2’,3’-二脱氧-3’-氟鸟苷合成路线 （共 28 条）
反应条件
1: With lithium hydroxide hydrate; water
T=65°C;
2: With hydrogenchloride in water
T=30 - 35°C; pH=6 - 6.2;
参考文献
MEDIVIR AB; KALAYANOV, Genadiy
Patent: WO2012/115578 A1, 2012 ;
Location in patent: Page/Page column 10-11 ;
反应条件
1: With sodium methylate; 2-hydroxyethanethiol in ethanol
4 h; Reflux;
2: With acetic acid in ethanol; water
T=20°C; 0.5 h;
参考文献
MEDIVIR AB; KALAYANOV, Genadiy
Patent: WO2012/115578 A1, 2012 ;
Location in patent: Page/Page column 11 ;
反应条件
acetic acid
T=80°C; 2 h;
参考文献
Ajinomoto Co., Inc.
Patent: EP1816135 A1, 2007 ;
Location in patent: Page/Page column 30 ;
反应条件
ammonia in methanol
Ambient temperature;
参考文献
Herdewijn; Balzarini; Baba; Pauwels; Van Aerschot; Janssen; De Clerq
Journal of Medicinal Chemistry, 1988 , vol. 31, # 10 p. 2040 - 2048
反应条件
sodium methylate; 2-hydroxyethanethiol in methanol
T=50°C; 48 h;
参考文献
Torii, Takayoshi; Onishi, Tomoyuki; Izawa, Kunisuke; Maruyama, Tokumi; Demizu, Yosuke; Neyts, Johan; De Clercq, Erik
Nucleosides, Nucleotides and Nucleic Acids, 2006 , vol. 25, # 4-6 p. 655 - 665
反应条件
2-hydroxyethanethiol; sodium hydroxide in water
1.5 h; Inert atmosphereRefluxLarge scale reaction;
参考文献
Brodszki, Martin; Baeckstroem, Birthe; Malmgren, Hakan; Wennerberg, Johan; Larsson, Torbjoern; Pelcman, Mikael; Waehling, Horst; Wallberg, Hans; Horvath, Karol
Organic Process Research and Development, 2011 , vol. 15, # 5 p. 1027 - 1032
反应条件
1: 61 percent / Raney Ni / toluene / 14 h / 90 °C
2: 69 percent / aq. AcOH / 2 h / 80 °C
View Scheme
参考文献
Torii, Takayoshi; Onishi, Tomoyuki; Izawa, Kunisuke; Maruyama, Tokumi
Tetrahedron Letters, 2006 , vol. 47, # 34 p. 6139 - 6141
反应条件
1: 91 percent / perfluorobutanesulfonyl fluoride; i-Pr2NEt / ethyl acetate / 20 h / 65 °C
2: 61 percent / Raney Ni / toluene / 14 h / 90 °C
3: 69 percent / aq. AcOH / 2 h / 80 °C
View Scheme
参考文献
Torii, Takayoshi; Onishi, Tomoyuki; Izawa, Kunisuke; Maruyama, Tokumi
Tetrahedron Letters, 2006 , vol. 47, # 34 p. 6139 - 6141
反应条件
1: 60 percent / NEt3 / dimethylformamide / 2 h / 40 °C
2: 91 percent / perfluorobutanesulfonyl fluoride; i-Pr2NEt / ethyl acetate / 20 h / 65 °C
3: 61 percent / Raney Ni / toluene / 14 h / 90 °C
4: 69 percent / aq. AcOH / 2 h / 80 °C
View Scheme
参考文献
Torii, Takayoshi; Onishi, Tomoyuki; Izawa, Kunisuke; Maruyama, Tokumi
Tetrahedron Letters, 2006 , vol. 47, # 34 p. 6139 - 6141
反应条件
PNPase; calcium chloride in water
T=40 - 60°C; 5 h; Enzymatic reaction;
参考文献
Komatsu, Hironori; Araki, Tadashi
Tetrahedron Letters, 2003 , vol. 44, # 14 p. 2899 - 2901
