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    • 2. 发明授权
    • Process for the preparation of benzo(a)quinolizidine derivatives
    • 苯并(a)喹嗪衍生物的制备方法
    • US4102886A
    • 1978-07-25
    • US624470
    • 1975-10-21
    • Csaba SzantayLajos SzaboLaszlo TokeIstvan TothSandor ViragErzsebet KanyoAgoston David
    • Csaba SzantayLajos SzaboLaszlo TokeIstvan TothSandor ViragErzsebet KanyoAgoston David
    • C07D455/06C07D491/056C07D491/14
    • C07D491/14C07D455/06
    • A process for the preparation of a compound of the formula I or a salt thereof ##STR1## wherein R.sup.1 and R.sup.2 each represent hydrogen or a C.sub.1-4 alkoxy group, or together form a methylenedioxy group;R.sup.3, r.sup.4, r.sup.5 and R.sup.6 are the same or different and are hydrogen or a group of the formula --CH.sub.2 --(CH.sub.2).sub.n --R.sup.7 with the proviso that at least one of the members R.sup.3, R.sup.4, R.sup.5 and R.sup.6 is other than hydrogen; R.sup.7 is carboxyl or a carboxylic acid derivative group;N = 0.1 or 2 which comprises reacting a compound of the formula II ##STR2## with an organic secondary amine and reacting the N-amine of the formula III ##STR3## thus obtained wherein R.sup.8 and R.sup.9 each represent a C.sub.1-5 alkyl group, or together with the adjacent nitrogen atom form a 5- or 6-membered heterocyclic ring which can contain a further heteroatom, with a compound of the formula IVch.sub.2 .dbd. ch -- (ch.sub.2).sub.n -- R.sup.10 (IV)wherein R.sup.10 is a cyano or alkoxycarbonyl group.
    • 一种制备式I化合物或其盐的方法,其中R 1和R 2各自代表氢或C 1-4烷氧基,或一起形成亚甲二氧基; R 3,R 4,R 5和R 6相同或不同,为氢或式-CH 2 - (CH 2)n -R 7的基团,条件是至少有一个R 3,R 4,R 5和R 6不是 氢; R7是羧基或羧酸衍生物基团; N = 0.1或2,其包含用有机仲胺反应式II化合物,并使由此得到的式III的N-胺反应,其中R 8和R 9各自表示C 1-5烷基, 或者与相邻的氮原子一起形成可以含有另外的杂原子的5或6元杂环与式IV的化合物CH2 = CH-(CH2)n-R10(IV),其中R10是氰基或 烷氧基羰基。