作者
Chao Li, Jie Wang, Lisa M Barton, Shan Yu, Maoqun Tian, David S Peters, Manoj Kumar, Antony W Yu, Kristen A Johnson, Arnab K Chatterjee, Ming Yan, Phil S Baran
发表日期
2017/6/9
期刊
Science
卷号
356
期号
6342
页码范围
eaam7355
出版商
American Association for the Advancement of Science
简介
INTRODUCTION
The boronic acid is a functional group of enormous utility in materials science, chemosensor development, and drug discovery. In medicinal chemistry, boronic acids have been harnessed as a replacement for various structural motifs (a bioisostere) to improve the potency or pharmacokinetic profiles of lead compounds. However, the widespread incorporation of alkyl boronic acids has been largely hampered by the challenges associated with their preparation. Consequently, only two alkyl boronic acids are currently in clinical use, namely Velcade and Ninlaro. Few methods are capable of delivering alkyl boronates from readily available starting materials; most exhibit modest functional group compatibility. Indeed, boronate motifs are often installed at the early stage of a synthesis and thus consume disproportionate effort from the standpoint of planning and manipulation in multistep processes …
引用总数
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学术搜索中的文章
C Li, J Wang, LM Barton, S Yu, M Tian, DS Peters… - Science, 2017