Column Chromatography-Free Solution-Phase Synthesis of a Natural Piper-Amide-like Compound Library
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- 作者：Sumin Kim ; Chaemin Lim ; Sukjin Lee ; Seokwoo Lee ; Hyunkyung Cho ; Joo-Youn Lee ; Dong Sup Shim ; Hee Dong Park ; Sanghee Kim
- 刊名：ACS Combinatorial Science
- 出版年：2013
- 出版时间：April 8, 2013
- 年：2013
- 卷：15
- 期：4
- 页码：208-215
- 全文大小：353K
- 年卷期：v.15,no.4(April 8, 2013)
- ISSN：2156-8944
文摘
We have achieved an efficient solution-phase parallel synthesis of a library of natural piper-amide-like compounds from the bifunctional 尾-phosphono-N-hydroxy-succinimidyl ester intermediate. The primary important feature in our study is the construction of natural-product-like molecules through the adaptation of sophisticated organic reactions that create water-soluble byproducts for a chromatography-free purification. This simple and efficient method rapidly provides a combinatorial library of high yield and purity. The library was evaluated against GPCR targets to demonstrate its potential use as a tool for drug discovery and in chemical biology.