6-[(1E)-2-[4-(4-氟苯基)-6-异丙基-2-[甲基(甲磺酰)氨基]-5-嘧啶]乙烯基]-2,2-二甲基-1,3-二氧六环-4-乙酸叔丁酯合成路线 (共 24 条)
反应条件
potassium carbonate in dimethyl sulfoxide T=25 - 75°C; 5 - 7 h;
参考文献
US2005/124639 A1, ;
Page/Page column 8-9; 10 ;
反应条件
1: N-[5-[(diphenylphosphinoyl)-methyl]-4-(4-fluorophenyl)-6-isopropyl-pyrimidindin-2-yl]-N-methyl-methanesulfonamide With sodium hexamethyldisilazane in tetrahydrofuran T=-76 - -74°C; 1.16667 h; 2: tert-butyl 3,5-dideoxy-2,4-O-(1-methylethylidene)-L-erythro-hexuronate in toluene T=-76 - 10°C; 2.08333 h;
参考文献
US2004/49036 A1, ;
Page 3 ;
反应条件
sodium hexamethyldisilazane in tetrahydrofuran T=-75 - -10°C; Julia-Kocienski Olefination; 2 h;
参考文献
WO2012/98048 A1, ;
Page/Page column 18-19 ;
反应条件
N,N-dicyclohexylmethylamine; Pd0(tris(tert-butyl)phosphine)2 in water; N,N-dimethyl-formamide T=50°C; 96 h;
参考文献
US2008/207903 A1, ;
Page/Page column 16 ;
反应条件
lithium hexamethyldisilazane in tetrahydrofuran T=-75 - -10°C; Julia-Kocienski Olefination; 2.33333 h;
参考文献
WO2012/98048 A1, ;
Page/Page column 17-18 ;
反应条件
triethylamine in dichloromethane T=-25 - -20°C; 1 h;
参考文献
WO2009/157014 A2, ;
Page/Page column 37: 48-49 ;
反应条件
1: N-[4-(4-fIuoro-phenyl)-6-isopropyI-5-(pyridine-2-sulfonyImethyl)-pyrimidin-2-yl]-N-methyI-methanesuIfonamide With potassium carbonate in dimethyl sulfoxide T=35 - 40°C; 2: 1,1-Dimethylethyl 6-formyl-2,2-dimethyl-1,3-dioxane-4-acetate in dimethyl sulfoxide T=75 - 80°C; 12 h;
参考文献
WO2010/23678 A1, ;
Page/Page column 18 ;
反应条件
1: N-[5-(3,5-bis-trifluoromethyl-benzenesulfonyl methyl)-4-(4-fluoro-phenyl)-6-isopropyI-pyrimidin-2-yI]-N-methyl-methanesulfonamide With potassium carbonate in dimethyl sulfoxide T=35 - 40°C; 2: 1,1-Dimethylethyl 6-formyl-2,2-dimethyl-1,3-dioxane-4-acetate in dimethyl sulfoxide T=75 - 80°C; 12 h;
参考文献
WO2010/23678 A1, ;
Page/Page column 18; 19 ;
反应条件
1: dimethyl [4-(4-fluorophenyl)-6-isopropyl-2-[methyl (methylsulfonyl) amino]pyrimidine-5-ylmethyl]phosphonate With sodium hexamethyldisilazane in tetrahydrofuran T=-78°C; 0.333333 h; Inert atmosphere; 2: tert-butyl 3,5-dideoxy-2,4-O-(1-methylethylidene)-L-erythro-hexuronate in tetrahydrofuran T=-35 - 0°C; 21 h; Product distribution / selectivity;
参考文献
EP2351762 A1, ;
Page/Page column 11 ;
反应条件
sodium methylate in tetrahydrofuran T=-15 - 10°C; Reagent/catalystTime;
参考文献
US2013/150579 A1, ;
Paragraph 0067 ;