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99. Microwave-Assisted Synthesis of Substituted 2(1H)-Quinolones as Maxi-K+ Channel Openers
T. Glasnov, W. Stadlbauer, C.O. Kappe, Sci. Pharm., 73 (2),188 (2005).

Abstract:
A novel synthetic strategy for the synthesis of 4-aryl-2(1H)-quinolone compounds for the treatment of male erectile dysfunction is described. Our approach includes a cyclization step, chlorination/hydrolysis, Suzuki C-C coupling, bromination, and finally a Heck reaction, all under microwave conditions. Having optimized the sequence on mg scale a succesfull MW-scale-up to gram quantities with comparable yields was performed.


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