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The development and use of novel iridium complexes as catalysts for ortho-directed hydrogen isotope exchange reactions

机译:新型铱配合物作为邻位定向氢同位素交换反应催化剂的开发和应用

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摘要

The preparation and application of groups of new iridium complexes are described. In particular, iridium complexes possessing phosphine ligands and a bulky N-heterocyclic carbene have been shown to be robust and readily handled species and have been applied in a range of directed hydrogen-deuterium and -tritium exchange processes and, in particular, with drug-like substrates or within ADMET-related studies. Overall, these new iridium(I) complexes are shown to be highly active catalysts and display catalytic activity far in excess of the industry standard, Crabtree's catalyst, with excellent levels of labelling being achieved over short reaction times and at low metal complex loadings, whilst tolerating a wide range of functional moieties. Furthermore and again in contrast to systems employing Crabtree's catalyst, the low catalyst loadings and short reaction times made possible by these emerging iridium carbene comple have delivered tritiated products with very good levels of labelling and without any appreciable by-product waste production.
机译:描述了一组新的铱配合物的制备和应用。特别是,具有膦配体和庞大的N杂环卡宾的铱配合物已被证明是坚固且易于处理的物种,并已应用于一系列定向氢-氘和-tri交换过程,尤其是与药物-例如底物或与ADMET相关的研究。总体而言,这些新型铱(I)配合物被证明是高活性催化剂,其催化活性远远超过了工业标准Crabtree的催化剂,在较短的反应时间和较低的金属配合物负载下实现了出色的标记水平,而耐受广泛的功能部分。此外,与使用Crabtree催化剂的系统形成对比的是,这些新兴的铱卡宾化合物可实现低催化剂装载量和较短的反应时间,从而使ti化产品的标签水平非常高,并且不会产生明显的副产品废物。

著录项

  • 作者

    Nilsson, G.N.; Kerr, W.J.;

  • 作者单位
  • 年度 2010
  • 总页数
  • 原文格式 PDF
  • 正文语种 {"code":"en","name":"English","id":9}
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