5-(4-氯苯在)噻吩-2-羧酸合成路线 （共 17 条）
反应条件
1: 71 percent / 5percent NaOH / 0.5 h / 80 °C 2: 30percent H2O2 / pyridine / 5 h 3: 80 percent / iodine / dioxane / 24 h / 80 °C View Scheme
参考文献
Campaigne, E.; White, R.L.
Journal of Heterocyclic Chemistry, 1988 , vol. 25, p. 367 - 373
反应条件
alkaline aqueous sodium hypobromite solution
参考文献
Buu-Hoi; Hoan
Recueil des Travaux Chimiques des Pays-Bas, 1950 , vol. 69, p. 1455,1466
反应条件
1: aqueous hydrochloric acid; sodium nitrite; aq. NaOH solution 2: aluminium chloride; carbon disulfide 3: alkaline aqueous sodium hypobromite solution View Scheme
参考文献
Buu-Hoi; Hoan
Recueil des Travaux Chimiques des Pays-Bas, 1950 , vol. 69, p. 1455,1466
反应条件
sulfuric acid in toluene
7 h; Heating;
参考文献
Noguchi, Toshiya; Hasegawa, Masahiro; Tomisawa, Kazuyuki; Mitsukuchi, Morihiro
Bioorganic and Medicinal Chemistry, 2003 , vol. 11, # 22 p. 4729 - 4742
反应条件
1: 86 percent / H2SO4 / toluene / 7 h / Heating
2: LiAlH4 / diethyl ether / Heating
3: HMPA; thionyl chloride / tetrahydrofuran / 20 °C
4: 18-crown-6 / acetonitrile / 20 °C
5: KOH / ethanol; H2O / Heating
6: 67 percent / H2SO4 / Heating
View Scheme
参考文献
Noguchi, Toshiya; Hasegawa, Masahiro; Tomisawa, Kazuyuki; Mitsukuchi, Morihiro
Bioorganic and Medicinal Chemistry, 2003 , vol. 11, # 22 p. 4729 - 4742
反应条件
1: 5-(4-chloro-phenyl)-thiophene-2-carboxylic acid With n-butyllithium in tetrahydrofuran; hexane
T=-78 - 0°C; 5 h;
2: methanol With hydrogenchloride; hydrazine
48 h; Heating / reflux;
参考文献
Bristol-Myers Squibb Company
Patent: US2008/269110 A1, 2008 ;
Location in patent: Page/Page column 18-19 ;
US 20080269110 A1
反应条件
1: 5-(4-chloro-phenyl)-thiophene-2-carboxylic acid With n-butyllithium in tetrahydrofuran; hexane
T=-78 - 0°C; 4 h;
2: N,N-dimethyl-formamide in tetrahydrofuran; hexane
T=-70 - -10°C; 2 h;
3: With hydrogenchloride; water in tetrahydrofuran; hexane
T=-30 - 20°C;
参考文献
ASTRAZENECA AB
Patent: WO2007/11284 A1, 2007 ;
Location in patent: Page/Page column 31-32 ;
WO 2007/011284 A1
