2,4,5-三氟苯甲酰乙酸乙酯合成路线 （共 34 条）
反应条件
1: propanedioic acid monoethyl ester With n-butyllithium; triphenylemethane in tetrahydrofuran Metallation; 2: 2,4,5-Trifluorobenzoyl chloride in tetrahydrofuran T=20°C; Acetylation; 1 h;
参考文献
Jung, Michael E.; Yang, Eric C.; Vu, Binh T.; Kiankarimi, Mehrak; Spyrou, Emmanouil; Kaunitz, Jon
Journal of Medicinal Chemistry, 1999 , vol. 42, # 19 p. 3899 - 3909
反应条件
1: With zinc(II) chloride in 1,2-dichloro-ethane Heating / reflux; 2: With hydrogenchloride; water in 1,2-dichloro-ethane T=90°C; 1 h;
参考文献
LG LIFE SCIENCES LTD.
Patent: WO2007/64077 A1, 2007 ;
Location in patent: Page/Page column 8 ;
反应条件
1: malonic acid ethyl ester monopotassium salt With triethylamine; magnesium chloride in acetonitrile T=20°C; Transmetallation; 2.5 h; 2: 2,4,5-Trifluorobenzoyl chloride With triethylamine in acetonitrile T=20°C; Acylation; Decarboxylation; 16 h;
参考文献
Hay, Alastair M.; Hobbs-Dewitt, Sheila; MacDonald, Alasdair A.; Ramage, Robert
Synthesis, 1999 , # 11 p. 1979 - 1985
反应条件
1: diethylmalonate potassium salt With triethylamine; magnesium chloride in acetonitrile T=20 - 25°C; 2.5 h; 2: 2,4,5-Trifluorobenzoyl chloride With triethylamine in acetonitrile T=20°C; 18 h;
参考文献
Baker, William R.; Cai, Shaopei; Dimitroff, Martin; Fang, Liming; Huh, Kay K.; Ryckman, David R.; Shang, Xiao; Shawar, Ribhi M.; Therrien, Joseph H.
Journal of Medicinal Chemistry, 2004 , vol. 47, # 19 p. 4693 - 4709
反应条件
1: malonic acid ethyl ester monopotassium salt With magnesium chloride in tetrahydrofuran; toluene T=0°C; 2: With triethylamine in tetrahydrofuran; toluene T=0 - 50°C; 1 - 5 h; 3: 2,4,5-Trifluorobenzoyl chloride With hydrogenchloride more than 3 stages;
参考文献
WO2006/15194 A2, ;
Page/Page column 15 ;
反应条件
hydrogenchloride; ammonia in tetrahydrofuran
反应条件
1.1: tetrahydrofuran / 2 h / 60 °C 2.1: MeMgBr / tetrahydrofuran; diethyl ether / 0.33 h 2.2: tetrahydrofuran; diethyl ether / 60 °C 2.3: aq. HCl / tetrahydrofuran; diethyl ether / pH 5 - 6 View Scheme
参考文献
Journal of Medicinal Chemistry, , vol. 45, # 25 p. 5564 - 5575
反应条件
1: propanedioic acid monoethyl ester With methylmagnesium bromide in tetrahydrofuran; diethyl ether 0.333333 h; 2: imidazol-1-yl-(2,4,5-trifluoro-phenyl)-methanone in tetrahydrofuran; diethyl ether T=60°C; 3: With hydrogenchloride in tetrahydrofuran; diethyl ether pH=5 - 6; Further stages.;
参考文献
Journal of Medicinal Chemistry, , vol. 45, # 25 p. 5564 - 5575
反应条件
sodium hydride T=20°C;
参考文献
Chepyala, Naveenkumar R.; Durgi, Rajashaker R.; Tatini, Lakshmi K.; Subbaraju, Gottumukkala V.; Hindupur, Rama M.; Dhanvada, Muralimohan R.
Letters in Organic Chemistry, 2011 , vol. 8, # 9 p. 637 - 643
