Solvent- and Catalyst-Free Huisgen Cycloaddition to Rufinamide in Flow with a Greener, Less Expensive Dipolarophile

被引:48
作者
Borukhova, Svetlana [1 ]
Noel, Timothy [1 ]
Metten, Bert [2 ]
de Vos, Eric [2 ]
Hessel, Volker [1 ]
机构
[1] Eindhoven Univ Technol, Dept Chem Engn & Chem Micro Flow Chem & Proc Tech, NL-5612 AZ Eindhoven, Netherlands
[2] SA Ajinomoto OmniChem NV, B-9230 Wetteren, Belgium
基金
欧洲研究理事会;
关键词
cycloaddition; green chemistry; microflow chemistry; novel process windows; solvent free; PROCESS DESIGN; PROCESS WINDOWS; DRUG DISCOVERY; COST-ANALYSIS; CHEMISTRY; MICROREACTOR;
D O I
10.1002/cssc.201300684
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
Give it a flow: A continuous-flow process for the synthesis of a 1,2,3-triazole precursor of Rufinamide has been developed. The protocol involves a solvent- and catalyst-free operation and utilizes reaction temperatures above the melting point of the target product to prevent microreactor clogging, resulting in a decrease of the operating time from hours to minutes. Copyright © 2013 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.
引用
收藏
页码:2220 / 2225
页数:6
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