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Selective N-alkylation of azoles via anion-binding catalysis

US National Institute of General Medical Sciences grant open #nih-1F32GM156017-01A1

Summary

Project Summary Azoles are ubiquitous amongst bioactive molecules, present in approximately one third of commercial pharmaceuticals. However, selective preparation of N-alkylated azoles is an outstanding synthetic challenge. As a result, stereochemistry and N-regioselectivity are often achieved through the separation of isomeric mixtures or introduced during de novo ring synthesis. This approach creates a significant synthetic barrier when evaluating analogs of bioactive molecules during drug discovery campaigns. Therefore, a selective method to install alkyl fragments on existing azoles is po

Selective N-alkylation of azoles via anion…
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