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专注于绿色合成的可持续方法开发。

A focus on sustainable method development for greener synthesis.

作者信息

Tyler Jasper L, Katzenburg Felix, Glorius Frank

机构信息

Westfälische Wilhelms-Universität Münster, Organisch-Chemisches Institut Corrensstraße 36 48149 Munster Germany

出版信息

Chem Sci. 2023 Jun 29;14(27):7408-7410. doi: 10.1039/d3sc90120c. eCollection 2023 Jul 12.

DOI:10.1039/d3sc90120c
PMID:37449072
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC10337756/
Abstract

Given the current global climate and health challenges, sustainability and cost-effectiveness are becoming unavoidable factors that must be considered in the development of new synthetic methodologies. In a recent publication, Kavthe (R. D. Kavthe, K. S. Iyer, J. C. Caravez and B. H. Lipshutz, , 2023, , 6399, https://doi.org/10.1039/D3SC01699D) have succinctly demonstrated how employing more sustainable methodology can vastly reduce the environmental impact associated with the synthesis of the antimalarial drug candidate MMV688533. The most notable feature of this newly reported synthetic route is the application of aqueous micellar conditions to two Sonogashira coupling reactions that simultaneously improve the yield, catalyst loading and sustainability of these key steps.

摘要

鉴于当前全球气候和健康挑战,可持续性和成本效益正成为新合成方法开发中必须考虑的不可避免的因素。在最近的一篇出版物中,卡夫特(R. D. 卡夫特、K. S. 伊耶、J. C. 卡拉韦兹和B. H. 利普舒茨,《化学科学》,2023年,第6399页,https://doi.org/10.1039/D3SC01699D)简要展示了采用更具可持续性的方法如何能大幅降低与抗疟药物候选物MMV688533合成相关的环境影响。这条新报道的合成路线最显著的特点是将水相胶束条件应用于两个Sonogashira偶联反应,这同时提高了这些关键步骤的产率、催化剂用量和可持续性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e9f6/10337756/45fba23cce66/d3sc90120c-f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e9f6/10337756/45fba23cce66/d3sc90120c-f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e9f6/10337756/45fba23cce66/d3sc90120c-f1.jpg

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J Org Chem. 2024 May 3;89(9):6138-6148. doi: 10.1021/acs.joc.4c00122. Epub 2024 Apr 22.
抗疟药物 MMV688533 具有提供单剂量治愈的潜力,并且具有很高的抗药性障碍。
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