5’-脱氧-5-氟胞嘧啶核苷合成路线 （共 12 条）
反应条件
potassium carbonate in methanol; N,N-dimethyl-formamide 24 h; Heating / reflux;
参考文献
ANGIOGENE PHARMACEUTICALS LIMITED; THE GRAY LABORATORY CANCER RESEARCH TRUST
Patent: WO2006/32921 A1, 2006 ;
Location in patent: Page/Page column 37-38 ;
反应条件
ammonia in methanol; water T=45 - 55°C; Product distribution / selectivity;
参考文献
MacDonald, Peter Lindsay; Rossetto, Pierluigi; Gallina, Maurizio
Patent: US2009/209754 A1, 2009 ;
Location in patent: Page/Page column 9-10 ;
反应条件
erbium(III) triflate in water T=120°C; 0.5 h; Microwave irradiation;
参考文献
Procopio, Antonio; Gaspari, Marco; Nardi, Monica; Oliverio, Manuela; Romeo, Roberto
Tetrahedron Letters, 2008 , vol. 49, # 12 p. 1961 - 1964
反应条件
ammonia in methanol T=60°C; 10 h;
参考文献
Chinese Chemical Letters, , vol. 21, # 2 p. 163 - 166
反应条件
sodium chloride in acetonitrile T=37°C; 168 h; var. pHs; Product distribution;
参考文献
Chemical and Pharmaceutical Bulletin, , vol. 40, # 9 p. 2568 - 2571
反应条件
1: 5'-Deoxy-5-fluorocytidine With pyridine; thionyl chloride in acetonitrile T=-5 - 0°C; 2: chloroformic acid n-pentyl ester in acetonitrile T=-5 - 20°C;
参考文献
GENERICS [UK] LIMITED; MYLAN INDIA PRIVATE LIMITED; GORE, Vinayak Govind; PATKAR, Laxmikant; BAGUL, Amit; EDAKE, Mahesh
Patent: WO2011/67588 A1, 2011 ;
Location in patent: Page/Page column 41 ;
反应条件
1: 5'-Deoxy-5-fluorocytidine in acetonitrile T=25 - 30°C; 0.25 h; 2: With hydrogenchloride in dichloromethane; acetonitrile 0.5 h; 3: 1-(pentyloxycarbonyl)imidazole in dichloromethane; acetonitrile 5 h; Reflux;
参考文献
GENERICS [UK] LIMITED; MYLAN INDIA PRIVATE LIMITED; GORE, Vinayak Govind; PATKAR, Laxmikant Narahari; BHALERAO, Rahul; HUBLIKAR, Mahesh Gorakhnath; POKHARKAR, Kiran Shivaji
Patent: WO2011/104540 A1, 2011 ;
Location in patent: Page/Page column 19 ;
反应条件
pyridine in tetrahydrofuran 9 - 10 h; Reflux;
参考文献
GENERICS [UK] LIMITED; MYLAN INDIA PRIVATE LIMITED; GORE, Vinayak Govind; PATKAR, Laxmikant Narahari; BHALERAO, Rahul; HUBLIKAR, Mahesh Gorakhnath; POKHARKAR, Kiran Shivaji
Patent: WO2011/104540 A1, 2011 ;
Location in patent: Page/Page column 21 ;
反应条件
pyridine in tetrahydrofuran 9 - 10 h; Reflux;
参考文献
GENERICS [UK] LIMITED; MYLAN INDIA PRIVATE LIMITED; GORE, Vinayak Govind; PATKAR, Laxmikant Narahari; BHALERAO, Rahul; HUBLIKAR, Mahesh Gorakhnath; POKHARKAR, Kiran Shivaji
Patent: WO2011/104540 A1, 2011 ;
Location in patent: Page/Page column 20-21 ;
反应条件
1.1: thionyl chloride / acetonitrile / 0.25 h / -5 - 0 °C 1.2: -5 - 0 °C 1.3: pH 6 - 7 2.1: pyridine / dichloromethane / -5 - 20 °C 3.1: sodium hydroxide; water / methanol / -5 - 0 °C 3.2: pH 4 - 6 View Scheme
参考文献
GENERICS [UK] LIMITED; MYLAN INDIA PRIVATE LIMITED; GORE, Vinayak Govind; PATKAR, Laxmikant; BAGUL, Amit; EDAKE, Mahesh
Patent: WO2011/67588 A1, 2011 ;
