CAS: 195532-12-8; 8-Cyano-1-Cyclopropyl-6-Fluoro-7-((4As,7As)-Hexahydro-1H-Pyrrolo[3,4-B]Pyridin-6(2H)-yl)-4-Oxo-1,4-Dihydroquinoline-3-Carboxylic Acid

上下游产品

7-氯-8-氰基-1-环丙基-6-氟-1,4-二氢-4-氧代-3-喹啉羧酸 7-Chloro-8-Cyano-1-Cyclopropyl-6-Fluoro-1,4-Dihydro-4-Oxo-3-Quinolinecarboxylic Acid 117528-65-1

Ethyl 2-(2,4-Dichloro-3-Cyano-5-Fluorobenzoyl)-3-Cyclopropylaminoacrylate置于硫酸,溶剂黄146,三乙胺体系中,用 二氯甲烷,水,乙腈 用作溶剂,化学反应 73.0H,反应生成普拉沙星
参考文献:一种普拉沙星的合成方法
标题:一种普拉沙星的合成方法
摘要:本发明涉及一种普拉沙星的合成方法,该方法采用价廉易得的化合物为原料,经氯化,酰化,亲核取代,环化,水解,烷基化反应得到目标产物普拉沙星.本发明的亲核取代目标物β‑取代胺基‑α‑取代苯甲酰丙烯酸酯化合物质量好,纯度在98%以上,收率达到80~90%,较现有技术提高10%以上;本发明提供的酯水解方法及产品质量好,反应收率达到93~98%;用有机碱代替传统无机碱作为环化反应催化剂,操作简单,无污染,成本大幅度降低;以卤代烃作为烷基化溶剂,化学反应温度为室温条件,反应温和易于操作,20~40oc下进行烷基化反应比现有技术在高温下进行烷基化反应产生的杂质少,收率高,且卤代烃类溶剂易回收套用,污染大大减少,对环境友好.

专利信息

专利号:US-9353057-B2
优先权日:2003-12-30
标 题:Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof
发明人：GALLOP MARK A; DAI XUEDONG; SCHEUERMAN RANDALL A; RAILLARD STEPHEN P; MANTHATI SURESH K; YAO FENMEI; PHAN THU; LUDWIKOW MARIA; PENG GE; BHAT SEEMA
权利人:XENOPORT INC
摘要:Methods for synthesis of 1-(acyloxy)-alkyl carbamates, particularly, the synthesis of 1-(acyloxy)-alkyl carbamate prodrugs of primary or secondary amine-containing drugs are described. Also described are methods for synthesis of 1-(acyloxy)-alkyl N-hydroxysuccinimidyl carbonates which are useful intermediates in the synthesis of 1-(acyloxy)-alkyl carbamates are also described.

专利号:US-11332444-B2
优先权日:2018-04-25
标题:Method for the hydrolysis of quinolonecarboxylic esters
发明人：FEY PETER; BERWE MATHIAS; WIRTHS Joerg; WISCHNAT RALF; LONGERICH MARKUS; DIETZEL ANTJE
权利人:BAYER ANIMAL HEALTH GMBH
摘要:Quinolonecarboxylic esters of the general formula (II) are hydrolyzed to quinolonecarboxylic acids of the general formula (I):The method comprises the step A):A) reacting compounds of the formula (II) with a mixture comprising acetic acid, sulfuric acid and waterIn step A), ≥30 to ≤40 mol of acetic acid, ≥0.3 to ≤1 mol of sulfuric acid and ≥0.9 to ≤2.5 mol of water are used per mole of compounds of the formula (II). The method is particularly suitable for the synthesis of the intermediate (I) in the synthesis of pradofloxacin.

专利号:US-2015158809-A9
优先权日:2013-02-26
标 题 :Method of making 1-(acyloxy)-alkyl carbamate compounds
发明人：WANG HUAN; LIU PENG; DAI QUNYING; YIN HAO; RAILLARD STEPHEN P
权利人:XENOPORT INC
摘要:Methods of preparing carbamate prodrugs of amine-containing drugs are provided. Carbonates useful in the synthesis of the carbamate prodrugs are also provided.

专利号:US-2005222431-A1
优先权日:2003-12-30
标 题:Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof

专利号:US-7227028-B2
优先权日:2003-12-30
标题 :Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof

专利号:US-2007244331-A1
优先权日:2003-12-30
标 题 :Synthesis of Acyloxyalkyl Carbamate Prodrugs and Intermediates Thereof