5-氯苯并[1,3]二恶茂-4-胺合成路线 （共 5 条）
反应条件
trifluoroacetic acid in dichloromethane T=20°C; 3 h;
参考文献
Ple, Patrick A.; Green, Tim P.; Hennequin, Laurent F.; Curwen, Jon; Fennell, Michael; Allen, Jack; Lambert-Van Der Brempt, Christine; Costello, Gerard
Journal of Medicinal Chemistry, 2004 , vol. 47, # 4 p. 871 - 887
反应条件
1.1: LDA / tetrahydrofuran / 0.5 h / -78 °C 1.2: 84 percent / tetrahydrofuran / -78 - 20 °C 2.1: 81 percent / diphenoxyphosphoryl azide; Et3N / dioxane / 4 h / 100 °C 3.1: 93 percent / TFA / CH2Cl2 / 3 h / 20 °C View Scheme
参考文献
Ple, Patrick A.; Green, Tim P.; Hennequin, Laurent F.; Curwen, Jon; Fennell, Michael; Allen, Jack; Lambert-Van Der Brempt, Christine; Costello, Gerard
Journal of Medicinal Chemistry, 2004 , vol. 47, # 4 p. 871 - 887
反应条件
1: 81 percent / diphenoxyphosphoryl azide; Et3N / dioxane / 4 h / 100 °C 2: 93 percent / TFA / CH2Cl2 / 3 h / 20 °C View Scheme
参考文献
Ple, Patrick A.; Green, Tim P.; Hennequin, Laurent F.; Curwen, Jon; Fennell, Michael; Allen, Jack; Lambert-Van Der Brempt, Christine; Costello, Gerard
Journal of Medicinal Chemistry, 2004 , vol. 47, # 4 p. 871 - 887
反应条件
1: in acetonitrile
T=80°C; 2.5 h;
2: in toluene
3 h; Heating / reflux; Product distribution / selectivity;
参考文献
ASTRAZENECA AB; ASTRAZENECA UK LIMITED
Patent: WO2006/64217 A2, 2006 ;
Location in patent: Page/Page column 56-57 ;
WO 2006/064217 A2
反应条件
1.1: N-ethyl-N,N-diisopropylamine; trichlorophosphate / chlorobenzene / 10.67 h / 95 - 100 °C
2.1: sodium tert-pentoxide / 1-methyl-pyrrolidin-2-one
2.2: 2.5 h / 60 °C
View Scheme
参考文献
Ford, J. Gair; OKearney-Mcmullan, Anne; Pointon, Simon M.; Powell, Lyn; Siedlecki, Paul S.; Purdie, Mark; Withnall, Jane; Frances Wood, Phil OKeefe
Organic Process Research and Development, 2010 , vol. 14, # 5 p. 1088 - 1093
