(3R,7aS)-7A-甲基-3-(三氯甲基)-3,5,6,7-四氢吡咯并[1,2-c]恶唑-1-酮合成路线 （共 5 条）
反应条件
1: (3R,7aS)-3-(trichloromethyl)tetrahydropyrrolo[1,2-c]oxazol-1(3H)-one With lithium diisopropyl amide in tetrahydrofuran T=-78°C; 2 h; 2: methyl iodide in tetrahydrofuran T=-78 - 20°C; 4 h;
参考文献
Su, Bo; Deng, Meng; Wang, Qingmin
European Journal of Organic Chemistry, 2013 , # 10 p. 1979 - 1985
反应条件
1: (3R,7aS)-3-(trichloromethyl)tetrahydropyrrolo[1,2-c]oxazol-1(3H)-one With n-butyllithium; N-ethyl-N,N-diisopropylamine in tetrahydrofuran T=-78 - 0°C; 0.833333 h; 2: methyl iodide in tetrahydrofuran T=-50 - 20°C; 2.08333 h;
参考文献
NEUREN PHARMACEUTICALS LIMITED; NEUREN PHARMACEUTICALS INC.
Patent: WO2006/127702 A2, 2006 ;
Location in patent: Page/Page column 30 ;
反应条件
1.1: 77 percent / CHCl3 / 6 h / Heating 2.1: n-butyllithium; diisopropylamine / tetrahydrofuran / 0.83 h / -78 °C 2.2: 63 percent / tetrahydrofuran / 2 h / -78 - -50 °C View Scheme
参考文献
Su, Bo; Deng, Meng; Wang, Qingmin
European Journal of Organic Chemistry, 2013 , # 10 p. 1979 - 1985
反应条件
hydrogenchloride T=20°C;
参考文献
Tong, Sok-Teng; Harris, Paul W. R.; Barker, David; Brimble, Margaret A.
European Journal of Organic Chemistry, 2008 , # 1 p. 164 - 170
反应条件
1: 100 percent / thionyl chloride / 3 h / Heating
2: 92 percent / triethylamine; bis(2-oxo-3-oxazolidinyl)phosphinic chloride / CH2Cl2 / 20.5 h / 20 °C
3: 90 percent / aqueous sodium hydroxide / dioxane / 19 h / 20 °C
View Scheme
参考文献
Harris, Paul W.R.; Brimble, Margaret A.; Muir, Victoria J.; Lai, Michelle Y.H.; Trotter, Nicholas S.; Callis, David J.
Tetrahedron, 2005 , vol. 61, # 42 p. 10018 - 10035
