{"title":"一种合成喹诺酮类抗生素的新方法","authors":"A. Jackson, O. Meth–Cohn","doi":"10.1039/C39950001319","DOIUrl":null,"url":null,"abstract":"A simple protocol for the synthesis of quinolone antibiotics is exemplified for the synthesis of norfloxacin; 3-chloro-4-fluoroaniline with triethyl orthoformate is transformed into its N-ethyl-N-formyl derivative which reacts with methyl malonyl morpholide and phosphoryl chloride at 100 °C to give 6-fluoro-7-chloro-1-ethylquinol-4-one-3-carboxylic acid, which has previously been converted into norfloxacin by the action of piperazine.","PeriodicalId":17282,"journal":{"name":"Journal of The Chemical Society, Chemical Communications","volume":"23 1","pages":"1319-1319"},"PeriodicalIF":0.0000,"publicationDate":"1995-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"110","resultStr":"{\"title\":\"A new short and efficient strategy for the synthesis of quinolone antibiotics\",\"authors\":\"A. Jackson, O. Meth–Cohn\",\"doi\":\"10.1039/C39950001319\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"A simple protocol for the synthesis of quinolone antibiotics is exemplified for the synthesis of norfloxacin; 3-chloro-4-fluoroaniline with triethyl orthoformate is transformed into its N-ethyl-N-formyl derivative which reacts with methyl malonyl morpholide and phosphoryl chloride at 100 °C to give 6-fluoro-7-chloro-1-ethylquinol-4-one-3-carboxylic acid, which has previously been converted into norfloxacin by the action of piperazine.\",\"PeriodicalId\":17282,\"journal\":{\"name\":\"Journal of The Chemical Society, Chemical Communications\",\"volume\":\"23 1\",\"pages\":\"1319-1319\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"1995-01-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"110\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Journal of The Chemical Society, Chemical Communications\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.1039/C39950001319\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"\",\"JCRName\":\"\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Journal of The Chemical Society, Chemical Communications","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.1039/C39950001319","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
引用次数: 110
摘要
举例说明了合成诺氟沙星的喹诺酮类抗生素的简单方案;3-氯-4-氟苯胺与原甲酸三乙酯转化为其n -乙基- n -甲酰基衍生物，该衍生物与丙二酰甲酯和氯磷酰在100℃下反应得到6-氟-7-氯-1-乙基喹啉-4- 1- 3-羧酸，该羧酸先前通过哌嗪的作用转化为诺氟沙星。
A new short and efficient strategy for the synthesis of quinolone antibiotics
A simple protocol for the synthesis of quinolone antibiotics is exemplified for the synthesis of norfloxacin; 3-chloro-4-fluoroaniline with triethyl orthoformate is transformed into its N-ethyl-N-formyl derivative which reacts with methyl malonyl morpholide and phosphoryl chloride at 100 °C to give 6-fluoro-7-chloro-1-ethylquinol-4-one-3-carboxylic acid, which has previously been converted into norfloxacin by the action of piperazine.
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