异烟酸-N-氧化物置于氯化亚砜,三氯氧磷体系中,化学反应 7.0H,反应生成 2-氯吡啶-4-甲酰氯
参考文献:Vinylogous Carbinolamine Tumor Inhibitors. 24. Synthesis,Chemistry,And Antineoplastic Activity Of .Alpha.-Halopyridinium Salts: Potential Pyridone Prodrugs Of Acylated Vinylogous Carbinolamine Tumor Inhibitors.
标题:Vinylogous Carbinolamine Tumor Inhibitors. 24. Synthesis,Chemistry,And Antineoplastic Activity Of .Alpha.-Halopyridinium Salts: Potential Pyridone Prodrugs Of Acylated Vinylogous Carbinolamine Tumor Inhibitors.
摘要:A Series Of 4-And 5-[2,3-Dihydro-6,7-Bis[[(N-Alkylcarbamoyl)Oxy]Methyl]-1H-Pyrrol Izin-5-Yl]-2-Halopyridinium Iodides Were Synthesized. The Rates Of Hydrolysis Of The Alpha-Halopyridinium Salts To The Corresponding Pyridones,And The Reactivities Of The Carbamate Moieties Were Studied As A Function Of Ph,Buffer Composition,And Ionic Strength. The 4-And 5-Pyrrolizinyl-2-Halopyridinium Iodides And The Corresponding Pyridones Were Evaluated Against P388 Lymphocytic Leukemia In Vivo. The Alpha-Fluoropyridinium Compounds Were Active But The Alpha-Chloro Compounds Were Not. This Activity Was Correlated With The Rates Of Hydrolysis Of The Alpha-Halopyridinium Compounds To The Active Pyridone. Compounds That Were Active In The P388 Screen Were Evaluated In L1210 Leukemia,M5076 Carcinoma,And Mx-1 Mammary Xenograft Assays In Mice.
DOI:10.1021/jm00168A021