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Two-Component Coupling of Carbodiimides and Hydrazides Provides Convergent Access to Biologically Active Compounds.

Elisabeth T HennessyMaximilian D PalkowitzJosep SauríAaron C Sather
Published in: Organic letters (2022)
A novel, convergent synthesis of aminotriazoloquinazolines is reported. These heterocycles are reliably prepared via a "click-like" reaction between readily available aryl carbodiimides and acyl or aryl hydrazides. Such products are of particular interest with respect to their inhibitory activity against the A 2A and A 2B adenosine receptors, and the title two-component coupling reaction has greatly accelerated the discovery of potent/selective chemical matter in this space.
Keyphrases
  • electron transfer
  • room temperature
  • small molecule
  • high throughput
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  • protein kinase
  • ionic liquid