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.

Keywords:

natural products; combinatorial chemistry; chromatography-free; solution-phase synthesis