Institute of Pharmaceutical Chemistry University of Szeged, H-6720, Szeged, Eötvös u. 6, Hungary.
MTA-SZTE Stereochemistry Research Group Hungarian Academy of Sciences, H-6720, Szeged, Eötvös u. 6, Hungary.
Chem Rec. 2016 Jun;16(3):1018-33. doi: 10.1002/tcr.201500286. Epub 2016 Mar 21.
There is a great need for effective transformations and a broad range of novel chemical entities. Continuous-flow (CF) approaches are of considerable current interest: highly efficient and selective reactions can be performed in CF reactors. The reaction setup of CF reactors offers a wide variety of possible points where versatility can be introduced. This article presents a number of selective and highly efficient gas-liquid-solid and liquid-solid reactions involving a range of reagents and immobilized catalysts. Enantioselective transformations through catalytic hydrogenation and organocatalytic reactions are included, and isotopically labelled compounds and pharmaceutically relevant 1,2,3-triazoles are synthesized in CF reactors. Importantly, the catalyst bed can be changed to a solid-phase peptide synthesis resin, with which peptide synthesis can be performed with the utilization of only 1.5 equivalents of the amino acid.
非常需要有效的转化和广泛的新型化学实体。连续流 (CF) 方法目前引起了相当大的兴趣:可以在 CF 反应器中进行高效和选择性的反应。CF 反应器的反应设置提供了广泛的可能点,可以引入多功能性。本文介绍了一系列涉及多种试剂和固定化催化剂的选择性和高效的气-液-固和液-固反应。包括通过催化氢化和有机催化反应的对映选择性转化,并在 CF 反应器中合成了同位素标记化合物和药物相关的 1,2,3-三唑。重要的是,可以将催化剂床更换为固相肽合成树脂,仅使用 1.5 当量的氨基酸即可进行肽合成。