4-氯吡咯并[2,3-D]嘧啶合成路线 (共 17 条)
反应条件
trichlorophosphate 1 h; Refluxneat (no solvent);
参考文献
Organic Process Research and Development, , vol. 13, # 5 p. 928 - 932
反应条件
1: ethanol / 16 h / Reflux 2: trichlorophosphate / 1 h / Reflux View Scheme
反应条件
1: sodium ethanolate / ethanol / 72 h / 20 °C 2: ethanol / 16 h / Reflux 3: trichlorophosphate / 1 h / Reflux View Scheme
反应条件
1.1: potassium hydroxide / 40 h / Reflux 1.2: 20 °C / pH 6.5 - 7.5 2.1: trichlorophosphate / Reflux View Scheme
参考文献
WO2012/93809 A2, ;
WO 2012/093809 A2
参考文献
Kamath, Vivekanand P.; Juarez-Brambila, Jesus J.; Morris, Christopher B.; Winslow, Christopher D.; Morris Jr., Philip E.
Organic Process Research and Development, 2009 , vol. 13, # 5 p. 928 - 932
反应条件
1: NaH / tetrahydrofuran / 1 h / 20 °C 2: NaH / tetrahydrofuran / 1 h 3: 6.83 g / NBS / methanol; tetrahydrofuran View Scheme
参考文献
BIOCRYST PHARMACEUTICALS, INC.; BABU, Yarlagadda, S.; KOTIAN, Pravin, L.; BANTIA, Shanta; WU, Minwan; KUMAR, V., Satish
Patent: WO2014/78778 A2, 2014 ;
反应条件
N-bromosuccinmide in tetrahydrofuran T=20°C; Inert atmosphere;
参考文献
Khoje, Abhijit Datta; Kulendrn, Aisvareya; Charnock, Colin; Wan, Baojie; Franzblau, Scott; Gundersen, Lise-Lotte
Bioorganic and Medicinal Chemistry, 2010 , vol. 18, # 20 p. 7274 - 7282
反应条件
ammonium hydroxide in 1,4-dioxane T=160°C; 20 h;
参考文献
Goeminne, Annelies; Berg, Maya; McNaughton, Michael; Bal, Gunther; Surpateanu, Georgiana; Van der Veken, Pieter; Prol, Stijn De; Versees, Wim; Steyaert, Jan; Haemers, Achiel; Augustyns, Koen
Bioorganic and Medicinal Chemistry, 2008 , vol. 16, # 14 p. 6752 - 6763
参考文献
Sizova, O. S.; Britikova, N. E.; Novitskii, K. Yu.; Shcherbakova, L. I.; Pershin, G. N.; et al.
Pharmaceutical Chemistry Journal, 1982 , vol. 16, # 11 p. 834 - 838
Khimiko-Farmatsevticheskii Zhurnal, 1982 , vol. 16, # 11 p. 1338 - 1343
反应条件
caesium carbonate in N,N-dimethyl-formamide
T=20°C; 18 h;
参考文献
TAKEDA PHARMACEUTICAL COMPANY LIMITED
Patent: WO2007/4749 A1, 2007 ;
Location in patent: Page/Page column 112-113 ;
WO 2007/004749 A1