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Front Cover: An Integrated Continuous‐Flow Synthesis of a Key Oxazolidine Intermediate to Noroxymorphone from Naturally Occurring Opioids (Eur. J. Org. Chem. 44/2017)
European Journal of Organic Chemistry ( IF 2.5 ) Pub Date : 2017-11-09 , DOI: 10.1002/ejoc.201701544
Alejandro Mata 1, 2 , David Cantillo 1, 2 , C. Oliver Kappe 1, 2
Affiliation  

The Front Cover shows the synthetic sequence towards noroxymorphone, a key intermediate in the preparation of important opioid antagonists such as naltrexone or naloxone. The process starts from oripavine, a naturally occurring compound in the poppy plant extract, and consists of a sequential oxidation with hydrogen peroxide to give the 14‐hydroxymorphinone derivative followed by hydrogenation and palladium‐catalyzed aerobic N‐demethylation. All synthetic steps have been integrated under continuous flow conditions. More information can be found in the Full Paper by A. Mata, D. Cantillo, and C. O. Kappe. See also the Full Paper by B. Gutmann, C. O. Kappe et al.
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中文翻译:

前盖:从天然存在的阿片类药物到去甲羟吗啡酮的中间体关键恶唑烷的连续连续流合成(Eur。J. Org。Chem。44/2017)

封面显示了去甲羟吗啡酮的合成序列,去甲羟吗啡酮是制备重要的阿片类拮抗剂(如纳曲酮或纳洛酮)的关键中间体。该过程从罂粟植物提取物中的天然化合物Oripavine开始,包括依次用过氧化氢氧化得到14-hydroxymorphinone衍生物,然后进行氢化和钯催化的好氧N-去甲基化。所有合成步骤均已在连续流动条件下整合。有关更多信息,请参见A. Mata,D。Cantillo和CO Kappe撰写的全文。另请参见B. Gutmann,CO Kappe等人的论文全文。
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更新日期:2017-11-09
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