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liuxing3982木虫 (正式写手)
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[求助]
求助将中文翻译成英文的文章摘要，不胜感激
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| [摘 要] 本文主要是对加米霉的合成工艺进行改进，优化更适合放大生产的工艺，通过改变中间体的纯化方法，更换反应试剂，使整个反应过程更安全环保，成本更低；该路线以9-脱氧-9-同型红霉素 A(E)肟为原料，在碱性催化剂的作用下生成9-脱氧-9-同型红霉素 A(Z)肟，再经过贝克曼重排反应生成红霉素亚安醚，然后经过硼氢化钠还原生成9-脱氧-8a-氮杂-8a-同型红霉素A，最后经过还原胺化反应得到加米霉素；并且用乙腈作溶剂培养出加米霉素单晶，该单晶数据被英国剑桥晶体学数据库收录，晶体的CCDC号为1913324；加米霉素的X射线衍射单晶结构测定表明，其结构为单斜晶系，C2空间群，具有手性，晶胞参数：a[Å]=27.536(6)，b[Å]=9.6582(19)，c[Å]=18.529(4)，α[˚]=90β[˚]˚=114.00(3)，γ[˚]=90V[Å3]=4501.6(15)，Z=4，Dc[mg/m3]=1.177，[mm–1]=0.086，F(000)=1750，GOF=1.043，Rint=0.0417，R1a, wR2b[I >2σ(I)]=0.0492,0.1291，Residuals [eÅ-3]= 0.0564, 0.1354. 加米霉素晶型的确定为后续研究加米霉素制剂新剂型等方面提供新选择。 |
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Inorg@USF
木虫 (正式写手)
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【答案】应助回帖
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试试啊， Abstract This article is mainly to improve the synthesis process of Candida, optimize the process that is more suitable for scale-up production. By changing the purification method of intermediates and replacing the reaction reagents, the entire reaction process is safer and more environmentally friendly, and lower cost. The scheme is to choose 9-deoxy-9-homo-erythromycin A(E) oxime as raw material, synthesized 9-deoxy-9-homo-erythromycin A(Z) oxime with alkaline catalyst, and produced erythromycin sulfonate through Beckmann rearrangement reaction, then reduced it with sodium borohydride to convert to 9-deoxy-8a-aza-8a-homoerythromycin A, finally undergoed reductive amination reaction to obtain gamimycin. THe single crystal of gamimycin was obtained with acetonitrile as a solvent. The crystal data is indexed in the Cambridge Crystallographic Database of the United Kingdom. The CCDC number of the crystal was 1913324; X-ray diffraction single crystal structure determination of gamimycin showed that its structure was a monoclinic system, C2 Space group, with chirality, unit cell parameters: a[Å]=27.536(6), b[Å]=9.6582(19), c[Å]=18.529(4), α[˚]=90β [˚]˚=114.00(3), γ[˚]=90V[Å3]=4501.6(15), Z=4, Dc[mg/m3]=1.177, [mm–1]=0.086, F (000)=1750, GOF=1.043, Rint=0.0417, R1a, wR2b[I >2σ(I)]=0.0492,0.1291, Residuals [eÅ-3]= 0.0564, 0.1354. Determination of the crystal form of Gamimycin provides a new option for the follow-up study of new dosage forms of Gamimycin preparations. |
2楼2020-06-21 10:06:17
