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用于无溶剂和无催化剂合成杂环化合物、药物及酯类的高压活化法。

High-pressure activation for the solvent- and catalyst-free syntheses of heterocycles, pharmaceuticals and esters.

作者信息

Plasse Kelsey, Wright Valerie, Xie Guoshu, Vlocskó R Bernadett, Lazarev Alexander, Török Béla

机构信息

Department of Chemistry, University of Massachusetts Boston, 100 Morrissey Blvd, Boston, MA, USA.

Pressure BioSciences Inc., 480 Neponset Street, Unit 10B, Canton, MA, USA.

出版信息

Beilstein J Org Chem. 2025 Jul 2;21:1374-1387. doi: 10.3762/bjoc.21.102. eCollection 2025.

Abstract

High hydrostatic pressure (HHP) was found to be an efficient activation method in several catalyst- and solvent-free reactions and has found application for the syntheses of heterocycles and the preparation of active pharmaceutical ingredients (APIs) via acylation and acid- and solvent-free esterification. The reactions were carried out at ambient pressure (control) and under HHP (up to 3.8 kbar) conditions. These representative reactions provided higher yields for the products and HHP enabled truly green processes that are catalyst- and solvent-free, to occur with high yields and producing only non-toxic by-products. A computational study accompanies the experimental data to interpret the outcome of the reactions.

摘要

高静水压(HHP)被发现是几种无催化剂和无溶剂反应中的一种有效活化方法,并且已应用于杂环化合物的合成以及通过酰化反应和无酸无溶剂酯化反应制备活性药物成分(API)。反应在常压(对照)和高静水压(高达3.8千巴)条件下进行。这些典型反应使产物具有更高的产率,并且高静水压使得真正的绿色过程能够在无催化剂和无溶剂的情况下以高收率发生,并且仅产生无毒副产物。一项计算研究结合实验数据来解释反应结果。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f439/12230333/2ccd49dd8343/Beilstein_J_Org_Chem-21-1374-g002.jpg

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