Building a Sulfonamide Library by Eco-Friendly Flow Synthesis

被引：58

作者：

Gioiello, Antimo ^{[1
]}

Rosatelli, Emiliano ^{[1
]}

Teofrasti, Michela ^{[1
]}

Filipponi, Paolo ^{[1
]}

Pellicciari, Roberto ^{[1
]}

机构：

[1] Univ Perugia, Dipartimento Chim & Tecnol Farmaco, I-06123 Perugia, Italy

来源：

ACS COMBINATORIAL SCIENCE | 2013年 / 15卷 / 05期

关键词：

sulfonamide; flow chemistry; eco-friendly synthesis; compound library; INHIBITORS; FACILE; ANTICANCER; REAGENTS; SOLVENT;

D O I：

10.1021/co400012m

中图分类号：

O69 [应用化学];

学科分类号：

081704 ;

摘要：

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.

引用

页码：235 / 239

页数：5

共 32 条

[1] Improved chemoselective, ecofriendly conditions for the conversion of primary alkyl halides into nitroalkanes under PEG400 [J].