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Updated: Apr 18, 2026

Facile Preparation of 4-Substituted Quinazoline Derivatives
Published on: February 15, 2016
Synthesis of 4-quinolones via a carbonylative Sonogashira cross-coupling using molybdenum hexacarbonyl as a CO source
Linda Åkerbladh1, Patrik Nordeman, Matyas Wejdemar
1Organic Pharmaceutical Chemistry, and §Science for Life Laboratory, Department of Medicinal Chemistry, BMC, Uppsala University , Box-574, SE-751 23 Uppsala, Sweden.
Abstract:
A palladium-catalyzed CO gas-free carbonylative Sonogashira/cyclization sequence for the preparation of functionalized 4-quinolones from 2-iodoanilines and alkynes via two different protocols is described. The first method (A) yields the cyclized products after only 20 min of microwave (MW) heating at 120 °C. The second method (B) is a gas-free one-pot two-step sequence which runs at room temperature, allowing the use of sensitive substituents (e.g., nitro and bromide groups). For both protocols, molybdenum hexacarbonyl was used as a solid source of CO.
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