Litcius/Paper detail

Benzylic C–H isocyanation/amine coupling sequence enabling high-throughput synthesis of pharmaceutically relevant ureas

Sung‐Eun Suh, Leah E. Nkulu, Shishi Lin, Shane W. Krska, Shannon S. Stahl

2021Chemical Science48 citationsDOIOpen Access PDF

Abstract

-fluorobenzenesulfonimide]. The isocyanate products may be used without isolation or purification in a subsequent coupling step with primary and secondary amines to afford hundreds of diverse ureas. These results provide a template for implementation of C-H functionalization/cross-coupling in drug discovery.

Topics & Concepts

SelectivityCombinatorial chemistryReagentCatalysisCoupling (piping)Amine gas treatingThroughputChemistrySequence (biology)Organic chemistryMaterials scienceComputer scienceWirelessBiochemistryMetallurgyTelecommunicationsCatalytic C–H Functionalization MethodsSynthesis and Catalytic ReactionsCyclopropane Reaction Mechanisms