Browsing by Author "Puerto Galvis, Carlos Eduardo"

Now showing 1 - 4 of 4
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    Cantharidin-Based Small Molecules as Potential Therapeutic Agents
    (2013) Puerto Galvis, Carlos Eduardo; Vargas Méndez, Leonor Yamile; Kouznetsov, Vladimir V.
    Chemical and pharmacological information on cantharidin-based small molecules was analyzed. The review summarizes new facts about blister beetles’ metabolites for the period 2006–2012. General synthetic approaches to cantharidin-based small molecules as well as their chemical transformations and biological activities related to cantharidin, norcantharidin, cantharidimide, and norcantharimide analogs, especially their inhibitory activity of phosphoprotein phosphatases in cancer treatment, were discussed in this mini review, which could help to design new small molecule modulators for other biological models.
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    Gd(OTf)3-catalyzed synthesis of geranyl esters for the intramolecular radical cyclization of their epoxides mediated by titanocene (III)
    (2015) García Santos, William H.; Puerto Galvis, Carlos Eduardo; Kouznetsov, Vladimir V.
    A selective and mild method for the esterification of a variety of carboxylic acids with geraniol is developed. We demonstrated that the use of triphenylphosphine, I2, 2-methylimidazole or imidazole and a catalytic amount of Gd(OTf)3 resulted to be more active than the previous protocols, providing a 16-membered library of geranyl esters in higher yields and in shorter reaction times. The use of essential oil of palmarosa (Cymbopogon martinii), enriched with geraniol, as a raw material for the synthesis of the target compounds complemented and proved how sustainable and eco-friendly this protocol is. Finally, the selective 6,7-epoxidation of the obtained geranyl esters led us to study their regio-controlled radical cyclization mediated by titanocene(III) for the synthesis of novel (8-hydroxy-9,9-dimethyl-5-methylene cyclohexyl)methyl esters in moderate yields and with excellent stereoselectivities.
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    Síntesis de nuevos derivados del eugenol con actividad dual para el tratamiento de la enfermedad de Alzheimer
    (2014) Lizarazo Muñoz, Juan Camilo; Vargas Méndez, Leonor Yamile; Puerto Galvis, Carlos Eduardo
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    Yb(OTf)3-Catalyzed Bromination Reactions of Natural Product-like N-Benzyl Cinnamamides: A Facile Route to Diverse N-Substituted Amides of Pharmacological Interest
    (2013) Puerto Galvis, Carlos Eduardo; Hernandez Barajas, José G.; Kouznetsov, Vladimir V.
    Diverse natural product-like N-benzyl cinnamamides were prepared by condensation of trans-cinnamic acid with substituted benzylamines in the presence of boric acid as catalyst. The further evaluation of this amides as a substrates of the bromo-arylation reaction, in the presence of N-bromosuccinimide (NBS) as the halogen source and under the catalysis of Yb(OTf)3, generate a different types of N-substituted amides: N-aryl 2,3-dibromopropanamides, N-(2-bromobenzyl) cinnamamides and tetrahydro-2-benzazepin-3-one as a new molecules. Here we discuss the formation of these main products on the basis of the electronic nature of the substituents present in the N-benzyl aromatic ring of the prepared cinnamamides.