The present invention relates to certain novel quinolone compounds of the present invention represented by the following formula(l) and novel processes for preparing same.
wherein:
X is a nitrogen atom or a C-Y group wherein Y is a hydrogen, fluorine, chlorine or bromine atom or a methoxy or methyl group;
R1 is a C1 -6 alkyl group optionally substituted with a halogen atom or a hydroxy radical, an alkenyl group, a C3-6 cycloalkyl group, a phenyl group substituted with a halogen atom or a divalent group of -OCH2*CH(CH3)-, -SCH2*CH2-or -SCH2*CH(CH3)- which forms an oxazine or thiazine ring together with the nitrogen atom to which R1 is attached and with X wherein X is C-Y;
R2 is a hydrogen atom, a carboxy protecting group or a pharmaceutically acceptable metal or organic cation;
R3 and R4, which may be the same or different, are a hydrogen atom, a lower alkyl group, an acyl group or a nitrogen protecting group metabolizable in vivo;
Z is a hydrogen or halogen atom, an amino, hydroxy or methyl group; and
n is 1 to 3.
本发明涉及下式(l)所代表的本发明的某些新型
喹诺酮化合物及其新型制备工艺。
其中
X是氮原子或C-Y基团,其中Y是氢、
氟、
氯或
溴原子或甲氧基或甲基;
R1 是任选被卤素原子或羟基取代的 C1 -6 烷基、烯基、C3-6 环烷基、被卤素原子或 -O *CH(
CH3)-、-S *
CH2-或 -S *CH( )-二价基团取代的苯基,该二价基团与 R1 所连接的氮原子和 X 一起形成恶嗪环或
噻嗪环,其中 X 是 C-Y;
R2 是氢原子、羧基保护基团或药学上可接受的
金属或有机阳离子;
R3 和 R4(可以相同或不同)是氢原子、低级烷基、酰基或可在体内代谢的氮保护基团;
Z 是氢原子或卤素原子、
氨基、羟基或甲基;以及
n 为 1 至 3。