(E)-1-[(1S)-1-(4-氟苯基)乙基]-3-[3-甲氧基-4-(4-甲基-1H-咪唑-1-基)亚苄基]哌啶-2-酮合成路线 (共 10 条)
反应条件
sodium t-butanolate in toluene T=-13°C; 2.61667 h; Product distribution / selectivity;
参考文献
Eisai RandD Management Co., Ltd.
Patent: EP1950211 A1, 2008 ;
Location in patent: Page/Page column 64 ;
反应条件
1: With p-methylbenzenesulfonyl (tosylate); p-toluenesulfonic acid sodium salt in toluene T=100°C; 36 h; 2: With sodium hydroxide; water in tetrahydrofuran; toluene T=20°C; 0.05 h; Product distribution / selectivity;
参考文献
Eisai RandD Management Co., Ltd.
Patent: EP1950211 A1, 2008 ;
Location in patent: Page/Page column 64 ;
反应条件
sodium hydride in N,N-dimethyl-formamide T=0 - 20°C;
参考文献
EP1953151 A1, ;
Page/Page column 13 ;
反应条件
1: With sodium tetrahydroborate in isopropyl alcohol T=20°C; 12 h; 2: With water in isopropyl alcohol; toluene Product distribution / selectivity;
参考文献
Eisai RandD Management Co., Ltd.
Patent: EP1950211 A1, 2008 ;
Location in patent: Page/Page column 62 ;
反应条件
1: 1-[(S)-1-(4-fluorophenyl)ethyl]piperidin-2-one With n-butyllithium; diisopropylamine in tetrahydrofuran; cyclohexane; toluene T=-20°C; 1.76667 - 148 h; 2: 3-methoxy-4-(4-methyl-1H-imidazol-1-yl)benzaldehyde in tetrahydrofuran; cyclohexane; toluene T=-20°C; 1.66667 - 2.66667 h; 3: With acetic anhydride; sodium t-butanolate Product distribution / selectivity; more than 3 stages;
参考文献
Eisai RandD Management Co., Ltd.
Patent: US2008/306272 A1, 2008 ;
Location in patent: Page/Page column 8; 9 ;
反应条件
1: 1-[(S)-1-(4-fluorophenyl)ethyl]piperidin-2-one With lithium diisopropyl amide in tetrahydrofuran; cyclohexane T=-70°C; 1 h; 2: diethyl chlorophosphate in tetrahydrofuran; cyclohexane T=-70°C; 1 h; 3: 3-methoxy-4-(4-methyl-1H-imidazol-1-yl)benzaldehyde With lithium diisopropyl amide Product distribution / selectivity; more than 3 stages;
参考文献
Eisai RandD Management Co., Ltd.
Patent: EP1950211 A1, 2008 ;
Location in patent: Page/Page column 60 ;
反应条件
sodium methylate in tetrahydrofuran; methanol T=0 - 20°C; 0.583333 h; Product distribution / selectivity;
参考文献
EP1950211 A1, ;
Page/Page column 52-53 ;
反应条件
lithium hydroxide in tetrahydrofuran; ethanol T=20°C; 18 h; Product distribution / selectivity;
参考文献
EP1950211 A1, ;
Page/Page column 56-57 ;
反应条件
triethylamine in ethanol T=50 - 70°C; 23 h; Product distribution / selectivity;
参考文献
EP1950211 A1, ;
Page/Page column 61 ;
反应条件
piperidine; pyridine T=65°C; 20 - 25 h; Product distribution / selectivity;
参考文献
EP1950211 A1, ;
Page/Page column 58-59 ;