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Rapid Synthesis of a Natural Product-Inspired Uridine Containing Library.
ACS Combinatorial Science ( IF 3.903 ) Pub Date : 2020-08-24 , DOI: 10.1021/acscombsci.0c00011
Wei-Chieh Cheng,Wan-Ju Liu,Kung-Hsiang Hu,Yee-Ling Tan,Yan-Ting Lin,Wei-An Chen,Lee-Chiang Lo

The preparation of natural product-inspired nucleoside analogs using solution-phase parallel synthesis is described. The key intermediates containing alkyne and N-protected amino moieties were developed to allow for further skeleton and substituent diversity using click chemistry and urea or amide bond formation. Rapid purification was accomplished using solid-phase extraction. The obtained library comprised 80 molecules incorporating two diversity positions and one chiral center, each of which was efficiently prepared in good purity and acceptable overall yield. A bacterial morphology study was also performed.

中文翻译:

受天然产物启发的含尿苷库的快速合成。

描述了使用液相平行合成法制备受天然产物启发的核苷类似物。开发了包含炔烃和 N 保护氨基部分的关键中间体,以允许使用点击化学和脲或酰胺键形成进一步的骨架和取代基多样性。使用固相萃取完成快速纯化。获得的文库包含 80 个包含两个多样性位置和一个手性中心的分子,每个分子都以良好的纯度和可接受的总收率有效制备。还进行了细菌形态学研究。
更新日期:2020-08-24
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