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Solid-Phase Synthesis of 2,3,5-Trisubstituted 4H-Imidazolones

机译:2,3,5-三取代的4H-咪唑酮的固相合成

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摘要

The rapid synthesis of large organic compound collections by combinatorial methods using solid-phase approaches continues to be a promising strategy for the discovery of new pharmaceutical lead compounds. The focus of this field of research, which initially involved the synthesis of peptides and oligonucleotides, is now on the synthesis of small organic molecules on the solid phase. Heterocycles, such as benzo-diazepines, hydantoins, pyrrolidines, bicyclic guanidines, have received special attention in combinatorial synthesis because of their biologically relevant properties. This strategy has permitted the rapid synthesis of large numbers of heterocyclic compounds in a short time period, facilitating their use in high-throughput screening.
机译:使用固相方法通过组合方法快速合成大型有机化合物集合,仍然是发现新的药物先导化合物的有前途的策略。该研究领域的最初关注于肽和寡核苷酸的合成,现在的重点是固相上有机小分子的合成。杂环,例如苯并二氮杂卓,乙内酰脲,吡咯烷,双环胍,由于其生物学相关性质而在组合合成中受到了特别的关注。该策略已允许在短时间内快速合成大量杂环化合物,从而有助于其在高通量筛选中的使用。

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