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Molecules 2018, 23(5), 1193; https://doi.org/10.3390/molecules23051193

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

Instituto de Química Rosario, Facultad de Ciencias Bioquímicas y Farmacéuticas, Universidad Nacional de Rosario-CONICET, Suipacha 531, Rosario S2002LRK, Argentina
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Received: 7 May 2018 / Revised: 11 May 2018 / Accepted: 14 May 2018 / Published: 16 May 2018
(This article belongs to the Special Issue Solid Phase Synthesis)
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Abstract

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. View Full-Text
Keywords: diversity oriented synthesis; solid-phase organic synthesis; β-lactam derivatives; olefin metathesis; cholesterol absorption inhibitors diversity oriented synthesis; solid-phase organic synthesis; β-lactam derivatives; olefin metathesis; cholesterol absorption inhibitors
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Méndez, L.; Poeylaut-Palena, A.A.; Mata, E.G. Molecular Diversity by Olefin Cross-Metathesis on Solid Support. Generation of Libraries of Biologically Promising β-Lactam Derivatives. Molecules 2018, 23, 1193.

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