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

Elisabeth T. Hennessy; Maximilian D. Palkowitz; Josep Sauri; Aaron C. Sather

doi:10.1021/acs.orglett.2c02555

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

Elisabeth T. Hennessy, Maximilian D. Palkowitz, Josep Sauri, Aaron C. Sather

Research output: Indexed journal article › Article › peer-review

4 Citations (Scopus)

Abstract

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.

Original language	English
Number of pages	4
Journal	Organic Letters
Early online date	24 Aug 2022
DOIs	https://doi.org/10.1021/acs.orglett.2c02555
Publication status	Published - 2 Sept 2022
Externally published	Yes

Keywords

Adenosine

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10.1021/acs.orglett.2c02555

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AU - Hennessy, Elisabeth T.

AU - Palkowitz, Maximilian D.

AU - Sauri, Josep

AU - Sather, Aaron C.

PY - 2022/9/2

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AB - 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.

KW - Adenosine

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

Abstract

Keywords

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