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Synfacts 2006(7): 0637-0637  
DOI: 10.1055/s-2006-941826
Synthesis of Natural Products and Potential Drugs
© Georg Thieme Verlag Stuttgart · New York

Synthesis of (±)-Rolipram

Contributor(s): Philip Kocienski
K. Tonogaki, K. Itami*, J.-I. Yoshida*
Kyoto University and Nagoya University, Japan
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Publikationsverlauf

Publikationsdatum:
22. Juni 2006 (online)

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Significance

Rolipram is a selective inhibitor of phosphodiesterase-4. It is an antiinflammatory agent and an antidepressant. This latest in a long list of syntheses boasts a Pd-catalyzed three-component coupling to generate a vinylboronate intermediate which then undergoes a subsequent Pd-catalyzed carbonylation.