dna兼容的氰基转化为硫酰胺反应
首发时间:2024-01-19
摘要:本文发展了一种dna兼容的官能团转化反应,将dna偶联的腈化物转化为硫酰胺。首先通过二硫化碳和硫化钠水合物反应生成三硫代碳酸钠阴离子,再和dna偶联的腈化物反应将氰基转化为硫酰胺,该反应操作简便,条件温和。发展该反应扩展了dna编码分子库(dna-encoded libraries,dels)领域的化学多样性,为先导化合物的发现奠定了基础。
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dna-compatible transformation of nitriles into thioamides
abstract:in this paper, a dna-compatible functional group transformation reaction was developedto convert dna-conjugated nitriles to thioamides. first, carbon disulfide wasreacted with sodium sulfide nonahydrate to generate sodium trithiocarbonate anion, and then reacted with dna-conjugated nitriles to convert the cyano group to thioamides. this reaction was simple to operate and had mild conditions. the development of this reaction expanded the chemical diversity in the field of dna-encoded libraries (dels) and laid the foundation for the discovery of lead compounds.
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