N-(5-氯苯并[d][1,3]二氧代l-4-基)-7-氟-5-((四氢-2H-吡喃-4-基)氧基)喹唑啉-4-胺合成路线 （共 7 条）
反应条件
sodium tert-pentoxide in 1-methyl-pyrrolidin-2-one
T=55°C; 5 h; Large scale reaction;
参考文献
Raw, Steven A.; Taylor, Brian A.; Tomasi, Simone
Organic Process Research and Development, 2011 , vol. 15, # 3 p. 688 - 692
反应条件
1: 5,7-difluoro-N-(5-chloro-1,3-benzodioxol-4-yl)quinazolin-4-amine hydrochloride With sodium tert-pentoxide in 1-methyl-pyrrolidin-2-one
2: 4-hydroxytetrahydro-4H-pyran With sodium tert-pentoxide in 1-methyl-pyrrolidin-2-one
T=60°C; 2.5 h;
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
反应条件
1: 4-hydroxytetrahydro-4H-pyran With potassium tert-butylate in tetrahydrofuran
0.333333 h;
2: 5,7-difluoro-N-(5-chloro-1,3-benzodioxol-4-yl)quinazolin-4-amine hydrochloride in tetrahydrofuran
T=50°C; 4.58333 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 57 ;
WO 2006/064217 A2
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
反应条件
1: 3 h / 44 °C / Large scale reaction
2: sodium tert-pentoxide / 1-methyl-pyrrolidin-2-one / 5 h / 55 °C / Large scale reaction
View Scheme
参考文献
Raw, Steven A.; Taylor, Brian A.; Tomasi, Simone
Organic Process Research and Development, 2011 , vol. 15, # 3 p. 688 - 692
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
