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Updated: Jun 7, 2026

Facile Preparation of 4-Substituted Quinazoline Derivatives
Published on: February 15, 2016
Chemodivergent Approach to 1,2,3-Triazole-Fused Quinazolines
Roman S Tatevosian1, Gennadij V Latyshev1, Yury N Kotovshchikov1
1Chemistry Department, M. V. Lomonosov Moscow State University, Moscow 119991, Russia.
Researchers created a new method for synthesizing triazole-fused quinazolines using cyclization reactions. This efficient process allows for diverse chemical synthesis of these important heterocyclic compounds.
Area of Science:
- Organic Chemistry
- Medicinal Chemistry
- Heterocyclic Chemistry
Background:
- 1,2,3-triazole-fused quinazolines are important heterocyclic scaffolds.
- Efficient synthesis of these compounds is crucial for drug discovery and materials science.
Purpose of the Study:
- To develop a convenient and efficient method for synthesizing 1,2,3-triazole-fused quinazolines.
- To explore the chemodivergent synthesis of related dihydro derivatives.
- To demonstrate potential applications in catalysis.
Main Methods:
- Cyclization of 5-iodotriazoles with pendant sulfonamide moieties.
- Base-promoted C(sp2)-N bond formation via halogen substitution.
- Optimization of base and solvent for chemodivergent outcomes.
Main Results:
- Successful assembly of 1,2,3-triazole-fused quinazolines.
- Chemodivergent synthesis of quinazoline and dihydroquinazoline derivatives.
- Demonstrated utility in Rh-catalyzed denitrogenative amidation reactions.
Conclusions:
- A novel and convenient synthetic route to triazole-fused quinazolines has been established.
- The method allows for controlled synthesis of related dihydro derivatives.
- The synthesized heterocycles show promise in catalytic applications, particularly in amidation reactions.
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