2-氨基-4-氯吡咯并[2,3-D]嘧啶合成路线 （共 36 条）
反应条件
N,N-dimethyl-aniline; trichlorophosphate 2 h; reflux;
参考文献
Liebigs Annalen der Chemie, , p. 15 - 19
反应条件
1: 82 percent / EtONa / ethanol / 6 h / Heating 2: 88 percent / 0.2N aq. HCl / 1 h / 20 °C 3: 50 percent / POCl3 / 6 h / Heating View Scheme
参考文献
Russian Journal of Bioorganic Chemistry, , vol. 21, # 11 p. 756 - 761
Bioorganicheskaya Khimiya, , vol. 21, # 11 p. 874 - 880
反应条件
1: 78 percent / 1 N NaOH / methanol / 3 h / Heating 2: 76 percent / benzyltriethylammonium chloride, N,N-dimethylaniline, POCl3 / acetonitrile / 1 h / Heating View Scheme
参考文献
Liebigs Annalen der Chemie, , # 1 p. 137 - 146
反应条件
1: 88 percent / 0.2N aq. HCl / 1 h / 20 °C 2: 50 percent / POCl3 / 6 h / Heating View Scheme
参考文献
Russian Journal of Bioorganic Chemistry, , vol. 21, # 11 p. 756 - 761
Bioorganicheskaya Khimiya, , vol. 21, # 11 p. 874 - 880
反应条件
1: With antimony trichloride in 1,2-dichloro-ethane T=-10°C; 0.0833333 h; 2: With tert.-butylnitrite in 1,2-dichloro-ethane T=-10°C; 3 h;
参考文献
VALEANT RESEARCH and DEVELOPMENT
Patent: WO2006/122003 A2, 2006 ;
Location in patent: Page/Page column 30-31 ;
WO 2006/122003 A2
反应条件
1: 1) sodium hydride (60percent in oil) / 1) acetonitrile, RT, 0.5 h; 2) acetonitrile, RT, 2 h 2: 86 percent / methanol / 1 h / Heating 3: 92 percent / sodium iodide, chlorotrimethylsilane / acetonitrile View Scheme
参考文献
Ramasamy; Imamura; Robins; Revankar
Tetrahedron Letters, 1987 , vol. 28, # 43 p. 5107 - 5110
反应条件
1.1: hydrogenchloride; sodium nitrite / water / 0.25 h / 0 °C 1.2: 2 h / 0 - 80 °C 1.3: pH 8 2.1: N,N-dimethyl-formamide / 2.15 h / 20 °C View Scheme
参考文献
ABBOTT LABORATORIES; ABBOTT LABORATORIES TRADING (SHANGHAI) COMPANY, LTD.; VAN CAMP, Jennifer; XU, Xiangdong; OSUMA, Augustine, Toby; GREGG, Robert; LONGENECKER, Kenton, L.
Patent: WO2012/45195 A1, 2012 ;
WO 2012/045195 A1
反应条件
1: 1) sodium hydride (60percent in oil) / 1) acetonitrile, RT, 0.5 h; 2) acetonitrile, RT, 2 h 2: 91 percent / methanolic ammonia / 12 h / Ambient temperature; pressure bottle View Scheme
参考文献
Ramasamy; Imamura; Robins; Revankar
Journal of Heterocyclic Chemistry, 1988 , vol. 25, # 6 p. 1893 - 1898
反应条件
1: 1) KOH, tris<2-(2-methoxyethoxy)ethyl>amine / 1) MeCN, 10 min, 2) r.t., 20 h 2: 77 percent / 90percent aq. CF3COOH / 1 h / Ambient temperature 3: 76 percent / methanol / 24 h / Ambient temperature View Scheme
参考文献
Seela; Soulimane; Mersmann; Jurgens
Helvetica Chimica Acta, 1990 , vol. 73, # 7 p. 1879 - 1887
反应条件
1: 1) KOH, tris<2-(2-methoxyethoxy)ethyl>amine / 1) MeCN, 10 min, 2) r.t., 20 h 2: 77 percent / 90percent aq. CF3COOH / 1 h / Ambient temperature 3: 61 percent / 2N NaOH / dioxane / 3 h / Heating View Scheme
参考文献
Seela; Soulimane; Mersmann; Jurgens
Helvetica Chimica Acta, 1990 , vol. 73, # 7 p. 1879 - 1887
