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    • 6. 发明授权
    • Antiinflammatory thieno [2,3-c]pyridine derivatives
    • 抗炎噻吩并[2,3-c]吡啶衍生物
    • US4496568A
    • 1985-01-29
    • US487355
    • 1983-04-25
    • Jean-Pierre MaffrandDaniel Frehel
    • Jean-Pierre MaffrandDaniel Frehel
    • C07D513/02A61K31/435A61K31/4365A61P29/00C07D495/04A61K31/44
    • C07D495/04
    • This invention relates to a process for the preparation of antiinflammatory thieno [2,3-c]- and [3,2-c]pyridines having respectively the following formulae: ##STR1## in which R.sub.1 and R.sub.2, which may be the same or different, represent each a hydrogen atom or an alkyl group, and their pharmaceutically acceptable acid addition salts, comprising:(a) condensing a compound of the following formulae (VII) or (VIII), respectively, ##STR2## with a sulfonyl chloride having the formula ClSO.sub.2 R.sub.3, in which R.sub.3 is a lower alkyl radical or a phenyl radical optionally substituted with a halogen atom or a lower alkyl group, within a two-phase solvent system and in the presence of sodium carbonate;(b) oxidizing in a solvent medium the resulting alcohols having respectively the following formula (V) or (VI): ##STR3## (c) treating the resulting ketones, having the following formula (III) or (IV): ##STR4## with a basic agent having the formula RO.sup.- M.sup.+ in which R is a branched- or straight-chain aliphatic alkyl radical and M.sup.+ is an alkali metal cation, within an alcohol solvent having the formula ROH, and at the reflux temperature of the reaction mixture, to give the compounds of the formula (I) or (II), respectively.
    • 本发明涉及分别具有以下分子式的抗炎噻吩并[2,3-c] - 和[3,2-c]吡啶的制备方法:其中R 1和R 2可以相同或不同, 不同的,各自表示氢原子或烷基,以及它们的药学上可接受的酸加成盐,其包括:(a)分别将下式(VII)或(VIII)的化合物与具有 其中R3是低级烷基或任选被卤素原子或低级烷基取代的苯基的式ClSO 2 R 3在两相溶剂体系内和在碳酸钠存在下; (b)在溶剂介质中氧化分别具有下式(Ⅴ)或(Ⅵ)的所得醇:(Ⅵ)(Ⅵ)(c)处理所得酮,具有下式(III )或(IV):其中R是支链或直链脂族烷基,M +是碱金属阳离子,具有式RO-M +的碱性试剂,(IV) 在具有式ROH的醇溶剂中,并在反应混合物的回流温度下分别得到式(I)或(II)的化合物。