Continuous-Flow Supercritical CO2 Platform for In-Situ Synthesis and Purification of Small Molecules for Drug Discovery
Sergio Alcalde
1
,
Raúl Porcar
1, 2
,
Raul 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
1
Departamento de Química Inorgánica y Orgánica, Grupo de Química Sostenible y Supramolecular, Universidad Jaume I, E-12071 Castellón, Spain
|
2
Departamento de Química Orgánica y Bio-Orgánica, Facultad de Ciencias, UNED, E-28040 Avda. Esparta s/n, Las Rozas, 28232 Madrid, Spain
|
3
Centro de Investigación Lilly S.A., Avda. de la Industria 30, Alcobendas, Madrid 28108, Spain
|
Publication type: Journal Article
Publication date: 2023-02-03
scimago Q1
wos Q1
SJR: 0.865
CiteScore: 5.4
Impact factor: 3.5
ISSN: 10836160, 1520586X
Organic Chemistry
Physical and Theoretical Chemistry
Abstract
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.
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Total citations:
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Citations from 2025:
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GOST
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Alcalde S. et al. Continuous-Flow Supercritical CO2 Platform for In-Situ Synthesis and Purification of Small Molecules for Drug Discovery // Organic Process Research and Development. 2023. Vol. 27. No. 2. pp. 276-285.
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Alcalde S., Porcar R., Porcar R., De La Puente M. L., Cumming G. R., Mateos C., García-Losada P., Anta C., Rincón J. A., García-Verdugo E. Continuous-Flow Supercritical CO2 Platform for In-Situ Synthesis and Purification of Small Molecules for Drug Discovery // Organic Process Research and Development. 2023. Vol. 27. No. 2. pp. 276-285.
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RIS
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TY - JOUR
DO - 10.1021/acs.oprd.2c00253
UR - https://pubs.acs.org/doi/10.1021/acs.oprd.2c00253
TI - Continuous-Flow Supercritical CO2 Platform for In-Situ Synthesis and Purification of Small Molecules for Drug Discovery
T2 - Organic Process Research and Development
AU - Alcalde, Sergio
AU - Porcar, Raúl
AU - Porcar, Raul
AU - De La Puente, María Luz
AU - Cumming, Graham R
AU - Mateos, Carlos
AU - García-Losada, Pablo
AU - Anta, Cristina
AU - Rincón, Juan A.
AU - García-Verdugo, Eduardo
PY - 2023
DA - 2023/02/03
PB - American Chemical Society (ACS)
SP - 276-285
IS - 2
VL - 27
SN - 1083-6160
SN - 1520-586X
ER -
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BibTex (up to 50 authors)
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@article{2023_Alcalde,
author = {Sergio Alcalde and Raúl Porcar and Raul Porcar and María Luz De La Puente and Graham R Cumming and Carlos Mateos and Pablo García-Losada and Cristina Anta and Juan A. Rincón and Eduardo García-Verdugo},
title = {Continuous-Flow Supercritical CO2 Platform for In-Situ Synthesis and Purification of Small Molecules for Drug Discovery},
journal = {Organic Process Research and Development},
year = {2023},
volume = {27},
publisher = {American Chemical Society (ACS)},
month = {feb},
url = {https://pubs.acs.org/doi/10.1021/acs.oprd.2c00253},
number = {2},
pages = {276--285},
doi = {10.1021/acs.oprd.2c00253}
}
Cite this
MLA
Copy
Alcalde, Sergio, et al. “Continuous-Flow Supercritical CO2 Platform for In-Situ Synthesis and Purification of Small Molecules for Drug Discovery.” Organic Process Research and Development, vol. 27, no. 2, Feb. 2023, pp. 276-285. https://pubs.acs.org/doi/10.1021/acs.oprd.2c00253.