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A series of penicillide analogues, with modifications at C‐3 and C‐9 positions, are synthesized as potential cholesteryl ester transfer protein (CETP) inhibitors. The preliminary in vitro inhibition assay provided some valuable structure‐activity relationship information about penicillide.

Synthesis of Imidazo[1,2-a]pyridines via Three-Component Reaction of 2-Aminopyridines, Aldehydes and Alkynes. -The novel Cu-catalyzed approach tolerates a variety of functionalities at the substrates. However, in some cases no transformation is possible. -(LIU, P.; FANG, L.-S.; LEI*, X.; LIN, G.-Q.; Tetrahedron Lett. 51 (2010) 35, 4605-4608,

A convergent approach to dibenzodioxocinones was explored, thereby racemic penicillide ((±)‐1a) could be obtained in 13 steps in 4.2% overall yield, based on 5‐amino‐2‐methylphenol (5) (Schemes 2–4).

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