7-氟-1,4-二氢-1-[(1S)-1-(羟基甲基)-2-甲基丙基]-6-碘-4-氧代-3-喹啉甲酸乙酯合成路线 （共 7 条）
反应条件
potassium carbonate in DMF (N,N-dimethyl-formamide)
T=20°C; 22 h;
参考文献
SATOH, Motohide; Aramaki, Hisateru; Yamashita, Masaki; Inoue, Masafumi; Kawakami, Hiroshi; Shinkai, Hisashi; Nakamura, Hiroshi; Matsuzaki, Yuji; Wamaki, Shuichi
Patent: US2008/207618 A1, 2008 ;
Location in patent: Page/Page column 33-34 ;
反应条件
potassium carbonate in N,N-dimethyl-formamide
T=20°C; 22 h;
参考文献
CONCERT PHARMACEUTICALS, INC.
Patent: WO2009/35662 A1, 2009 ;
Location in patent: Page/Page column 21-24 ;
反应条件
1: in tetrahydrofuran
T=20 - 50°C; 0.5 - 2 h;
2: With potassium carbonate in DMF (N,N-dimethyl-formamide)
T=60 - 70°C; 1.5 - 2.5 h; Product distribution / selectivity;
参考文献
JAPAN TOBACCO INC.
Patent: WO2005/113508 A1, 2005 ;
Location in patent: Page/Page column 13-14; 19; 24-25; 47 ;
反应条件
in hexane; ethyl acetate
Heating / reflux; Product distribution / selectivity;
参考文献
JAPAN TOBACCO INC.
Patent: WO2005/113508 A1, 2005 ;
Location in patent: Page/Page column 42 ;
反应条件
1: tetrahydrofuran
2: K2CO3 / dimethylformamide / 70 °C
View Scheme
参考文献
Sato, Motohide; Motomura, Takahisa; Aramaki, Hisateru; Matsuda, Takashi; Yamashita, Masaki; Ito, Yoshiharu; Kawakami, Hiroshi; Matsuzaki, Yuji; Watanabe, Wataru; Yamataka, Kazunobu; Ikeda, Satoru; Kodama, Eiichi; Matsuoka, Masao; Shinkai, Hisashi
Journal of Medicinal Chemistry, 2006 , vol. 49, # 5 p. 1506 - 1508
反应条件
1.1: sulfuric acid / dichloromethane / 0.5 h / 0 - 5 °C
1.2: 5 °C
2.1: thionyl chloride / N,N-dimethyl-formamide; toluene / 85 - 90 °C / Inert atmosphere
3.1: N-ethyl-N,N-diisopropylamine / toluene / 4.5 h / 90 - 95 °C
4.1: toluene / 1.5 h / 20 °C / Cooling
5.1: potassium carbonate / N,N-dimethyl-formamide / 20 °C
View Scheme
参考文献
MATRIX LABORATORIES LTD; VELLANKI, Siva, Rama, Prasad; DHAKE, Vilas, Nathu; RAVI, Satyanarayana; NUCHU, Ravi; PULIYALA, Ravindra; SHAIK, Mahaboob, Basha; DATTA, Debashish
Patent: WO2011/4389 A2, 2011 ;
反应条件
1.1: sodium tetrahydroborate / tetrahydrofuran / 0.25 h
1.2: 0 - 20 °C
2.1: toluene / 1.5 h / 20 °C / Cooling
3.1: potassium carbonate / N,N-dimethyl-formamide / 20 °C
View Scheme
参考文献
MATRIX LABORATORIES LTD; VELLANKI, Siva, Rama, Prasad; DHAKE, Vilas, Nathu; RAVI, Satyanarayana; NUCHU, Ravi; PULIYALA, Ravindra; SHAIK, Mahaboob, Basha; DATTA, Debashish
Patent: WO2011/4389 A2, 2011 ;
