CAS: 113952-21-9; 5-Carbamoyl-10,11-Dihydro-11-Oxo-5H-Dibenzazepine-10-Yl Acetate

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potassium acetate oxcarbazepine [bis(acetoxy)iodo]benzene azepine-5-carboxamidecis-10,11-dihydro-10,11-dihydroxy-5H-dibenzazepine-5-carboxamide azepine-5-carboxamidetrans-10,11-dihydro-10,11-dihydroxy-5H-dibenzazepine-5-carboxamide

📜奥卡西平,碘苯二乙酸置于溶剂黄146体系中,化学反应 16.0H,以27%的收率获得10-乙酰氧基奥卡西平
参考文献:Complementation Of Biotransformations With Chemical C-h Oxidation: Copper-Catalyzed Oxidation Of Tertiary Amines In Complex Pharmaceuticals
标题:Complementation Of Biotransformations With Chemical C-h Oxidation: Copper-Catalyzed Oxidation Of Tertiary Amines In Complex Pharmaceuticals
摘要:The Isolation,Quantitation,And Characterization Of Drug Metabolites In Biological Fluids Remain Challenging. Rapid Access To Oxidized Drugs Could Facilitate Metabolite Identification And Enable Early Pharmacology And Toxicity Studies. Herein,We Compared Biotransformations To Classical And New Chemical C-H Oxidation Methods Using Oxcarbazepine,Naproxen,And An Early Compound Hit (Phthalazine 1). These Studies Illustrated The Low Preparative Efficacy Of Biotransformations And The Inability Of Chemical Methods To Oxidize Complex Pharmaceuticals. We Also Disclose An Aerobic Catalytic Protocole (Cui/air) To Oxidize Tertiary Amines And Benzylic Ch'S In Drugs. The Reaction Tolerates A Broad Range Of Functionalities And Displays A High Level Of Chemoselectivity,Which Is Not Generally Explained By The Strength Of The C-H Bonds But By The Individual Structural Chemotype. This Study Represents A First Step Toward Establishing A Chemical Toolkit (Chemotransformations) That Can Selectively Oxidize C-H Bonds In Complex Pharmaceuticals And Rapidly Deliver Drug Metabolites.
Doi:10.1021/ja405471H