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Synfacts 2011(5): 0473-0473  
DOI: 10.1055/s-0030-1259771
Synthesis of Natural Products and Potential Drugs
© Georg Thieme Verlag Stuttgart ˙ New York

Synthesis of (R)-Baclofen and (R)-Rolipram

Contributor(s): Philip Kocienski
C. Shao, H.-J. Yu, N.-Y. Wu, P. Tian, R. Wang, C.-G. Feng*, G.-Q. Lin*
Shanghai Institute of Organic Chemistry and Lanzhou University, P. R. of China
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Publication History

Publication Date:
15 April 2011 (online)

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Significance

Short asymmetric syntheses of (R)-(-)-rolipram and (R)-(-)-baclofen illustrate the utility of a rhodium-catalyzed conjugate addition of arylboronic acids to α,β-unsaturated-δ-lactams using the chiral diene C as a ligand. A further eleven arylboronic acids were added to lactam B to illustrate the scope of the reaction.