The oxetane ring has evolved as a useful bioisostere for dimethyl and carbonyl groups for the improvement of physiochemical properties of drug candidates. Herein, we report the generation and utilization of highly unstable 3-oxetanyllithium as a hitherto unexplored nucleophile leveraging flash technology. A range of different electrophiles are suitable reaction partners in this protocol, and we demonstrate the utility of this protocol in late-stage pharmaceutical analogue synthesis.
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| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC11041934 | PMC |
| http://dx.doi.org/10.1021/acs.orglett.4c00644 | DOI Listing |
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