CAS: 59711-96-5; Etimicin

该化合物是一种主要用于抗菌特性的乳胶球菌抗生素,主要来自细菌微生物的天然产物,其化学结构具有氨基糖和氨基环的复杂安排,而氨基环则具有典型的亚甲酸盐表面效应.这一结构使得它能够与细菌脊髓结结膜结合,抑制蛋白合成,并最终导致细菌细胞死亡.Etimicin展示了多种针对各种长效阴性细菌和一些克丁阳性细菌的多种活动,使其在治疗严重感染方面有所助益.人们特别注意到,这种化学结构对于耐抗其他抗生素的菌株具有效力.然而,与其他亚甲酸胶球表面一样,异丙素可以产生...

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    合成工艺路线路线简述

      📜,乙醛置于盐酸,三乙酰氧基硼氢化钠,哌啶体系中,用 水,二甲基亚砜 作为反应溶剂,化学反应 3.0H,反应生成 依替米星
      参考文献:一种硫酸依替米星的制备方法
      标题:一种硫酸依替米星的制备方法
      摘要:本发明公开了一种硫酸依替米星的制备方法.本发明采用fmoc‑cl保护庆大霉素c1A的3,2',6',3"位氨基,经纯化,蒸干后得到四芴甲氧羰基庆大霉素c1A;然后在酸性条件下加入乙醛水溶液n‑乙基化,再采用三乙酰氧基硼氢化钠进行还原;最后加入哌啶/dmso溶液脱保护;反应液用大孔吸附树脂柱初步纯化后,再经弱酸性阳离子吸附树脂二次纯化,纯化的产物加入硫酸反应制得硫酸依替米星.该方法上保护基时选择性高,副反应少;整个反应过程,反应条件温和,操作简便,更易于工业化的生产;产物纯度高,收率高.

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      专利信息


      专利号:WO-2022222249-A1
      优先权日:2021-04-24
      标 题:Method for obtaining 1-n-ethyl gentamicin c1a by using pipeline reaction hydrolysis
      发明人:WANG BIN; JIANG YINGQING; YOU LAN; YUAN WENJUN; LI PEIPENG
      权利人:WUXI JIYU SHANHE PHARMACEUTICAL CO LTD
      摘要:Involved is a method for obtaining 1-N-ethyl gentamicin C1a by using hydrolysis in a pipeline reactor. The method comprises the following steps: 1) pumping an etimicin synthesis solution and a NaOH solution into a temporary storage tank to be hydrolyzed, and mixing to obtain a reaction mixed solution; 2) opening a pipeline reactor to enable the temperature of a pipeline to reach about 100°C; 3) pumping the reaction mixed solution in step 1) into the pipeline reactor, controlling the temperatures of the inlet and outlet of a first reaction pipeline (1) to be 95-100°C, controlling the temperatures of the inlet and outlet of a second reaction pipeline (2) to be 100-110°C, keeping the temperature of the solution at 100-105°C, and performing hydrolysis for 6 hours; 4) after the reaction is completed, opening the circulating water supply valve and the circulating water return valve of a clamping sleeve on the pipeline reactor (3), and cooling to be close to room temperature; and 5) pumping a hydrolyzed reaction solution into a hydrolysis storage tank from the pipeline reactor (3).

      专利号:CN-117567226-A
      优先权日:2023-11-15
      标 题:Synthesis method of alpha-amino acid compound

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      ✅ COA系统入驻 | 共享模式

      主要参考文献


      1: Shao W, Zhong D, Jiang H, Han Y, Yin Y, Li R, Qian X, Chen D, Jing L. A new aminoglycoside etimicin shows low nephrotoxicity and ototoxicity in zebrafish embryos. J Appl Toxicol. 2020 Oct 22. doi: 10.1002/jat.4093. Epub ahead of print. 41(6):866-878. doi: 10.1038/s41401-019-0342-5. Epub 2020 Jan 14.
      3: Wang HX, Zhang LR, Ma XC, Ma TX. Influence of piperacillin on pharmacokinetics of etimicin in healthy volunteers. Acta Pharmacol Sin. 2002 Apr;23(4):376-80. 34(5):479-86. doi: 10.1177/0960327114550887. Epub 2014 Sep 17. 28(12):3365-71. doi: 10.1007/s11274-012-1148-5. Epub 2012 Sep 15.
      146:96-102. doi: 10.1016/j.jpba.2017.08.027. Epub 2017 Aug 24. 23(1):1-5. doi: 10.1007/s10895-012-1121-6. Epub 2012 Aug 24. 973C:97-103. doi: 10.1016/j.jchromb.2014.10.018. Epub 2014 Oct 23. 39(8):1471-9. doi: 10.1002/jssc.201501317. 55(5):902-7. doi: 10.1016/j.jpba.2011.03.005. Epub 2011 Mar 8.

      合成参考文献


      参考文献:10.1016/j.jpba.2014.04.024
      摘要:Wang Y, Zhang Z, Wu L, Zhang X, Wang H, Ye W, Li P. Isolation and structure characterization of related impurities in etimicin intermediate P1 by LC/ESI–MSn and NMR. Journal of Pharmaceutical and Biomedical Analysis. 2014 Aug;97():97–102. doi: 10.1016/j.jpba.2014.04.024.
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