CC BY 4.0 · SynOpen
DOI: 10.1055/a-2407-4709
paper

A convenient synthesis of CHF2O-containing pyrrolidines and related compounds — Perspective building blocks for drug discovery

1   Building Blocks Production, Enamine Ltd, Kyiv, Ukraine (Ringgold ID: RIN376198)
2   Department of Organic Chemistry, Ivan Franko National University of Lviv, Lviv, Ukraine (Ringgold ID: RIN112865)
,
Ivan Virstiuk
1   Building Blocks Production, Enamine Ltd, Kyiv, Ukraine (Ringgold ID: RIN376198)
2   Department of Organic Chemistry, Ivan Franko National University of Lviv, Lviv, Ukraine (Ringgold ID: RIN112865)
,
Daria Menshykova
1   Building Blocks Production, Enamine Ltd, Kyiv, Ukraine (Ringgold ID: RIN376198)
3   Department of Organic Chemistry, National Technical University of Ukraine Igor Sikorsky Kyiv Polytechnic Institute, Kiiv, Ukraine (Ringgold ID: RIN187495)
,
2   Department of Organic Chemistry, Ivan Franko National University of Lviv, Lviv, Ukraine (Ringgold ID: RIN112865)
› Author Affiliations

Fluorine-containing organic molecules, including CHF2O-derivatives, are among the most sought-after in medicinal chemistry. In the current work, a mini-library of 21 compounds with a CHF2O-motif incorporated with azetidine, pyrrolidine (proline), piperidine, 2-azabicyclo[2.2.1]heptane, and 8-azabicyclo[3.2.1]octane cores were synthesized. A multigram scale (10 to 30 g) procedure for synthesizing title compounds from commercially available amino alcohols was studied.



Publication History

Received: 14 July 2024

Accepted after revision: 30 August 2024

Accepted Manuscript online:
04 December 2024

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