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
caesium carbonate in dimethyl sulfoxide T=25 - 35°C; 3 h; Product distribution / selectivity;
参考文献
WO2007/125547 A2, ;
Page/Page column 55; 69 ;
反应条件
sodium methylate in tetrahydrofuran T=-15 - 10°C; Product distribution / selectivity;
参考文献
WO2011/132172 A1, ;
Page/Page column 18-19 ;
WO 2011/132172 A1
反应条件
1.1: tetrabutylammomium bromide; hydrogen bromide / toluene; water / 1.5 h / 90 - 95 °C 2.1: sodium hydroxide / water; acetone 3.1: tetrabutylammomium bromide; dihydrogen peroxide / dichloromethane; water / 10 - 20 °C 3.2: 0.5 h / 20 °C 4.1: dichloromethane; water / 2 h / 20 °C 4.2: 0.5 h / Reflux 5.1: sodium t-butanolate / tetrahydrofuran / -20 - -15 °C View Scheme
反应条件
1: sodium hydrogencarbonate / tetrabutylammomium bromide / 1-methyl-pyrrolidin-2-one / 6 h / 130 °C 2: sodium hydrogencarbonate; 3-chloro-benzenecarboperoxoic acid / dichloromethane / 22 h / 20 - 25 °C 3: sodium hexamethyldisilazane / tetrahydrofuran / 2 h / -75 - -10 °C View Scheme
反应条件
1: sodium hydrogencarbonate / tetrabutylammomium bromide / 1-methyl-pyrrolidin-2-one / 6 h / 130 °C 2: sodium hydrogencarbonate; 3-chloro-benzenecarboperoxoic acid / dichloromethane / 22 h / 20 - 25 °C 3: lithium hexamethyldisilazane / tetrahydrofuran / 2.33 h / -75 - -10 °C View Scheme
反应条件
1.1: sodium hydrogencarbonate; sodium hypochlorite; potassium bromide; 4-hydroxy-2,2,6,6-tetramethyl piperidinyloxy, free radical / ethyl acetate; water / 1 h / -10 - 5 °C / Inert atmosphere 2.1: sodium hexamethyldisilazane / tetrahydrofuran / 0.33 h / -78 °C / Inert atmosphere 2.2: 21 h / -35 - 0 °C View Scheme
反应条件
1: ammonium molibdate; tetrabutylammomium bromide; dihydrogen peroxide / dichloromethane / 10 h / 0 - 5 °C 2: sodium methylate / tetrahydrofuran / -15 - 10 °C View Scheme
参考文献
WO2011/132172 A1, ;
WO 2011/132172 A1
反应条件
1.1: N-ethyl-N,N-diisopropylamine / dichloromethane / 0 - 5 °C 1.2: pH 3.5 1.3: 20 °C 2.1: ammonium molibdate; tetrabutylammomium bromide; dihydrogen peroxide / dichloromethane / 10 h / 0 - 5 °C 3.1: sodium methylate / tetrahydrofuran / -15 - 10 °C View Scheme
参考文献
WO2011/132172 A1, ;
WO 2011/132172 A1
反应条件
1.1: sodium hydroxide / water; acetone 2.1: tetrabutylammomium bromide; dihydrogen peroxide / dichloromethane; water / 10 - 20 °C 2.2: 0.5 h / 20 °C 3.1: dichloromethane; water / 2 h / 20 °C 3.2: 0.5 h / Reflux 4.1: sodium t-butanolate / tetrahydrofuran / -20 - -15 °C View Scheme
反应条件
1.1: tetrabutylammomium bromide; dihydrogen peroxide / dichloromethane; water / 10 - 20 °C 1.2: 0.5 h / 20 °C 2.1: dichloromethane; water / 2 h / 20 °C 2.2: 0.5 h / Reflux 3.1: sodium t-butanolate / tetrahydrofuran / -20 - -15 °C View Scheme
