CAS: 256328-82-2; (S)-N-((S)-1-((4S,5S)-4-Benzyl-2-Oxooxazolidin-5-yl)-3-Phenylpropan-2-yl)-2-(3-((2-Isopropylthiazol-4-yl)Methyl)-3-Methylureido)-3-Methylbutanamide

该化合物是一种复杂的有机化合物,其特征是其手感中心和多种功能组.它有一个氧化氮环,表明它可能从事生物活动,特别是在抗生素特性方面. 黄素微生物的出现表明它可能与生物目标发生相互作用,加强其药用特征.这种化合物有可能展示具体的立体化学学,影响它与酶和感官的相互作用.其结构包括氨化物联系,这种联系在生物活性分子中很常见,而且芳基环的存在可能有助于其稳定性和可溶性特性特性,特别是在抗生性化学特性中,这种化合物的遗传性病菌体结构显示其他疾病的潜力.

结构式图片

上下游产品

(4S,5S)-5-((2S)-2-amino-3-phenyl-propyl)-4-benzyl-1,3-oxazolidin-2-one N-((N-Methyl-N-((2-isopropyl-4-thiazolyl)methyl)amino)-carbonyl)-L-valine ritonavir

合成工艺路线路线简述

    📜利托那韦置于potassium Tert-Butylate,氧气体系中,用 四氢呋喃 用作溶剂,化学反应生成去噻唑基甲基 利托那韦
    参考文献:Isayama-mukaiyama钴催化的氢过氧化硅烷化在制备利托那韦氢过氧化物中的应用
    标题:Isayama-mukaiyama钴催化的氢过氧化硅烷化在制备利托那韦氢过氧化物中的应用
    摘要:我们报告了噻唑-5-基甲基((2 S,3 S,5 S)-5-((S)-2-(3-((2-(2-Hydroperoxypropan-2-Yl)thiazol-4-基)甲基)-3-甲基脲基)-3-甲基丁酰胺基)-3-羟基-1,6-二苯基己-2-基)氨基甲酸酯,利托那韦的氢过氧化物杂质,也被称为利托那韦usp杂质g.发现利托那韦的结构和大量易受氧化作用的官能团,强迫降解是一种非选择性和不足的策略.因此,应用了多步合成.总体策略涉及将丙烯基部分最初引入到末端噻唑中,从而能够使用co(thd)2(0.1 Equiv)/ O 2进行选择性氧化 结构组装后(isayama-mukaiyama钴催化的氢过氧化硅烷化).
    Doi:10.1016/j.Tetlet.2016.10.022

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    ✅ COA系统入驻 | 共享模式

    主要参考文献


    1: Rojas J, Lonca M, Imaz A, Estrada V, Asensi V, Miralles C, Domingo P, Montero M, Del Rio L, Fontdevila J, Perez I, Cruceta A, Gatell JM, Arnedo M, Martínez E. Improvement of lipoatrophy by switching from efavirenz to lopinavir/ritonavir. HIV Med. 2016 May;17(5):340-9. doi: 10.1111/hiv.12314. Epub 2015 Sep 10. doi: 10.1093/jac/dkv447. Epub 2016 Jan 7. doi: 10.1111/bcp.12873. Epub 2016 Feb 24. Antiretroviral resistance at virological failure in the NEAT 001/ANRS 143 trial: raltegravir plus darunavir/ritonavir or tenofovir/emtricitabine plus darunavir/ritonavir as first-line ART. J Antimicrob Chemother. 2016 Apr;71(4):1056-62. doi: 10.1093/jac/dkv427. Epub 2015 Dec 24. doi: 10.1093/jac/dkv436. Epub 2015 Dec 18. Efficacy and safety of once-daily ritonavir-boosted atazanavir or darunavir in combination with a dual nucleos(t)ide analogue backbone in HIV-1-infected combined ART (cART)-naive patients with severe immunosuppression: a 48 week, non-comparative, randomized, multicentre trial (IMEA 040 DATA trial). J Antimicrob Chemother. 2016 Apr 10. pii: dkw103. [Epub ahead of print] doi: 10.1007/s12072-015-9699-9. Epub 2016 Feb 17. doi: 10.1016/j.ejpb.2016.01.018. Epub 2016 Feb 6. doi: 10.1093/cid/ciw028. Epub 2016 Jan 20.
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