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Method for preparing Derivatives of 1.6 - naftiridina useful as CARDIOTONIC,Chemical Intermediates for the preparation of starting materials involved in the proceidimiento to prepare Derivatives of 1.6 - naftiridina.
Method for preparing Derivatives of 1.6 - naftiridina useful as CARDIOTONIC,Chemical Intermediates for the preparation of starting materials involved in the proceidimiento to prepare Derivatives of 1.6 - naftiridina.
4-R min -5-Q-1,6-naphthyridin-2(1H)-ones (1), where R min is hydrogen or methyl and Q is hydroxymethyl, 1-hydroxyethyl alkanoyloxymethyl or 1-alkanoyloxyethyl, are produced by first reacting 4-R min -5-acetyl (or n-propanoyl)-6[2-(dilower-alkylamino]-2(1H)-pyridinone (III) with hydroxylamine or salt thereof to produce 4-R min -5-Q min -1,6-naphthyridin-2(1H)-one-6-oxide (II), where R min is defined as above and Q min is methyl or ethyl; next reacting II with an alkanoic anhydride to produce I where Q is alkanoyloxymethyl or 1-alkanoyloxyethyl; and, then hydrolyzing said alkanoyloxymethyl or -ethyl compound to produce I where Q is hydroxymethyl or 1-hydroxyethyl. Also shown is the cardiotonic use of II and I where Q is hydroxymethyl, 1-hydroxyethyl or alkanoyloxymethyl.
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机译:首先制备4-R min -5-Q-1,6-萘啶-2(1H)-(1),其中R min为氢或甲基,Q为羟甲基,生成1-羟乙基烷酰氧基甲基或1-烷酰氧基乙基。使4-R min -5-乙酰基(或正丙酰基)-6 [2-(二低级烷基氨基)-2(1H)-吡啶酮(III)与羟胺或其盐反应生成4-R min -5-Q min -1,6-萘啶-2(1H)-一6-氧化物(II),其中R min如上定义,Q min为甲基或乙基;然后将II与链烷酸酐反应生成I,其中Q为烷氧基氧基甲基或1-烷氧基氧基乙基;然后水解所述链烷氧基氧基甲基或-乙基化合物以产生I,其中Q为羟甲基或1-羟乙基;还显示II和I的强心用法,其中Q为羟甲基,1-羟乙基或烷酰氧基甲基。
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