7,8-二甲氧基-1,3-二氢-2H-3-苯并氮杂卓-2-酮合成路线 （共 13 条）
反应条件
1.1: sodium hydride / N,N-dimethyl-formamide; oil / 1 h / 25 °C
1.2: 50 °C
2.1: hydrogenchloride; water / ethanol / 60 °C
2.2: pH 8
3.1: potassium carbonate / acetonitrile / 4 h / Reflux
4.1: diethylamine; acetonitrile; ethanol / Resolution of racemate; Chiralpak.(R). AD
View Scheme
参考文献
LES LABORATOIRES SERVIER
Patent: US2011/294999 A1, 2011 ;
反应条件
1.1: potassium tert-butylate / N,N-dimethyl-formamide / 25 °C
1.2: 1.5 h / 40 °C
2.1: sodium iodide / acetone / 20 h / 55 - 58 °C
3.1: potassium carbonate / acetone / 3 h / 55 - 58 °C
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参考文献
BIOCON LIMITED; KOTHAKONDA, Kiran Kumar; RAMASAMY, Sivakumar; BANDARU, Sravan Kumar; VENKATA, Srinivas Pullela
Patent: WO2014/20534 A1, 2014 ;
反应条件
1: 1.) potassium tert-butoxide / 1.) DMSO, RT, 30 min, 2.) RT, 30 min
2: 2 h / 90 - 95 °C
3: H2 / Pd/C / acetic acid / 10 h / 3750.3 Torr / Ambient temperature
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参考文献
Reiffen; Eberlein; Muller; Psiorz; Noll; Heider; Lillie; Kobinger; Luger
Journal of Medicinal Chemistry, 1990 , vol. 33, # 5 p. 1496 - 1504
