Deprotective Lossen rearrangement: a direct and general transformation of Nms-amides to unsymmetrical ureas

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Abstract

Ureas stand out as potent pharmacophores in drug development, rendering them a prime focus for synthesis. Herein, we present an appealing entry point for urea synthesis from protected amines (Nms-amides) and relying on a Lossen-type rearrangement process as an elegant example of deprotective functionalisation. The method developed exhibits an exceptionally broad tolerance towards various protected amines, encompassing numerous drug derivatives, and delivers high reaction yields.

Original languageEnglish
Pages (from-to)15799-15803
Number of pages5
JournalChemical Science
Volume15
Issue number38
Early online date10 Sep 2024
DOIs
Publication statusPublished - 10 Sep 2024

Austrian Fields of Science 2012

  • 104015 Organic chemistry

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