CAS: 40273-47-0; 3-Fluoroisonicotinaldehyde

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3-Fluoro-4-(2-Phenylethenyl)Pyridine置于臭氧,氢气体系中,用54%的收率获得产物3-氟-4-吡啶甲醛
参考文献:Synthesis Of Some Fluorine-Containing Pyridinealdoximes Of Potential Use For The Treatment Of Organophosphorus Nerve-Agent Poisoning
标题:Synthesis Of Some Fluorine-Containing Pyridinealdoximes Of Potential Use For The Treatment Of Organophosphorus Nerve-Agent Poisoning
摘要:Fluoroheterocyclic Aldoximes Were Screened As Therapeutic Agents For The Treatment Of Anticholinesterase Poisoning. 2-Fluoropyridine-3-And-6-Aldoxime,And 3-Fluoropyridine-2-And-4-Aldoxime,Were Synthesised. Attempts To Obtain 3,5,6-Trifluoropyridine-2,4-Bis(Aldoxime) And-2-Aldoxime,However,Proved Unsuccessful. Pentafluorobenzaldoxime Was Prepared By Oximation Of Pentafluorobenzaldehyde. Acid Dissociation Constants (Pk(A)) And Second-Order Rate Constants (K(Ox)-) Of The Fluorinated Pyridinealdoximes Towards Satin Were Measured. 2,3,5,6-Tetrafluoropyridine-4-Aldoxime Had The Best Profile: Its K(Ox)-Approached That Of The Therapeutic Oxime P2S (310 Vs. 120 L Mol(-1) Min(-1)),But Its Higher Pk(A) (9.1 Vs. 7.8) Fell Short Of The Target Figure Of 8 Required For Reactivation Of Inhibited Acetylcholinesterase In Vivo. N-Alkylation Of The Fluorinated Pyridine-Aldoximes May Reduce Their Pk(A) Nearer To 8 And Enhance Their Therapeutic Potential. Crown Copyright (C) 2011 Published By Elsevier B.V. All Rights Reserved.
DOI:10.1016/j.Jfluchem.2011.05.028

专利信息

专利号:US-8536164-B2
优先权日:2010-12-20
标 题:Fused pyridine compounds as casein kinase inhibitors
发明人：BUTLER TODD W; CHANDRASEKARAN RAMALAKSHMI Y; MENTE SCOT R; SUBRAMANYAM CHAKRAPANI; WAGER TRAVIS T
权利人:BUTLER TODD W; CHANDRASEKARAN RAMALAKSHMI Y; MENTE SCOT R; SUBRAMANYAM CHAKRAPANI; WAGER TRAVIS T; PFIZER
摘要:Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I: n nand pharmaceutically acceptable salts thereof, wherein X, Y, A, R 4 , n, and R 7 are as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.