6-氟-7-氯-8-硝基-1,4-二氢-4-氧代喹啉-3-羧酸乙酯及其N-乙基物的亲核取代 |
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引用本文: | 周伟澄,刘庆,刘进前,张秀平.6-氟-7-氯-8-硝基-1,4-二氢-4-氧代喹啉-3-羧酸乙酯及其N-乙基物的亲核取代[J].中国医药工业杂志,1996(4). |
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作者姓名: | 周伟澄 刘庆 刘进前 张秀平 |
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作者单位: | 国家医药管理局上海医药工业研究院 |
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摘 要: | 6-氟-7-氯-8-硝基-1,4-二氢-4-氧代喹啉-3-羧酸乙酯(1)及其N-乙基物(2)与1-甲基哌嗪反应都形成7-取代的产物;与巯基乙醇反应,1形成7-取代产物,而2形成7,8-二取代产物;2与氟化钾反应得6,8-二氟-7-氯代化合物,而1与氟化钾在相同条件下不起反应。
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关 键 词: | 氟喹诺酮,亲核取代反应 |
NUCLEOPHILIC SUBSTITUTION OF ETHYL 6-FLUORO-7-CHLORO-8-NITRO-1, 4-DIHYDRO-4- OXOQUINOLINE-3-CARBOXYLATE AND ITS N-ETHVLATED PRODUCT |
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Authors: | ZHOU Wei-Cheng LIU Qing LIU Jin-Qian ZHANG Xiu-Ping |
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Abstract: | Both ethyl 6-fluoro-7-chloro-8-nitro-1, 4-dihydro-4-oxoquinoline 3-carboxylate (1) and its N-ethylated product 2 were reacted with 1-methylpi perazine to form the 7-methylpiperazinyl products (4 and 6).In the reaction with 2-mercaptoethanol,1 gave 7-(2-hydroxyethyl)thio-8-nitro compound 5,while 2 gave 7, 8-bis (2-hydroxyethyl) thio compound 7.2 reacted with KF to produce the 6,8-difluoro-7-chloroquinolone 8,but 1 was not changed in the same condition. |
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Keywords: | fluoroquinolone nucleophilic substitution |
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