Molecular Diversity by Olefin Cross-Metathesis on Solid Support. Generation of Libraries of Biologically Promising β-Lactam Derivatives

Molecules

ErnestoG. Mata¹  Luciana Méndez¹  AndrésA. Poeylaut-Palena¹ 

[1] Instituto de Química Rosario, Facultad de Ciencias Bioquímicas y Farmacéuticas, Universidad Nacional de Rosario-CONICET, Suipacha 531, Rosario S2002LRK, Argentina;

关键词: diversity oriented synthesis;    solid-phase organic synthesis;    β-lactam derivatives;    olefin metathesis;    cholesterol absorption inhibitors;   

DOI  :  10.3390/molecules23051193

来源: DOAJ

【 摘 要 】

The application of the reagent-based diversification strategy for generation of libraries of biologically promising β-lactam derivatives is described. Key features are the versatility of the linker used and the cross-metathesis functionalization at the cleavage step. From an immobilized primary library, diversity was expanded by applying different cleavage conditions, leading to a series of cholesterol absorption inhibitor analogues together with interesting hybrid compounds through incorporation of a chalcone moiety.

【 授权许可】

Unknown