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Lamb, Moxifloxacin: a review of its clinical potential in the management of community-acquired respiratory tract infections. Drugs, 2000. 59(1): p. 115-39.\n[2].\nCulley, C.M., et al., Moxifloxacin: clinical efficacy and safety. Am J Health Syst Pharm, 2001. 58(5): p. 379-88.\n[3].\nIoannidis, O., et al., Effect of moxifloxacin on the survival, lipid peroxidation and inflammation of immunosuppressed rats with soft tissue infection from Stenotrophomonas maltophilia. Microbiol Immunol, 2013.",[257,263,269,275],{"slug":258,"cid":259,"name":260,"nameZh":260,"cas":261,"imgSvg":262},"785894574106087400","J-1099322-6","1-环丙基-6,7-二氟-1,...","112811-72-0","https:\u002F\u002Fapi.chemical.xiaokangmed.com\u002Fimages\u002Fchem_structures_svg\u002F241\u002F112811-72-0.svg",{"slug":264,"cid":265,"name":266,"nameZh":266,"cas":267,"imgSvg":268},"785889864582172700","J-1583755-4","(S,S)-2,8-二氮杂双环...","151213-40-0","https:\u002F\u002Fapi.chemical.xiaokangmed.com\u002Fimages\u002Fchem_structures_svg\u002F273\u002F151213-40-0.svg",{"slug":270,"cid":271,"name":272,"nameZh":272,"cas":273,"imgSvg":274},"785881476074836000","J-1975936-0","盐酸莫西沙星","186826-86-8","https:\u002F\u002Fapi.chemical.xiaokangmed.com\u002Fimages\u002Fchem_structures_svg\u002F229\u002F186826-86-8.svg",{"slug":276,"cid":277,"name":278,"nameZh":278,"cas":279,"imgSvg":280},"785888885849722900","J-1357324-5","(Z)-3-(环丙基氨基)-2...","112811-70-8","https:\u002F\u002Fapi.chemical.xiaokangmed.com\u002Fimages\u002Fchem_structures_svg\u002F327\u002F112811-70-8.svg",[282],{"slug":270,"cid":271,"name":272,"nameZh":272,"cas":273,"imgSvg":274},[284],{"key":285,"value":286},"海关编码","29329970",[288,291,294,297,300],{"key":289,"value":290},"危害码 (欧洲)","Xn: Harmful;",{"key":292,"value":293},"风险声明 (欧洲)","R22",{"key":295,"value":296},"安全声明 (欧洲)","S26-S37\u002F39",{"key":298,"value":299},"WGK德国","3",{"key":285,"value":286},"\u003Cp>推荐如下合成路线,中间体1-环丙基-6,7-二氟-1,4-二氢-8-甲氧基-4-氧代-3-喹啉羧酸与硼的螯合物按文献[8]方法制备.\u003C\u002Fp>\u003Cp>\u003C\u002Fp>\u003Cp>(1).6-苄基-吡咯并[3,4-b]吡啶-5,7-二酮的制备\u003C\u002Fp>\u003Cp>在反应瓶中加入75.15g(0.45mol)和乙酸酐170ml(1.8mol),加热微回流搅拌反应4.5h.减压浓缩至干,剩余物加二烷100ml,搅拌加热至70 ºC,待溶解后减压蒸除溶剂,得白色固体.直接进行下步反应.\u003C\u002Fp>\u003Cp>在反应瓶中加入二烷200ml和上步骤所得白色固体，室温搅拌下滴加苄基胺（PhCH2NH2）49.2ml(0.45mol),约30min滴完,继续在室温搅拌1.5h.减压浓缩至干,剩余物中加入乙酸酐191ml(2.03mol)和乙酸钠5.54g(0.068mol),升温至125 ºC\u003C\u002Fp>\u003Cp>,在该温度保持搅拌3.5h.冷至室温,过滤,滤饼水洗,乙醇洗,抽干,干燥,得白色固体92.3g.滤液减压浓缩至体积40ml,室温放置过夜析晶,回收6.02g,共得98.3g,收率91.8%,mp161~163 ºC.\u003C\u002Fp>\u003Cp>(2) 6-苄基-六氢-吡咯并[3,4-b]吡啶-5,7-二酮的制备\u003C\u002Fp>\u003Cp>在高压釜中加入20g(0.084mol)、THF150ml和5%Pd\u002FC 2.5g,用N2置换釜内空气三次,氢气置换N2三次,充氢(85 ºC\u002F8Mpa)反应,直至不吸氢为止(大约5h),冷却,放余压,滤除反应液中Pd\u002FC,滤液减压浓缩至干,得黄色油状物粗品20.42g,不要纯化,直接进行下步反应.\u003C\u002Fp>\u003Cp>(3)6-苄基-八氢-吡咯并[3,4-b]吡啶的制备\u003C\u002Fp>\u003Cp>在反应瓶中于氮气保护下加入THF 500ml和LiAlH4 10.3g(0.27mol),并在搅拌下和氮气保护下滴加上步无水THF(60ml)溶液,加毕,搅拌缓慢升温至回流,搅拌回流16h.冷至室温,慢慢加入水10.5ml和THF100ml,滴加5%NaOH25ml,加毕,搅拌回流1h.冷却至室温,过滤,滤渣用THF洗，滤液及洗液合并，减压浓缩至干，得棕色黏稠状液体17.0g,收率93.7%.\u003C\u002Fp>\u003Cp>(4) (S,S)-6-苄基-八氢-吡咯并[3,4-b]吡啶的制备在\u003C\u002Fp>\u003Cp>反应瓶中加入L-(+)-酒石酸21.1g(0.141mol)、DMF60ml,搅拌加热到80 ºC溶解,30min内滴加[19.0g(0.088mol)]的DMF(20ml)溶液,同温度下搅拌1h,冷却至室温后再搅拌1h,放置过夜.过滤,滤饼用DMF洗,乙醇洗,用乙二醇单甲醚重结晶,得(R,R)- (S,S)-6-苄基-八氢-吡咯并[3,4-b]吡啶的L-酒石酸盐白色晶体13.6g,收率84.4%,mp112~120 ºC .\u003C\u002Fp>\u003Cp> 合并滤液和重结晶洗液,减压浓缩至干,剩余物中加水50ml,搅拌下加入30%NaOH水溶液50ml,干90~100 ºC 搅拌1h.冷却至室温,除去少量漂浮的黑色黏稠物,用环己烷(150ml*3)提取,有机层用无水硫酸钠干燥,过滤,滤液减压浓缩,得棕色液体10g,待用.\u003C\u002Fp>\u003Cp>在反应瓶中加入D-(-)-酒石酸11.0g(0.073mol)和DMF 35ml,搅拌加热至80 ºC 溶解,于30min内滴加上述所得之棕色液体的DMF(15ml)溶液,同温搅拌1h.自然冷却至室温后再搅拌1h,放置过夜.过滤,滤饼用(S,S)- (S,S)-6-苄基-八氢-吡咯并[3,4-b]吡啶的D-酒石酸盐12.5g,收率77.6%,mp112~120 ºC \u003C\u002Fp>\u003Cp> (S,S)- (S,S)-6-苄基-八氢-吡咯并[3,4-b]吡啶的D-酒石酸盐12.5g(0.034mol)加\u003C\u002Fp>\u003Cp>到反应瓶,加水40ml,搅拌溶解,搅拌下加入30%NaOH水溶液11ml,室温搅拌1h.用环己烷(150ml*3)提取,有机层用无水硫酸钠干燥,过滤,滤液减压浓缩至干,得黄色黏稠液(S,S)-6-苄基-八氢-吡咯并[3,4-b]吡啶 6.6g,收率89.4%.\u003C\u002Fp>\u003Cp>(5).(S,S)-八氢-6H-吡咯并[3,4-b]吡啶的制备\u003C\u002Fp>\u003Cp>在高压釜加入(S,S)-6-苄基-八氢-吡咯并[3,4-b]吡啶 6.5g(0.03mol)和甲醇\u003C\u002Fp>\u003Cp>50ml,搅拌溶解,加入5%Pd\u002FC 1.35g,于90 ºC \u002F9MPa下氢化(操作同(2))16h.过滤,滤液减压浓缩至干(浴温<45 ºC ).剩余物溶于水20ml,用环己烷(20ml*3)提取,有机层用水反提取(30ml*3),合并水层,加入NaOH 2g,用氯仿(30ml*3)提取,有机层用无水硫酸钠干燥,过滤,滤液减压浓缩至干,得浅黄色黏液.3.4g,收率89.9%.\u003C\u002Fp>\u003Cp>(6). (1-环丙基-6,7-二氟-1,4-二氢-8-甲氧基-4-氧代-3-喹啉羧酸-O3,O4)双(乙酰氧)-硼酸盐(或硼螯合物)的制备\u003C\u002Fp>\u003Cp>在反应瓶中加入硼酸57.2g(0.925mol)和氯化锌1.24g,再向该混合物中加入乙酸酐300ml,搅拌升温至110 ºC ,在该温度搅拌1.5h.再向该反应混合物中加入冰醋酸400ml,在同温度下搅拌1h.放冷后,在50~60 ºC加入1-环丙基-6,7-二氟-1,4-二氢-8-甲氧基-4-氧代-3-喹啉羧酸 200g(0.619mol),随后加入200ml冰醋酸,在同温度下搅拌5h.将反应混合物减压浓缩,剩余油状物中加入8L冰水,产生沉淀,过滤收集,再悬浮至3L水中,过滤,干燥,得到(1-环丙基-6,7-二氟-1,4-二氢-8-甲氧基-4-氧代-3-喹啉羧酸-O3,O4)双(乙酰氧)-硼酸盐(或硼螯合物) 249g,它是一亮橙黄色粉末状物,mp113~117 ºC\u003C\u002Fp>\u003Cp>(7) 莫西沙星的合成\u003C\u002Fp>\u003Cp>在反应瓶中加入(1-环丙基-6,7-二氟-1,4-二氢-8-甲氧基-4-氧代-3-喹啉羧酸-O3,O4)双(乙酰氧)-硼酸盐(或硼螯合物) 2.0g(4.73mmol)和乙腈10ml,搅拌溶解,再加入三乙胺0.5ml和(S,S)-八氢-6H-吡咯并[3,4-b]吡啶 0.66g(5.24mmol),搅拌回流3h.减压浓缩至干,剩余物加石油醚,捣碎分散固化,得黄色固体过滤,滤饼用石油醚洗,抽干,溶于7%NaOH溶液13.5ml,于80 ºC 搅拌3h,冷至室温,过滤,滤液用5%乙酸水溶液调至PH7,过滤,滤饼用5%乙酸水溶液溶解,过滤,滤液用5%NaOH水溶液调至PH7,过滤,滤饼用水洗,乙醇洗,抽干,干燥,得淡黄色固体莫西沙星 1.53g,收率80.5%,mp203~207 ºC\u003C\u002Fp>","2026-08-21T07:51:12.859463Z",false,[305,311,316,321,327,333],{"slug":306,"cid":307,"name":308,"nameZh":309,"cas":310},"785872510607429632","J-1334045-0","calcium saccharin","糖精钙","6485-34-3",{"slug":312,"cid":313,"name":314,"nameZh":314,"cas":315},"785911446427930624","J-69315-4","9-Bromo-10-(naphthalen-1-yl-d7)anthracene-1,2,3,4,5,6,7,8-d8","2330770-73-3",{"slug":317,"cid":318,"name":319,"nameZh":319,"cas":320},"785914490636996608","J-1241469-7","2-Chloro-4-(1-dibenzofuranyl)-6-(1-naphthalenyl)-1,3,5-triazine","2417986-80-0",{"slug":322,"cid":323,"name":324,"nameZh":325,"cas":326},"785871874079854592","J-1110697-5","Crystal Violet","结晶紫","548-62-9",{"slug":328,"cid":329,"name":330,"nameZh":331,"cas":332},"785895040399446016","J-1110640-3","Solvent Red 27","溶剂红27","1320-06-5",{"slug":334,"cid":335,"name":336,"nameZh":337,"cas":338},"785882572553981952","J-1110759-4","Methyl Violet 2B","甲基紫2B","8004-87-3",1792652772086,"zh-CN",[]]