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杂环化合物中的微波辅助反应及其在药物化学和超分子化学中的应用。

Microwave-assisted reactions in heterocyclic compounds with applications in medicinal and supramolecular chemistry.

作者信息

de la Hoz Antonio, Díaz-Ortiz Angel, Moreno Andrés, Sanchéz-Migallón Ana, Prieto Pilar, Carrillo José Ramón, Vázquez Ester, Gómez M Victoria, Herrero M Antonia

机构信息

Departamento de Química Orgánica, Facultad de Química, Universidad de Castilla-La Mancha, E-13071 Ciudad Real, Spain.

出版信息

Comb Chem High Throughput Screen. 2007 Dec;10(10):877-902. doi: 10.2174/138620707783220347.

DOI:10.2174/138620707783220347
PMID:18288949
Abstract

Microwave irradiation has been successfully applied in organic chemistry. Spectacular accelerations, higher yields under milder reaction conditions and higher product purities have all been reported. Indeed, a number of authors have described success in reactions that do not occur under conventional heating and modifications in selectivity (chemo-, regio- and stereoselectivity) have even been reported. Recent advances in microwave-assisted combinatorial chemistry include high-speed solid-phase and polymer-supported organic synthesis, rapid parallel synthesis of compound libraries, and library generation by automated sequential microwave irradiation. In addition, new instrumentation for high-throughput microwave-assisted synthesis continues to be developed at a steady pace. The impressive speed combined with the unmatched control over reaction parameters justifies the growing interest in this application of microwave heating. In this review we highlight our recent advances in this area, with a particular emphasis on cycloaddition reactions of heterocyclic compounds both with and without supports, applications in supramolecular chemistry and the reproducibility and scalability of organic reactions involving the use of microwave irradiation techniques.

摘要

微波辐射已成功应用于有机化学领域。文献报道了其显著的加速效果、在更温和反应条件下更高的产率以及更高的产物纯度。事实上,许多作者描述了在常规加热条件下无法发生的反应取得成功,甚至还报道了选择性(化学、区域和立体选择性)方面的改变。微波辅助组合化学的最新进展包括高速固相和聚合物负载的有机合成、化合物库的快速平行合成以及通过自动顺序微波辐射生成文库。此外,用于高通量微波辅助合成的新仪器也在稳步发展。令人印象深刻的速度以及对反应参数无与伦比的控制,使得人们对微波加热在该应用领域的兴趣日益浓厚。在本综述中,我们重点介绍了我们在该领域的最新进展,特别强调了杂环化合物在有或无载体情况下的环加成反应、在超分子化学中的应用以及涉及微波辐射技术的有机反应的重现性和可扩展性。

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Microwave-assisted reactions in heterocyclic compounds with applications in medicinal and supramolecular chemistry.杂环化合物中的微波辅助反应及其在药物化学和超分子化学中的应用。
Comb Chem High Throughput Screen. 2007 Dec;10(10):877-902. doi: 10.2174/138620707783220347.
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High-speed combinatorial synthesis utilizing microwave irradiation.利用微波辐射的高速组合合成。
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Recent applications of microwave irradiation to medicinal chemistry.微波辐射在药物化学中的最新应用。
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Applications of the combination of microwave and parallel synthesis in medicinal chemistry.微波与平行合成相结合在药物化学中的应用
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The application of microwave irradiation as new convenient synthetic procedure in drug discovery.微波辐射作为药物研发中一种新型便捷合成方法的应用。
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Solid-phase strategies for the design and synthesis of heterocyclic molecules of medicinal interest.用于设计和合成具有药用价值的杂环分子的固相策略。
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