Ross D. Jansen-van Vuuren (Author), Rahul Vohra (Author)

Abstract

Baricitinib, typically applied as a treatment for rheumatoid arthritis, has recently attracted the attention of clinicians and researchers as a potential treatment for COVID-19. Naturally, there has been a need for the preparation of the isotope-labelled analogue of baricitinib to probe the pharmacokinetics of baricitinib in this new role. As such, we have developed a simple synthetic route to deuterated [$^2$H$_5$]baricitinib, facilitating its formation over four steps and in a 29% overall yield based on starting [$^2$H$_5$]ethanethiol (19% if we start with [$^2$H$_5$]bromoethane instead). A critical component of the overall process involves the synthesis of [$^2$H$_5$]ethanesulfonyl chloride, and we describe in detail the two routes that were explored to optimize this step.

Keywords

baricitinib;COVID-19;devteracija;označevanje z devterijem;SARS-CoV-2;izotopolog;deuteration;deuterium-labelled;isotopologue;

Data

Language: English
Year of publishing:
Typology: 1.01 - Original Scientific Article
Organization: UL FKKT - Faculty of Chemistry and Chemical Technology
UDC: 547.1.057:615
COBISS: 101564163 Link will open in a new window
ISSN: 1099-1344
Views: 92
Downloads: 42
Average score: 0 (0 votes)
Metadata: JSON JSON-RDF JSON-LD TURTLE N-TRIPLES XML RDFA MICRODATA DC-XML DC-RDF RDF

Other data

Secondary language: Slovenian
Secondary keywords: baricitinib;COVID-19;devteracija;označevanje z devterijem;SARS-CoV-2;izotopolog;
Type (COBISS): Article
Pages: str. 156-161
Volume: ǂVol. ǂ65
Issue: ǂiss. ǂ6
Chronology: 30 May 2022
DOI: 10.1002/jlcr.3969
ID: 15437282
Recommended works:
, no subtitle data available
, no subtitle data available
, lessons from autopsy
, (diplomsko delo)
, immunolabelling as indisputable proof of SARS-CoV-2 virions in infected tissue