A Survey of the Borrowing Hydrogen Approach to the Synthesis of some Pharmaceutically Relevant Intermediates

A Survey of the Borrowing Hydrogen Approach to the Synthesis of some Pharmaceutically Relevant Intermediates
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DOI:
10.1021/acs.oprd.5b00199
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发表时间:
2015-10-01
影响因子:
3.4
通讯作者:
Newton, Rebecca
Newton, Rebecca
中科院分区:
化学3区
文献类型:
--
作者:
Leonard, John;Blacker, A. John;Newton, Rebecca

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利用“借氢策略”在合成一些典型的医药中间体进行了研究。这项工作的主要目的是调查在工业环境中使用标准实验室技术的当前方法的范围和局限性。在不同的复杂底物中获得了一些有趣而重要的结果;然而,这种方法也存在一些缺点,如负载高、周转差、催化剂易受底物失活等。这些都是未来研究和改进的重点领域。
The use of the "borrowing hydrogen strategy" in the synthesis of a number of typical pharmaceutical intermediates has been investigated. The main aim of this work was to investigate the scope and limitations of current methodology using standard laboratory techniques in an industrial context. Some interesting and significant results were achieved across a diverse set of complex substrates; however several drawbacks with this approach were identified, such as the high loading, poor turnover, and susceptibility to substrate inactivation of the catalysts. These are areas which are highlighted for future investigation and improvements.