Synthesis of Fluoroquinolones: Revisiting the Grohe Route in DES-Based Media

<b>Background</b>: The development of greener synthetic routes to active pharmaceutical ingredients (APIs) is a key challenge in sustainable chemistry. <b>Methods</b>: In this work, we explored the use of deep eutectic solvents (DESs) in the multi-step synthesis of a fluoroquinolone following the Grohe method. <b>Results</b>: Several steps of the synthetic sequence were successfully carried out using DESs, achieving moderate to good yields, while operating under mild reaction conditions and reducing purification requirements. Overall, the use of DESs led to an overall yield of up to 43%. A comprehensive greenness assessment, combining EcoScale scoring and the GSK and CHEM21 solvent selection guides, confirmed the superior sustainability profile of DESs, reflecting their lower toxicity, biodegradability, and reduced energy demands. <b>Conclusions</b>: These findings establish DESs as promising, eco-friendly alternatives to volatile and hazardous organic solvents for the synthesis of quinolone derivatives, offering a valuable step toward more sustainable pharmaceutical manufacturing.

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Publication Details

Journal
Pharmaceuticals
Published
2026-01-25
DOI
https://doi.org/10.3390/ph19020208
Primary Topic
Ionic liquids properties and applications
Type
article
Field-Weighted Citation Impact
0.00

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article

Synthesis of Fluoroquinolones: Revisiting the Grohe Route in DES-Based Media

Luís Domingues, Ana Rita Jesus, Rúben Neto
Pharmaceuticals
Ionic liquids properties and applications
article

Synthesis of Fluoroquinolones: Revisiting the Grohe Route in DES-Based Media

Luís Domingues, Ana Rita Jesus, Rúben Neto
article en

Abstract

<b>Background</b>: The development of greener synthetic routes to active pharmaceutical ingredients (APIs) is a key challenge in sustainable chemistry. <b>Methods</b>: In this work, we explored the use of deep eutectic solvents (DESs) in the multi-step synthesis of a fluoroquinolone following the Grohe method. <b>Results</b>: Several steps of the synthetic sequence were successfully carried out using DESs, achieving moderate to good yields, while operating under mild reaction conditions and reducing purification requirements. Overall, the use of DESs led to an overall yield of up to 43%. A comprehensive greenness assessment, combining EcoScale scoring and the GSK and CHEM21 solvent selection guides, confirmed the superior sustainability profile of DESs, reflecting their lower toxicity, biodegradability, and reduced energy demands. <b>Conclusions</b>: These findings establish DESs as promising, eco-friendly alternatives to volatile and hazardous organic solvents for the synthesis of quinolone derivatives, offering a valuable step toward more sustainable pharmaceutical manufacturing.

PharmaceuticalsVol. 19(2)
Instituto Português Da Qualidade (PT), Uninova (PT)
Ministério da Ciência, Tecnologia e Ensino Superior, Laboratório Associado para a Química Verde, Fundação para a Ciência e a Tecnologia
Responsible consumption and production
Openalex Percentile: Top 78%
Ionic liquids properties and applications
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Synthesis of Fluoroquinolones: Revisiting the Grohe Route in DES-Based Media — Luís Domingues, Ana Rita Jesus, et al. · Pharmaceuticals (2026) | TGRS Research Map | TGRS