Work

Deprotective Alkylation: A Platform for Alcohol‐to‐Amine Interconversion Using Nonafluoromesitylenesulfonamides

Year: 2026

Type: article

Abstract: The direct conversion of alcohols to amines remains a long-standing challenge in organic synthesis. In this study, we report a practical approach, based on the concept of deprotective functionalization, for the stereospecific synthesis of secondary and tertiary amines in high yields directly from alcohol precursors and Nms-amides. Our approach exploits the distinct reactivity of Nms-amides and has the potential to reduce step count in synthetic sequences. The versatility of the method is showcased through applications in late-stage functionalization and the efficient preparation of isotopically labeled compounds.

Source: Angewandte Chemie International Edition

DOI: 10.1002/anie.3520541

Authors: Jakub Brześkiewicz, Kunj Kapur, Boris Maryasin, Nuno Maulide

Institution: University of Vienna

Language: English

Topic: Fluorine in Organic Chemistry

Subfield: Pharmaceutical Science

Field: Pharmacology, Toxicology and Pharmaceutics

Domain: Life Sciences

Open Access status: hybrid

Estimated APC paid: $5,510

Funders: European Commission, Austrian Science Fund