Síntesis de heterociclos derivados de boro, mediante el protocolo de la química verde y su evaluación farmacológica

Abstract

In this work, a green approach to produce three sets of boron hybrid heterocyclic esters related to formylphenylboronic acids, is presented and discussed: Hantzsch (1,4-DHP's-B, 6-8 a-c), Biginelli (3,4-DHPM's-B, 9 a-c), and Meldrum (3,4-DHPD's-B, 10-12 a-c). To inside into the three types of esters, above mentioned, the transformations were made among the three regioisomers (ortho, meta, and para) of formylphenylboronic acid 1 a-c, three different β-dicarbonylic compounds 2-4, Meldrum's acid 5, and NH 4 AcO or urea.Related to the Green Chemistry protocol, it is convenient to highlight that a comparative study was performed: evaluating three different modes to activate the reactions (mantle heating as well as infrared and microwave irradiations), resulting microwave irradiation as the best procedure, providing the best yields (17-85 %) with the lower reaction times (15-20 min.); the use of ethanol as solvent (green due to good degradability) was also evaluated; in regard to the use of formylphenylboronic acids, it is worth nothing that they are green compounds, since they are easily degradable by action of enzymes into the liver to boric acid; it is also important to note that the transformations were conducted throughout multicomponent protocols ("one-pot"), being not necessary to isolate the intermediates, that after in situ suffer the corresponding generation of the target products.The products 6-12 a-c were spectroscopically characterized: by 1 H, 13 C, 11 B NMR as well as by EIMS, FAB + MS, HRMS, and infrared spectrophotometric absorption experiments. It is important to mention that the molecules 6-8 a-c and 9 a-c, in their respective FAB + -mode spectra, show adduct-ions related to interactions with the matrix (thioglycerol); these artifacts were invaluable tools to unequivocally characterize the studied molecules.In order to determine how much green are the offered process, a methodology recently described involving the analysis of the twelve Green Chemistry principles was employed; thus in this sense, this work was conveniently evaluated.Finally, a pharmacological screening, for some compounds, about the activity that present over acaricide agents on Rhipicephalus microplus genus tick was also performed; here eleven compounds were evaluated, and larvae eclosion percentage was determined by the Abstract Joel Martínez 4 adults immersion test. It is appropriated to highlight that, the compounds 12d and 12c, have good activity. On the other hand, only the phenylboronic acid showed important activity in larval mortality, when these eleven compounds were evaluated by packet larvae test. In accord to results, these compounds will be considered as potential ixodidae activity. Also, some relaxing activity studies were performed for the 6c, 7c, 8c, and HMOAm (it is 1,4-DHP's-B but with amide residue at 3 and 5 positions

Desarrollo De Un Banco De Control Dinámico Para El Manipulador Zebra 360 Del Ambiente Tecnoacademia-Cucuta

“…El diseño de un banco de control dinámico para robots requiere la asignación directa de un robot, en este caso de estudio, se empleó el manipulador ZEBRA 360 del ambiente de Tecnoacademia-Cúcuta. (Gil Martínez 2008) Se realiza esta investigación con fines académicos, donde se podrá aplicar los conocimientos efectuados en otros robots bajo el seguimiento de la misma metodología y clasificación. Se destaca su implicación en el estudio y desarrollo de la línea de control de robots, con lo que se espera crear competencias personales y permitir el desarrollo del interés en el aula sobre esta rama específica de la robótica.…”