SEMINARIOS AREA QUÍMICA ORGÁNICA FBIOYF/IQUIR

SEMINARIO QUÍMICA ORGÁNICA 04-09-23 EXPOSITOR :  Qco. Msc. Javier Cala TÍTULO :   " Descubrimiento y síntesis de Entrectinib, nuevo anticancerígeno 3-aminoindazol " FUENTE :   1) Discovery of Entrectinib: A New 3-Aminoindazole As a Potent Anaplastic Lymphoma Kinase (ALK), c-ros Oncogene 1 Kinase (ROS1), and Pan-Tropomyosin Receptor Kinases (Pan-TRKs) inhibitor Maria Menichincheri et al. J. Med. Chem. 2016 , 59, 7, 3392–3408 https://doi.org/10.1021/acs.jmedchem.6b00064 2) Total Synthesis of Entrectinib with Key Photo-Redox Mediated Cross-Coupling in Flow Morgan J. Cordell, Matt R. Adams, Dr. Jean-François Vincent-Rocan, Dr. John G. Riley Eur. J. Org. Chem. 2022 , e202101143 https://doi.org/10.1002/ejoc.202101143 DÍA, HORA y LUGAR : Lunes 4 de septiembre de 2023, 14:00 h, Aula 18 y virtual. Modalidad virtual, Link :  meet.google.com/hjn-ygro-twf  ( Plataforma MEET GOOGLE) Resumen :  By using photo-redox catalysis in flow the newly marketed drug entrectin...

SEMINARIO QUÍMICA ORGÁNICA 28-08-23 EXPOSITOR : Lic. Gabriel Di Gresia TÍTULO :   " Magic Chloro”: Profound Effects of the Chlorine Atom in Drug Discovery " . FUENTE :  Debora Chiodi and Yoshihiro Ishihara, J. Med. Chem. 2023 , 66 , 5305−5331 . DÍA, HORA y LUGAR : Lunes 28 de agosto de 2023, 14:00 h, Aula 18 y virtual. Modalidad virtual, Link :  meet.google.com/hjn-ygro-twf  ( Plataforma MEET GOOGLE) Resumen :  Chlorine is one of the most common atoms present in small-molecule drugs beyond carbon, hydrogen, nitrogen, and oxygen. There are currently more than 250 FDA-approved chlorine-containing drugs, yet the beneficial effect of the chloro substituent has not yet been reviewed. The seemingly simple substitution of a hydrogen atom (R = H) with a chlorine atom (R = Cl) can result in remarkable improvements in potency of up to 100,000-fold and can lead to profound effects on pharmacokinetic parameters including clearance, half-life, and drug exposure in vivo. Foll...

SEMINARIO QUÍMICA ORGÁNICA 14-08-23 EXPOSITOR : Dr. Sebastián A. Testero TÍTULO :   " Formal Cross-Coupling of Amines and Carboxylic Acids to Form sp3−sp2 Carbon−Carbon Bonds " . FUENTE :   James L. Douthwaite, Ruheng Zhao, Eunjae Shim, Babak Mahjour, Paul M. Zimmerman, and Tim Cernak*,  J. Am. Chem. Soc. 2023 , 145, 10930−10937 . DÍA, HORA y LUGAR : Lunes 14 de agosto de 2023, 14:00 h, Aula 18 y virtual. Modalidad virtual, Link :  meet.google.com/hjn-ygro-twf  ( Plataforma MEET GOOGLE) Resumen :  Amines and carboxylic acids are abundant synthetic building blocks that are classically united to form an amide bond. To access new pockets of chemical space, we are interested in the development of amine−acid coupling reactions that complement the amide coupling. In particular, the formation of carbon−carbon bonds by formal deamination and decarboxylation would be an impactful addition to the synthesis toolbox. Here, we report a formal cross-coupling of alkyl ami...