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CC BY 4.0 · SynOpen 2024; 08(04): 247-258
DOI: 10.1055/s-0040-1720142
DOI: 10.1055/s-0040-1720142
paper
A Convenient Synthesis of CHF2O-Containing Pyrrolidines and Related Compounds — Prospective Building Blocks for Drug Discovery
The authors greatly thank the Ministry of Education and Science of Ukraine and the Simons Foundation (Award Number 1290588) for their support.
Abstract
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 was synthesized. A multigram scale (10–30 g) procedure for synthesizing the title compounds from commercially available amino alcohols was studied.
Key words
fluorine - difluoromethoxy group - azetidine - pyrrolidine - proline - piperidine - building blocksSupporting Information
- Supporting information for this article is available online at https://doi.org/10.1055/s-0040-1720142.
- Supporting Information
Publication History
Received: 14 July 2024
Accepted after revision: 30 August 2024
Article published online:
14 October 2024
© 2024. The Author(s). This is an open access article published by Thieme under the terms of the Creative Commons Attribution License, permitting copying and reproduction so long as the original work is given appropriate credit. Contents may not be used for commercial purposes or adapted, remixed, transformed or built upon. (https://creativecommons.org/licenses/by/4.0/)
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