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    • 7. 发明申请
    • AN IMPROVED PROCESS FOR THE PREPARATION OF QUINOLONE DERIVATIVES
    • 改进喹诺酮衍生物的制备方法
    • WO0185692A3
    • 2002-06-06
    • PCT/IN0100042
    • 2001-03-19
    • NATCO PHARMA LTDPULLA REDDY MUDDASANIVENKAIAH CHOWDARY NANNAPANENI
    • PULLA REDDY MUDDASANIVENKAIAH CHOWDARY NANNAPANENI
    • C07C229/34C07D215/56C07C225/16
    • C07C229/34C07C2601/02C07D215/56
    • This invention relates to an improved process for the preparation of quinolone drugs of the formula (I), wherein R=C1-C6 alkyl, C3-C6 cycloalklyl, aryl, substituted aryl, NR R =diarylamino, arylalkylamino, C1-C6-dialkylamino, piprazinyl, N or C alkyl (C1-C6) substituted piperazinyl, morpholino, pyrrolidinyl, substituted pyrrolidinyl, aralkyl, substituted aralkyl etc. Some of the compounds falling within the formula (I) are ciprofloxacin, enrofloxin, pefloxacin, etc. These compounds are useful as antibacterial drugs. The process of the present invention for preparation of compound of formula (I) comprises in enhancing the reactivity of the displaceable halogen (X) in the compound of the formula (II) towards various amines of formula (III) wherein R = as defined for compound of formula (I), R =COOR (R =C1-C6 alkyl, aryl, aralkyl), nitrile a carboxamide (-CONR R , R and R = C1-C6 alkyl, C3-C6 cycloalkyl, aralkyl), X = Cl, Br, F; NR R = as defined above by introducing a nitro group ortho to the displaceable halo group and subsequently removing the nitro group in a conventional manner. The process of the present invention enhances the yield of the compound of the formula (I) and also improves the quality of the prepared compound.
    • 本发明涉及制备式(I)的喹诺酮药物的改进方法,其中R = C 1 -C 6烷基,C 3 -C 6环烷基,芳基,取代的芳基,NR 1 R 2 =二芳基氨基,芳基烷基氨基 C 1 -C 6 - 二烷基氨基,哌嗪基,N或C烷基(C 1 -C 6)取代的哌嗪基,吗啉代,吡咯烷基,取代的吡咯烷基,芳烷基,取代的芳烷基等。属于式(I)的化合物中的一些是环丙沙星,enrofloxin, 这些化合物可用作抗菌药物。 用于制备式(I)化合物的本发明的方法包括提高式(II)化合物中的可置换卤素(X)对式(III)的各种胺的反应性,其中R =如 式(I)化合物,R 3 = COOR 6(R 6 = C 1 -C 6烷基,芳基,芳烷基),腈甲酰胺(-CONR 7 R 8,R 7) 和R 8 = C 1 -C 6烷基,C 3 -C 6环烷基,芳烷基),X = Cl,Br,F; NR 1 R 2 =如上所定义,通过在可置换卤素基团的邻位引入硝基并随后以常规方式除去硝基。 本发明的方法提高了式(I)化合物的产率,并提高了制备的化合物的质量。