BTZ 043;2-[(2S)-2-甲基-1,4-二氧杂-8-氮杂螺[4.5]癸烷-8-基]-8-硝基-6-三氟甲基-4H-1,3-苯并噻嗪-4-酮合成路线 (共 5 条)
反应条件
in ethanol T=50 - 60°C; 0.333333 h;
参考文献
Makarov Vadim A.
Patent: EP2380886 A1, 2011 ;
Location in patent: Page/Page column 8 ;
反应条件
1: potassium ethylxanthate; 2-chloro-3-nitro-5-(trifluoromethyl)benzamide in ethanol T=20°C; 24 h; 2: (S)-2-methyl-1,4-dioxa-8-azaspiro[4.5]decane in acetic acid 24 h; Reflux;
参考文献
Makarov Vadim A.
Patent: EP2380886 A1, 2011 ;
Location in patent: Page/Page column 11 ;
反应条件
acetic acid in ethanol 24 h; Reflux;
参考文献
MAKAROV, Vadim, A.
Patent: WO2011/132070 A1, 2011 ;
Location in patent: Page/Page column 19 ;
反应条件
1: (S)-(+)-propylene glycol With trimethylsilyl trifluoromethanesulfonate; N-ethyl-N,N-diisopropylamine in dichloromethane T=20°C; 0.25 h; Inert atmosphere; 2: 8-nitro-2-(4-oxopiperidin-1-yl)-6-(trifluoromethyl)-4H-benzo[e][1,3]thiazin-4-one in dichloromethane 0.333333 h; Inert atmosphere;
参考文献
Karoli, Tomislav; Becker, Bernd; Zuegg, Johannes; Moellmann, Ute; Ramu, Soumya; Huang, Johnny X.; Cooper, Matthew A.
Journal of Medicinal Chemistry, 2012 , vol. 55, # 17 p. 7940 - 7944
反应条件
1.1: N-ethyl-N,N-diisopropylamine / water; ethanol / 0.67 h / 60 °C 2.1: trimethylsilyl trifluoromethanesulfonate; N-ethyl-N,N-diisopropylamine / dichloromethane / 0.25 h / 20 °C / |Inert atmosphere 2.2: 0.33 h / |Inert atmosphere View Scheme
参考文献
Karoli, Tomislav; Becker, Bernd; Zuegg, Johannes; Moellmann, Ute; Ramu, Soumya; Huang, Johnny X.; Cooper, Matthew A.
Journal of Medicinal Chemistry, 2012 , vol. 55, # 17 p. 7940 - 7944