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Communication | Regular issue | Vol 48, No. 11, 1998, pp.2225-2229
Published online, 1st January, 1970
DOI: 10.3987/COM-98-8322
Synthesis of N-Arylrolipram Derivatives - Potent and Selective Phosphodiesterase-IV Inhibitors - by Copper Catalyzed Lactam-Aryl Halide Coupling

Esther Aebischer, Edmond Bacher, F. W. Joachim Demnitz,* Thomas H. Keller, Miriam Kurzmeyer, Marta L. Ortiz, Esteban Pombo-Villar, and Hans-Peter Weber

*Novartis Pharma AG, Preclinical Research, S.350/315, CH-4002 Basel, Switzerland


The copper catalysed coupling of rolipram (1) with a wide variety of aryl halides (2) affords N-arylrolipram derivatives (3), potent and selective phosphodiesterase type-IV inhibitors.