9 documents found, page 1 of 1
Recentes avanços na funcionalização seletiva de quinolinas
Ferreira,Dartagnan S. P.; Murie,Valter E.; Santos,Thiago dos; Vieira,Paulo C.; Clososki,Giuliano C.Heterocyclic compounds form an important and extensive group of organic substances. Among nitrogenous heterocyclic molecules, quinolines stand out for exhibiting attractive chemical and biological properties. These substances can be used as ligands, sensors, luminescent and agrochemical materials. In addition, quinoline-containing compounds can exhibit a wide spectrum of pharmacological properties, allowing the...
Tenofovir Disoproxil Fumarate: New Chemical Developments and Encouraging in vit...
Clososki,Giuliano C.; Soldi,Rafael A.; Silva,Rodrigo M. da; Guaratini,Thais; Lopes,José N. C.; Pereira,Pâmela R. R.; Lopes,João L. C.; Santos,Thiago dosThe recent emergence of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) has led society to live with a serious public health problem. In this sense, repositioning of antiretrovirals has captured the attention of the scientific community. Tenofovir disoproxil fumarate (TDF) is an antiretroviral compound that is used to treat acquired immune deficiency syndrome (AIDS) and hepatitis B. In this short r...
Characterization and in silico Mutagenic Assessment of a New Betahistine Degrad...
Mello,Murilo B. M. de; Oliveira,Antonio A. F. de; Oliveira,Caroline L. de; Ultramari,Mariah A.; Gama,Fernando H. S.; Mascarello,AlessandraCurrently, the pharmaceutical industry devotes great attention to drug degradation products because these compounds can offer risks to patients. A previous degradation study of betahistine (N-α-methyl-2-pyridylethylamine) conducted under different stress conditions detected three main impurities named A, B and C. Degradation products were analyzed by high-resolution mass spectrometry in electrospray source and ...
Ketalization of Ketones to 1,3-Dioxolanes and Concurring Self-Aldolization Cata...
Barbosa,Sandro L.; Ottone,Myrlene; Almeida,Mainara T. de; Lage,Guilherme L. C.; Almeida,Melina A. R.; Nelson,David Lee; Santos,Wallans T. P. dosThe amorphous, mesoporous SiO2-SO3H catalyst with a surface area of 115 m2 g-1 and 1.32 mmol H+ per g was very efficient for the protonation of ketones on a 10% (m/m) basis, and the catalyst-bound intermediates can be trapped by polyalcohols to produce ketals in high yields or suffer aldol condensations within minutes under low-power microwave irradiation. The same catalyst can easily reverse the ketalization r...
Acetaminophen Prodrug: Microwave-Assisted Synthesis and in vitro Metabolism Eva...
Murie,Valter E.; Marques,Lucas M. M.; Souza,Glória E. P.; Oliveira,Anderson R. M.; Lopes,Norberto P.; Clososki,Giuliano C.Propacetamol is an acetaminophen prodrug of intravenous administration used to control fever and pain of perioperative period in multimodal analgesia therapy. After injection, it is completely converted by plasma esterases into N,N-diethylglycine and acetaminophen, its active metabolite whose mechanism of action is the inhibition of prostaglandin synthesis. Herein, we report an improved protocol for the synthes...
Zinc, Lithium and Magnesium Carbenoids: Chemical Properties and Relevant Applic...
Nishimura,Rodolfo H. V.; Murie,Valter E.; Soldi,Rafael A.; Lopes,João L. C.; Clososki,Giuliano C.Carbenoids are a class of highly reactive reagents that play an important role in modern organic synthesis. These species are very similar to singlet state carbenes since they have an ambiphilic character and react by a concerted mechanism allowing stereospecific transformations. Herein, we discuss these and other chemical aspects of zinc, lithium and magnesium carbenoids as well as relevant applications of the...
Application of the Negishi reaction in the synthesis of thiophene-based lignans...
Amaral,Mônica F. Z. J.; Callejon,Daniel R.; Riul,Thalita B.; Baruffi,Marcelo D.; Toledo,Fabiano T.; Lopes,Norberto P.; Clososki,Giuliano C.Lignans represent a well-known group of natural products with anti-protozoal activity. In the literature there are many examples of the anti-parasitic activity of synthetic analogues of lignans containing sulphur bridges. In this work, we have obtained thiophene-based analogues by using a selective and high performance synthetic strategy based on the Negishi cross-coupling reaction. The derivatives were quickly...
A short and efficient enantioselective synthesis of (+) and (-)-(Z)-7,15-hexade...
Clososki,Giuliano C.; Ricci,Luis C.; Costa,Carlos E.; Comasseto,João V.The (R) and the (S) enantiomers of the Z-7,15-hexadecadien-4-olide (4), the sex pheromone of Heptophylla picea, were synthesized. A known lipase-catalysed enantiolactonization in the key step afforded a common precursor for both enantiomers of the pheromone in 92% e.e.
A new approach to the synthesis of (±)-methyl jasmonate and (±)-baclofen via co...
Santos,Alcindo A. dos; Clososki,Giuliano C.; Simonelli,Fabio; Oliveira,Alfredo R. M. de; Marques,Francisco de A.; Zarbin,Paulo H. G.Introduction of a synthon equivalent to a carboxymethyl anion to enones and nitroalkenes, through a 1,4-addition reaction of 2,4,4-trimethyl-2-oxazoline cyanocuprate 3, proved to be an interesting methodology for the synthesis of natural products such as (±)-methyl jasmonate (1) and (±)-baclofen (2).