2-(4-氰基苯基)-1 3-二氧戊环合成路线 （共 8 条）
反应条件
toluene-4-sulfonic acid in toluene 18 h; Reflux;
参考文献
Boyer, Nicolas; Gloanec, Philippe; De Nanteuil, Guillaume; Jubault, Philippe; Quirion, Jean-Charles
European Journal of Organic Chemistry, 2008 , # 25 p. 4277 - 4295
反应条件
hydroxylamine hydrochloride; sodium carbonate in ethanol; water T=100°C; 4.5 h;
参考文献
Crestey, Francois; Lebargy, Cyril; Lasne, Marie-Claire; Perrio, Cecile
Synthesis, 2007 , # 21 art. no. Z14607SS, p. 3406 - 3410
反应条件
1: 92 percent / LAH / diethyl ether 2: 80 percent / Et3N / methanol / 2.5 h 3: 97 percent / aq. PTSA / acetone / 20 °C View Scheme
参考文献
Herre, Stephan; Steinle, Wencke; Rueck-Braun, Karola
Synthesis, 2005 , # 19 art. no. C08205SS, p. 3297 - 3300
反应条件
1: With methyl-magnesium chloride in diethyl ether
2: With water; ammonium chloride in diethyl ether
T=0°C;
参考文献
HOLDER, Swen; Zulch, Armin; Bar, Thomas; Maier, Thomas; Zimmermann, Astrid; Beckers, Thomas; Gekeler, Volker; Joshi, Hemant; Munot, Yogesh; Bhise, Umesh; Chavan, Sunil; Shivatare, Sachin; Patel, Sarvesh; Gore, Vikas
Patent: US2009/156604 A1, 2009 ;
Location in patent: Page/Page column 23-24 ;
反应条件
1: With ammonium chloride in diethyl ether
2: With water; ammonium chloride in diethyl ether
T=0°C;
参考文献
BAYER SCHERING PHARMA AKTIENGESELLSCHAFT
Patent: WO2009/21990 A1, 2009 ;
Location in patent: Page/Page column 60 ;
WO 2009/021990 A1
反应条件
1: benzyl bromide With iodine; magnesium in diethyl ether
T=20°C; 1 h; Inert atmosphere;
2: 4-(1,3-dioxacyclopent-2-yl)benzonitrile in diethyl ether
T=0°C; RefluxInert atmosphere;
3: With hydrogenchloride; water in diethyl ether
Cooling with iceInert atmosphere;
参考文献
ABBOTT LABORATORIES; HARRIS, Christopher, M.; HOBSON, Adrian, D.; WILSON, Noel, S.
Patent: WO2010/93704 A1, 2010 ;
Location in patent: Page/Page column 106 ;
WO 2010/093704 A1
反应条件
in tetrahydrofuran
T=0 - 20°C;
参考文献
Bilodeau, Mark T.; Balitza, Adrienne E.; Hoffman, Jacob M.; Manley, Peter J.; Barnett, Stanley F.; Defeo-Jones, Deborah; Haskell, Kathleen; Jones, Raymond E.; Leander, Karen; Robinson, Ronald G.; Smith, Anthony M.; Huber, Hans E.; Hartman, George D.
Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 11 p. 3178 - 3182
反应条件
1: in tetrahydrofuran
T=0 - 20°C; 5 h;
2: With ammonium chloride in tetrahydrofuran
T=0°C; Product distribution / selectivity;
参考文献
MERCK and CO., INC.
Patent: WO2006/135627 A2, 2006 ;
Location in patent: Page/Page column 89 ;
WO 2006/135627 A2
