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    • 2. 发明申请
    • PROCESS FOR THE PREPARATION OF METHYL-QUINOLINE DERIVATIVES
    • 制备甲基喹啉衍生物的方法
    • WO1991001314A1
    • 1991-02-07
    • PCT/HU1990000049
    • 1990-07-20
    • ALKALOIDA VEGYÉSZETI GYARSALAMON, ZoltánJEKO, JózsefIMRE, IlonaCZELLÉR, Magdolna
    • ALKALOIDA VEGYÉSZETI GYAR
    • C07D401/06
    • C07D401/06
    • The present invention relates to a process for the preparation of methyl-quinoline derivatives of general formula (I), or salts thereof, wherein X stands for hydrogen or a non-binding electron pair, R stands for hydrogen or a group of general formula (II), R stands for acyloxy or hydroxyl and the dotted line is an optionally aromatic ring. The invention is carried out by rearranging an N-oxide derivative of general formula (III), wherein R is as given above - with an organic carboxylic acid derivative containing halogen, preferably a halogen substituted aliphatic or aromatic carboxylic acid anhydride or carboxylic acid halide containing 1 to 8 carbon atoms, and reducing the obtained ester of general formula (IV), wherein R is as given above, and Ac stands for acyl - after or before the solvolysis of the ester group.
    • 本发明涉及制备通式(I)的甲基 - 喹啉衍生物或其盐的方法,其中X 1代表氢或非结合电子对,R 1代表氢或 通式(II)的基团,R 2代表酰氧基或羟基,虚线是任选的芳香环。 本发明通过将含有卤素的有机羧酸衍生物,优选卤素取代的脂肪族或芳族羧酸酐或羧酸的羧酸衍生物重新排列其中R 1如上所定义的通式(III)的N-氧化物衍生物 含有1至8个碳原子的酰卤,并且将所得的通式(Ⅳ)的酯还原,其中R 1如上所定义,并且Ac代表酰基 - 在酯基溶剂分解之后或之前。