The Carbodiimide Click Reaction Provides Rapid and Conver-gent Access to Aminotriazoloquinazolines

20 June 2022, Version 1
This content is a preprint and has not undergone peer review at the time of posting.

Abstract

A novel, convergent synthesis of aminotriazoloquinazolines is reported. These heterocycles are reliably prepared via a “click” reaction between readily available aryl carbodiimides and acyl hydrazides. Such products are of particular interest with respect to their inhibitory activity against the A2A and A2B adenosine receptors and the title “click” reaction has greatly accelerated the discovery of potent/selective chemical matter in this space.

Keywords

click
medicinal chemistry
discovery process chemistry
synthesis
drug discovery
mechanism

Supplementary materials

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Supporting Information
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Experimental procedures and analytical data for all new compounds
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