Continuous-Flow Supercritical CO2 Platform for In-Situ Synthesis and Purification of Small Molecules for Drug Discovery,Organic Process Research & Development

当前位置： X-MOL 学术 › Org. Process Res. Dev. › 论文详情

Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)

Continuous-Flow Supercritical CO2 Platform for In-Situ Synthesis and Purification of Small Molecules for Drug Discovery
Organic Process Research & Development ( IF 3.1 ) Pub Date : 2023-02-03 , DOI: 10.1021/acs.oprd.2c00253
Sergio Alcalde ₁ , Raúl Porcar _{1,

2} , María Luz De La Puente ₃ , Graham R. Cumming ₃ , Carlos Mateos ₃ , Pablo García-Losada ₃ , Cristina Anta ₃ , Juan A. Rincón ₃ , Eduardo García-Verdugo ₁

Affiliation

The use of supercritical CO₂ (scCO₂) as an enabling technology paves the way for an efficient in-line integration of the synthesis and purification of organic molecules. The scCO₂ platform presented here provides a streamlined process to produce a diverse family of triazoles, common drug precursors, by 1,3-dipolar copper-catalyzed azide-alkyne cycloaddition (CuAAC, Huisgen reaction), also decreasing the environmental impact by significantly reducing the use of traditional solvents. To further exemplify the potential of this scCO₂ platform, the synthesis and purification of rufinamide, a drug used to treat seizures associated with Lennox–Gastaut syndrome, is also reported.

中文翻译：

用于药物发现的小分子原位合成和纯化的连续流动超临界 CO2 平台

使用超临界 CO ₂ (scCO ₂ ) 作为使能技术为有机分子合成和纯化的高效在线整合铺平了道路。此处介绍的scCO ₂平台提供了一种简化的工艺，通过 1,3-偶极铜催化的叠氮化物-炔烃环加成反应（CuAAC，Huisgen 反应）生产多种三唑类（常见药物前体），同时还通过显着减少对环境的影响使用传统溶剂。_{为了进一步证明这种 scCO 2}平台的潜力，还报道了一种用于治疗与 Lennox-Gastaut 综合征相关的癫痫发作的药物 rufinamide 的合成和纯化。

更新日期：2023-02-03

点击分享查看原文

点击收藏

阅读更多本刊最新论文本刊介绍/投稿指南11