Continuous flow generation of highly reactive organometallic intermediates: a recent update

M Spennacchio, P Natho, M Andresini… - Journal of Flow …, 2024 - Springer
Reactive organometallic intermediates present a distinct opportunity for the creation of novel
carbon-carbon and carbon-heteroatom bonds. Whereas their utility in synthesis is well …

Quest for a cure: potential small-molecule treatments for COVID-19, part 2

DL Hughes - Organic Process Research & Development, 2021 - ACS Publications
During the first year of the outbreak of the COVID-19 pandemic, many drugs and drug
candidates have been evaluated as treatment options. None yet has proved to be an …

Continuous Flow C-Glycosylation via Metal–Halogen Exchange: Process Understanding and Improvements toward Efficient Manufacturing of Remdesivir

T von Keutz, JD Williams, CO Kappe - Organic Process Research …, 2020 - ACS Publications
As remdesivir is the first approved treatment for COVID-19 (SARS-CoV-2), its production is
likely to be of vital importance in the near future. Continuous flow processing has been …

Flash Chemistry Approach to Organometallic C-Glycosylation for the Synthesis of Remdesivir

T von Keutz, JD Williams, CO Kappe - Organic Process Research …, 2021 - ACS Publications
In a rapidly changing environment, such as the current COVID-19 pandemic, continuous
flow reactors bear the potential to increase the production of urgently needed active …

Copper-catalyzed one-pot synthesis of quinazolinones from 2-nitrobenzaldehydes with aldehydes: application toward the synthesis of natural products

S Sahoo, S Pal - The Journal of Organic Chemistry, 2021 - ACS Publications
A novel, efficient, and atom-economical approach for the construction of quinazolinones
from 2-nitrobenzaldehydes has been unveiled via copper-catalyzed nitrile formation …

Cyanoamidine cyclization approach to remdesivir's nucleobase

RR Knapp, V Tona, T Okada, R Sarpong… - Organic letters, 2020 - ACS Publications
We report an alternative approach to the unnatural nucleobase fragment seen in remdesivir
(Veklury). Remdesivir displays broad-spectrum antiviral activity and is currently being …

Evolution of the synthesis of Remdesivir. classical approaches and most recent advances

DF Vargas, EL Larghi, TS Kaufman - ACS omega, 2021 - ACS Publications
The broad-spectrum antiviral Remdesivir, a monophosphate nucleoside analogue prodrug
(ProTide), was repurposed. In May 2020, it received emergency approval by the FDA, being …

Stereochemical Editing via Coupled Epimerization and Optical Resolution to Sustainably Manufacture a Key Adagrasib Building Block

DR Snead, S Roshandel, C Chen - Organic Process Research & …, 2023 - ACS Publications
Epimerization and recycling of an unwanted piperazine stereoisomer enabled a more
sustainable, concise, and high-yielding synthesis of a chiral adagrasib building block. The …

Catalytic asymmetric synthesis of carbocyclic C-nucleosides

S Mishra, FCT Modicom, CL Dean… - Communications …, 2022 - nature.com
Access to carbocyclic C-nucleosides (CC-Ns) is currently restricted. The few methods
available to make CC-Ns suffer from long syntheses and poor modularity, hindering the …

Biocatalysis in the swiss manufacturing environment

K Hecht, HP Meyer, R Wohlgemuth, R Buller - Catalysts, 2020 - mdpi.com
Biocatalysis has undergone a remarkable transition in the last two decades, from being
considered a niche technology to playing a much more relevant role in organic synthesis …