Two-Component Coupling of Carbodiimides and Hydrazides Provides Convergent Access to Biologically Active Compounds, by Elisabeth T. Hennessy, Maximilian D. Palkowitz, Josep Saurí, and Aaron C. Sather. Org. Lett. 2022, 24, 34, 6331–6334. https://doi.org/10.1021/acs.orglett.2c02555
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 A2A and A2B adenosine receptors, and the title two-component coupling reaction has greatly accelerated the discovery of potent/selective chemical matter in this space.
Structure Elucidation by NMR 