Sociedad Química de México A.C.
CONFERENCIA PLENARIA DE LÁSZLÓ KÜRTI,
Se invita a estudiantes, profesores, investigadores e industriales de la Química, a participar en el
52° CONGRESO MEXICANO DE QUÍMICA,
36° CONGRESO NACIONAL DE EDUCACIÓN QUÍMICA
Y LA EXPO QUÍMICA 2017
" La Química nos une"
a celebrarse del 26 al 29 de septiembre 2017, en Puerto Vallarta, Jalisco, México, teniendo como sede Hotel The Westin Resort & Spa Puerto Vallarta
Prof. László Kürti
Department of Chemistry
László Kürti was born and raised in Hungary. He received his Ph.D. under the supervision of A.B. Smith at the University of Pennsylvania. There he authored the now popular textbook/reference book "Strategic Applications of Named Reactions in Organic Synthesis" with Barbara Czakó. Subsequently he was a Damon Runyon Cancer Fellow in the laboratory of E.J. Corey at Harvard University. László is now an Associate Professor of Chemistry at Rice University. The Kürti group focuses on the development of powerful new methods for the expedient enantioselective assembly of highly functionalized biaryls, heterocycles and carbocycles. László is the recipient of an NSF CAREER Award, Fellowship by the Japan Society for the Promotion of Science (JSPS), the 2014 Amgen Young Investigators’ Award as well as the 2015 Biotage Young Principal Investigator Award.
Synthetic organic chemistry is the critical foundation for the medical application of many complex organic molecules (i.e., natural products or drug molecules); it is the only way to produce these complex molecules in sufficient quantities for studies or clinical and commercial use. Moreover, synthetic chemistry enables the design and the preparation of novel drug molecules that can be used to study fundamental biological pathways or change the course of various diseases.
More than three quarters of known organic molecules and the overwhelming majority of currently used drug molecules contain heterocycles, yet the number of highly efficient methods to prepare these types of compounds is surprisingly low. I plan to address this deficiency in my research program, which will have a dual focus. On the one hand, my group will develop novel catalytic enantioselective transformations and apply these reactions for the rapid assembly of various heterocycles and carbocycles. Secondly, these hetero- and carbocyclic motifs are present in numerous natural products with potent biological activities, therefore we will have the opportunity to design and quickly prepare a large number of derivatives and screen them in a variety of assays to identify new drug leads. These newly developed methods will also allow the enantioselective preparation of other highly functionalized compounds that may be utilized for the catalysis of dozens of organic transformations.
My research program does not only seek to develop new and powerful transformations in organic chemistry and enable the synthesis of biologically relevant compounds to aid drug discovery, but it also provides an excellent platform for the education and training of both undergraduate and graduate students. The strongly interdisciplinary environment in the BioScience Research Collaborative (BRC) at Rice University allows my research group to pursue these goals and find many opportunities for fruitful collaboration
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Practical Direct Electrophilic Amination of Olefins and Aromatic Systems
amines and their derivatives are ubiquitous substances since they make up the overwhelming majority of drug molecules, agrochemicals as well as many compounds that are produced by plants and living organisms (i.e., natural products). Aromatic amines appear as substructures in more than one third of drug candidates while aziridines, in which the nitrogen atom is bridged between two carbon atoms, are high-reactive and versatile building blocks for a large variety of functionalized amines. Not surprisingly, organic chemists spend a considerable amount of their time with the synthesis and late-stage functionalization of amines that serve as key chemical building blocks for the preparation of biologically active compounds, especially in medicinal chemistry. There is an urgent need for the development of novel carbon-nitrogen bond-forming methods and reagents that expand the toolbox of synthetic organic chemists and enable the environmentally friendly construction of complex molecular structures using the fewest number of chemical steps and generating the least amount waste.
A highly attractive, but currently underdeveloped, approach is the utilization of weak bonds as a driving force to achieve the rapid formation of much stronger bonds under mild conditions. The Kürti lab has been exploring several fundamentally new strategies for the transition-metal-free direct: (i) primary amination of arylmetals such as aryl Grignard reagents and arylboronic acids; (ii) intramolecular C(sp2)-H amination of arenes; (iii) double arylation of a suitable nitrogen linchpin reagents to afford N,N-diarylamines. We have also discovered, in collaboration with the Falck (UTSW) and Ess labs (BYU), the Rh-catalyzed direct N-H/N-alkyl aziridination of olefins as well as the primary (-NH2) and NH-alkyl amination of arenes, transformations that eluded synthetic chemists for decades. In-depth experimental and computational studies have already identified the critical factors required for efficient olefin NH- and N-alkyl aziridination as well as direct arene primary amination and led to the development of practical and chemoselective aminating agents.