4-[(5-溴-2-吡啶)甲基]-吗啉合成路线 （共 6 条）
反应条件
1: With sodium tris(acetoxy)borohydride; acetic acid in anhydrous dichloroethane T=20°C; 0.5 h; 2: With sodium hydrogencarbonate in anhydrous dichloroethane
参考文献
LOCUS PHARMACEUTICALS, INC.
Patent: US2010/41642 A1, 2010 ;
Location in patent: Page/Page column 21 ;
反应条件
1: With acetic acid in dichloromethane 0.5 h; 2: With sodium tris(acetoxy)borohydride in dichloromethane T=20°C; 4 h;
参考文献
PROLYSIS LTD
Patent: WO2009/74812 A1, 2009 ;
Location in patent: Page/Page column 77 ;
WO 2009/074812 A1
反应条件
hydrogenchloride; sodium hydroxide; ammonium chloride; trifluoroacetic anhydride in n-heptane; dichloromethane
参考文献
Boehringer Ingelheim Pharmaceuticals, Inc.
Patent: US6822093 B2, 2004 ;
参考文献
Boehringer Ingelheim Pharmaceuticals, Inc.
Patent: US6822093 B2, 2004 ;
反应条件
1: With potassium acetate in 1,4-dioxane 0.25 h; 2: With tri-cyclo-hexyl-phosphine; tris-(dibenzylideneacetone)dipalladium(0) in 1,4-dioxane T=80°C; 8.25 h;
参考文献
PROLYSIS LTD
Patent: WO2009/74812 A1, 2009 ;
Location in patent: Page/Page column 78 ;
WO 2009/074812 A1
反应条件
1: 4-[(5-bromo-2-pyridinyl)-methyl]morpholine; lithium dibutyl(isopropyl)magnesate in tetrahydrofuran; hexanes
T=-20°C; 1 h;
2: boric acid trimethyl ester in tetrahydrofuran; hexanes
T=-18 - 20°C; 1 h;
参考文献
BOEHRINGER INGELHEIM INTERNATIONAL GMBH; BOEHRINGER INGELHEIM PHARMA GMBH and CO. KG
Patent: WO2007/44490 A2, 2007 ;
Location in patent: Page/Page column 16-17 ;
