Building a Sulfonamide Library by Eco-Friendly Flow Synthesis
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- 作者：Antimo Gioiello ; Emiliano Rosatelli ; Michela Teofrasti ; Paolo Filipponi ; Roberto Pellicciari
- 刊名：ACS Combinatorial Science
- 出版年：2013
- 出版时间：May 13, 2013
- 年：2013
- 卷：15
- 期：5
- 页码：235-239
- 全文大小：275K
- 年卷期：v.15,no.5(May 13, 2013)
- ISSN：2156-8944
文摘
A rapid and eco-friendly synthesis of a sulfonamide library under flow conditions is described. The study illustrates an efficient, safe, and easily scalable preparation of sulfonamides by use of a meso-reactor apparatus, thus demonstrating the impact of flow technologies within drug discovery. Waste minimization, employment of green media, and nontoxic reactants are achieved by the optimization of the flow setup and experimental protocol designed to sequentially synthesize primary, secondary, and tertiary sulfonamides. Isolation of the products involves only extraction and precipitation affording pure compounds in good to high yields without further purification for biological evaluation.