1073375-56-0Relevant academic research and scientific papers
A Catalytic Cross-Olefination of Diazo Compounds with Sulfoxonium Ylides
Neuhaus, James D.,Bauer, Adriano,Pinto, Alexandre,Maulide, Nuno
supporting information, p. 16215 - 16218 (2018/11/23)
A ruthenium-catalysed cross-olefination of diazo compounds and sulfoxonium ylides is presented. Our reaction design exploits the intrinsic difference in reactivity of diazo compounds and sulfoxonium ylides as both carbene precursors and nucleophiles, which results in a highly selective reaction.
Enantioselective conjugate addition of aliphatic thiols to divergently activated electron poor alkenes and dienes
Kowalczyk, Rafa?,Wierzba, Aleksandra J.,Boratyński, Przemys?aw J.,Ba?kowicz, Julia
supporting information, p. 5834 - 5842 (2015/03/30)
Divergently activated double bonds in electron poor 4-oxo-butenoates and (2E,4E)-6-oxo-2,4-dienoates underwent stereoselective and regioselective addition of mercaptans catalyzed by simple Cinchona alkaloids. Application of quinine and quinidine afforded both enantiomers of the 1,4-adducts with respect to the ketone carbonyl group in ees of up to 80%. Single recrystallization of some adducts resulted in further enrichment of up to 99%ee.
Design and synthesis of novel antimicrobials with activity against Gram-positive bacteria and mycobacterial species, including M. tuberculosis
Tiruveedhula, V.V.N. Phani Babu,Witzigmann, Christopher M.,Verma, Ranjit,Kabir, M. Shahjahan,Rott, Marc,Schwan, William R.,Medina-Bielski, Sara,Lane, Michelle,Close, William,Polanowski, Rebecca L.,Sherman, David,Monte, Aaron,Deschamps, Jeffrey R.,Cook, James M.
, p. 7830 - 7840 (2014/01/06)
The alarming increase in bacterial resistance over the last decade along with a dramatic decrease in new treatments for infections has led to problems in the healthcare industry. Tuberculosis (TB) is caused mainly by Mycobacterium tuberculosis which is responsible for 1.4 million deaths per year. A world-wide threat with HIV co-infected with multi and extensively drug-resistant strains of TB has emerged. In this regard, herein, novel acrylic acid ethyl ester derivatives were synthesized in simple, efficient routes and evaluated as potential agents against several Mycobacterium species. These were synthesized via a stereospecific process for structure activity relationship (SAR) studies. Minimum inhibitory concentration (MIC) assays indicated that esters 12, 13, and 20 exhibited greater in vitro activity against Mycobacterium smegmatis than rifampin, one of the current, first-line anti-mycobacterial chemotherapeutic agents. Based on these studies the acrylic ester 20 has been developed as a potential lead compound which was found to have an MIC value of 0.4 μg/mL against Mycobacterium tuberculosis. The SAR and biological activity of this series is presented; a Michael-acceptor mechanism appears to be important for potent activity of this series of analogs.
