Et3N / CH2Cl2 / 1.5 h / 20 °C View Scheme
参考文献
Bioorganic and Medicinal Chemistry, , vol. 7, # 8 p. 1743 - 1754
反应条件
1: 32 percent / Et3N / CH2Cl2 / 2 h / 20 °C 2: 39 percent / SnCl2*2H2O; conc. HCl / ethanol / 20 °C 3: 53 percent / Et3N / CH2Cl2 / 1.5 h / 20 °C View Scheme
参考文献
Bioorganic and Medicinal Chemistry, , vol. 7, # 8 p. 1743 - 1754
反应条件
1: 39 percent / SnCl2*2H2O; conc. HCl / ethanol / 20 °C 2: 53 percent / Et3N / CH2Cl2 / 1.5 h / 20 °C View Scheme
参考文献
Bioorganic and Medicinal Chemistry, , vol. 7, # 8 p. 1743 - 1754
反应条件
1.1: 85 percent / pyridine / 20 °C 2.1: 94 percent / K2CO3 / dimethylformamide / 4 h / 120 °C 3.1: t-BuOK / toluene / 0.5 h / Heating 3.2: 60 percent / conc. HCl / acetic acid / 5 h / Heating 4.1: 81 percent / polyphosphoric acid / 1.5 h / 80 - 100 °C 5.1: 32 percent / Et3N / CH2Cl2 / 2 h / 20 °C 6.1: 39 percent / SnCl2*2H2O; conc. HCl / ethanol / 20 °C 7.1: 53 percent / Et3N / CH2Cl2 / 1.5 h / 20 °C View Scheme
参考文献
Bioorganic and Medicinal Chemistry, , vol. 7, # 8 p. 1743 - 1754
反应条件
1.1: 100 percent / K2CO3 / acetone / 0.5 h / Heating 2.1: SnCl2*2H2O; conc. HCl / ethanol / 20 °C 3.1: 85 percent / pyridine / 20 °C 4.1: 94 percent / K2CO3 / dimethylformamide / 4 h / 120 °C 5.1: t-BuOK / toluene / 0.5 h / Heating 5.2: 60 percent / conc. HCl / acetic acid / 5 h / Heating 6.1: 81 percent / polyphosphoric acid / 1.5 h / 80 - 100 °C 7.1: 32 percent / Et3N / CH2Cl2 / 2 h / 20 °C 8.1: 39 percent / SnCl2*2H2O; conc. HCl / ethanol / 20 °C 9.1: 53 percent / Et3N / CH2Cl2 / 1.5 h / 20 °C View Scheme
参考文献
Bioorganic and Medicinal Chemistry, , vol. 7, # 8 p. 1743 - 1754
反应条件
1: SOCl2 2: 32 percent / Et3N / CH2Cl2 / 2 h / 20 °C 3: 39 percent / SnCl2*2H2O; conc. HCl / ethanol / 20 °C 4: 53 percent / Et3N / CH2Cl2 / 1.5 h / 20 °C View Scheme
参考文献
Bioorganic and Medicinal Chemistry, , vol. 7, # 8 p. 1743 - 1754
