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Solid phase parallel synthesis of highly substituted thiophene derivatives and identification of novel phosphodiesterase-4 (PDE-4) inhibitors

✍ Scribed by Yongxin Han; André Giroux; Carole Lépine; France Laliberté; Zheng Huang; Hélène Perrier; Christopher I Bayly; Robert N Young

Publisher: Elsevier Science
Year: 1999
Tongue: French
Weight: 826 KB
Volume: 55
Category: Article
ISSN: 0040-4020
DOI: 10.1016/s0040-4020(99)00686-9

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✦ Synopsis

A versatile protocol for solid phase synthesis of highly substituted thiophene derivatives and their activity against the PDE-4 enzyme are discussed. This protocol employs 3-hydroxymethylthiophene-2-boronic acid (5) as the scaffold and sequential palladium catalyzed cross-coupling reactions as the C-C bond forming step. This methodology allows convenient modification of the thiophene core from three directions, giving rise to structurally diverse derivatives with overall high chemical purity and yield.

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