CAS: 268545-13-7; 1-Cyclopropyl-6-Fluoro-8-Methoxy-7-((4Ar,7Ar)-Octahydro-6H-Pyrrolo[3,4-B]Pyridin-6-yl)-4-Oxo-1,4-Dihydroquinoline-3-Carboxylic Acid

该化合物是一种合成的氟己酮抗生素,其特点是其广泛频谱抗菌活动,主要有效防治各种克格鲁阳性和克格鲁阴性细菌,使其在治疗呼吸道感染,皮肤感染和其他细菌疾病方面有用.该化合物具有双环结构,带有管子环,有助于其行动机制,抑制细菌DNA酶和四型异构酶,即细菌DNA复制和转录所需的基本酶.莫西弗罗辛(Moxxixacin)的口服生物利用率良好,并经常以平板形式或静脉注射方式进行.其致癌基因包括相对长的半衰期,允许一次性服用.此外,该化合物具有有利的安全特征,但潜在的副作用可能包括胃肠扰动,...

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    上下游产品

    1-cyclopropyl-6,7-difluoro-1,4-dihydro-8-methoxy-4-oxo-3-quinolinecarboxylic acid (1S,6S)-2,8-diazabicyclo[4.3.0]nonane 3,O4-bis(propyloxy-O)borate1-cyclopropyl-6,7-difluoro-8-methoxy-4-oxo-1,4-dihydro-3-quinoline-carboxylic acid O3,O4-bis(propyloxy-O)borate moxifloxacin hydr°Chloride methyl 1-cyclopropyl-6-fluoro-8-methoxy-7-((4aS,7aS)-°Ctahydro-6H-pyrrolo[3,4-b]pyridin-6-yl)-4-oxo-1,4-dihydroquinoline-3-carboxylate N-methylmoxifloxacin 7-amino-1-cyclopropyl-6-fluoro-1,4-dihydro-8-methoxy-4-oxoquinoline-3-carboxylic acid 1-cyclopropyl-7-{(S,S)-2,8-diazabicyclo[4.3.0]non-8-yl}-6-fluoro-8-hydroxy-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid

    合成工艺路线路线简述

      📜(S,S)-2,8-二氮杂双环[4,3,0]壬烷,1-环丙基-6,7-二氟-1,4-二氢-8-甲氧基-4-氧代-3-喹啉羧酸置于nano Iron Oxide On Zro2 Coated Sulfonic Acid体系中,用 水 用作溶剂,化学反应 0.42H,以96%的收率获得莫西光学对映体
      参考文献:Nano-Fe3O4@zro2-So3H作为高效可回收催化剂用于氟喹诺酮类的绿色合成
      标题:Nano-Fe3O4@zro2-So3H作为高效可回收催化剂用于氟喹诺酮类的绿色合成
      摘要:已经制备了带有磺酸基团的核壳氧化锆包覆磁铁矿纳米颗粒(纳米-Fe3O4@zro2-H3Po4),并将其用作一种有效的酸催化剂,用于通过 7-卤代-6 氟喹诺酮-3 羧酸与各种哌嗪衍生物和 (4Ar,7Ar)-八氢-1H-吡咯并[3,4-B] 吡啶.反应在普通水或磁化水作用作溶剂中进行.在最终结果中,纳米 Fe3O4@zro2-So3H 在两种形式的水中都表现出非常好的催化性能.然而,磁化水显示出更好的结果.因此,这种新方法在回流条件下,在作为绿色溶剂的水中以可接受的收率和简单的后处理过程迅速实现了合适的产品.此外,
      Doi:10.2174/1570178615666171226162735

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      专利信息


      专利号:WO-2012131629-A1
      优先权日:2011-03-31
      标题 :A process for preparation of intermediate of moxifloxacin
      发明人:WANKHEDE KARUNA; JAGTAP ASHUTOSH; ROY MITA; HARIHARAN SIVARAMAKRISHNAN; KUMBHAR AJAY
      权利人:PIRAMAL HEALTHCARE LTD; WANKHEDE KARUNA; JAGTAP ASHUTOSH; ROY MITA; HARIHARAN SIVARAMAKRISHNAN; KUMBHAR AJAY
      摘要:The present invention provides a process for the preparation of racemic or chiral octahydro-6-(phenylmethyl)-1H-pyrrolo[3,4-b]pyridine of formula I, a key intermediate in the synthesis of moxifloxacin or its pharmaceutically acceptable salts. The process comprises reaction of racemic or chiral tetrahydro-6-(phenylmethyl)-1H- pyrrolo[3,4-b]pyridine-5,7(6H)-dione of formula II with a reducing agent, which is a mixture of two agents, that is mixture of dimethyl sulphate and sodium borohydride or aluminum chloride and sodium borohydride used in a molar ratio ranging from 1:1 to 1: 4, in the presence of a polar solvent at a temperature ranging from 15°C to 45°C 10 to obtain racemic or chiral octahydro-6-(phenylmethyl)-1H-pyrrolo[3,4-b]pyridine of formula I having purity ≥ 96%.

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