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    • 8. 发明授权
    • Process for the preparation of thieno-pyridine derivatives
    • 噻吩并吡啶衍生物的制备方法
    • US4127580A
    • 1978-11-28
    • US775314
    • 1977-03-07
    • Emile Braye
    • Emile Braye
    • C07D333/16C07D333/20C07D495/04C07D283/00
    • C07D495/04C07D333/16C07D333/20
    • This invention relates to a process for the preparation of thieno-pyridine derivatives having the structural formula: ##STR1## in which R.sub.1 represents an optionally substituted alkyl, aryl or aralkyl radical, and R.sub.2 and R.sub.3 represnt each hydrogen or a lower alkyl, aryl or heterocyclic radical, comprising:(a) reacting a derivative of the formula ##STR2## in which R.sub.2 and R.sub.3 are as defined for formula (I) and X represents hydrogen, or an alkali metal, or a radical Mg-Y in which Y represents halogen, with a halo-sulfonyl derivative having the formula:Hal--SO.sub.2 --R.sub.4 (III) in which Hal represents halogen and R.sub.4 represents an optionally substituted alkyl, aryl or aralkyl group, to give a compound having the formula: ##STR3## (b) subsequently reacting the latter compound with an amine of the formula:R.sub.1 --NH.sub.2 (V) in which R.sub.1 is as defined for the formula (I), to give a compound having the formula: ##STR4## and (c) subsequently cyclizing compound (VI) with formaldehyde to give the derivative of the formula (I).
    • 本发明涉及一种具有以下结构式的噻吩并吡啶衍生物的制备方法:其中R 1表示任选取代的烷基,芳基或芳烷基,R 2和R 3表示每个氢或低级烷基 ,芳基或杂环基团,包括: