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Reagent for the Synthesis of gem-Disubstituted Cyclopropanes
Cyclopropanes are important building blocks used in drug discovery research.1) Incorporation of cyclopropane moiety is known to not only improve metabolic stability and binding to target proteins through the conformation fixation, but also to adjust pKa and lipophilicity.
Cyclopropane-1,1-diboronic acid bis(pinacol) ester (1) can be utilized in the Suzuki-Miyaura coupling with aryl bromides to synthesize tertiary arylcyclopropylboronic esters.2) When aryl moiety is a phenyl group, the tertiary arylcyclopropylboronic esters can be converted to arylcyclopropyltrifluoroborate salts with potassium hydrogenfluoride, and then converted to gem-disubstituted cyclopropanes by the subsequent Suzuki-Miyaura coupling.
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References
- 1) The “Cyclopropyl Fragment” is a Versatile Player that Frequently Appears in Preclinical/Clinical Drug Molecules
- 2) A Modular Approach to the Synthesis of gem-Disubstituted Cyclopropanes
