H2020Индивидуална стипендия2020–2022

FI4P · Flow and Iron for Pharma

„Хоризонт 2020“ — Действия „Мария Склодовска-Кюри“

Период: 2020-03-16 → 2022-05-17
Финансиране от ЕС: 166 320 €
Участници: 1
Схема: MSCA-IF-EF-ST

Линиите свързват координатора с партньорите.

Накратко на български

Желязото като катализатор в процеси на непрекъснат поток се тества за създаване на химични структури, използвани в лекарствата. Автоматизирането на тези реакции подобрява точността на опитите и намалява излагането на опасни вещества.

Този кратък обзор е генериран от изкуствен интелект

Кратко обяснение, генерирано от езиков модел по текста на CORDIS. Оригиналът е по-долу.

Резултати накратко

Flow and Iron for Pharma

Synthetic chemistry must provide more and more sustainable methods to build the chemical structures needed from materials to life sciences. Transition metal catalysed cross-couplings have become a versatile tool for the organic chemist, and in this context we focused on using iron, a metal with low toxicity, high abundance and sometimes unique reactivity. To control the reactivity of the organometallic building blocks used in these cross-coupling reactions, we decided to leverage the advantages of continuous flow chemistry. Flow technology goes beyond transposing batch chemistry to flow reactors: it can enable unique process conditions and allow precise spatiotemporal control, while reducing the energy required to run processes thanks to efficient heat transfer properties. Over the course of the Action, an extensive optimisation of reaction conditions was carried out, with the aim to develop protocols of interest to the discovery and manufacture of pharmaceuticals. Due to results of limited synthetic utility, we decided to work on improving our discovery process and implement an automated flow chemistry platform. This allowed us to streamline optimisation protocols, improve experimental reproducibility and reduce exposure to hazardous chemicals. The interest of our in-house automated platform has been validated during the Action, and we expect its continued use for the development of further reaction conditions in our laboratory will eventually inspire others to adopt automation technology in synthetic chemistry.

Текст от CORDIS, на английски · Данни: CORDIS, © Европейски съюз

Цел на проекта

The demand for sustainable methods to build chemical bonds has led to the rise of catalytic reactions, especially using abundant and benign metals. In this context, iron has emerged as a powerful catalyst to mediate various transformations including cross-couplings between (pseudo)halide electrophilic partners and organometallic nucleophiles, usually Grignard reagents.We aim to develop a modular and versatile Flow-enabled Iron-catalysed cross-coupling protocol for Pharmaceutical applications (FI4P), leveraging the unique properties of flow chemistry to implement cross-couplings between organolithium derivatives and electrophiles. Building on the significant expertise of the academic host in this field, we will seek to harness flow technology to exert spatiotemporal control over reactive intermediates, thus ensuring the functionalisation of halide precursors with reactive lithium organyls generated in situ. The particularly high reaction rates observed in iron-catalysed cross-couplings will allow the incorporation of valuable functional groups usually incompatible with organolithium derivatives.This approach will deliver a sustainable method to assemble relevant molecular scaffolds of interest to the pharmaceutical industry. With the involvement of NovAliX, an industrial partner specialised in transferring academic innovations into industrial processes, we will eventually apply our synthetic protocol to the large-scale manufacture of valuable APIs and the generation of a small collection of molecules designed to complement our existing library for Fragment Based Drug Design.

Оригинален текст от CORDIS (на английски).

Участници

UNIVERSITE DE LIEGE · LIEGEКоординаторБелгия