Authors:Farman Ullah, Qin Zang, Salim Javed, Aihua Zhou, Christopher A. Knudtson, Danse Bi, Paul R. Hanson, and Michael G. Organ
A microwave-assisted, continuous-flow organic synthesis (MACOS) protocol for the synthesis of functionalized 1,2,5-thiadiazepane 1,1-dioxide library, utilizing a one-pot elimination and inter-/intramolecular double aza-Michael addition strategy is reported. The optimized protocol in MACOS was utilized for scale-out and further extended for library production using a multicapillary flow reactor. A 50-member library of 1,2,5-thiadiazepane 1,1-dioxides was prepared on a 100- to 300-mg scale with overall yields between 50 and 80% and over 90 % purity determined by proton nuclear magnetic resonance (1H-NMR) spectroscopy.
Authors:Michael G. Organ, Paul R. Hanson, Alan Rolfe, Thiwanka B. Samarakoon, and Farman Ullah
The generation of stereochemically rich benzothiaoxazepine-1,1´-dioxides for enrichment of high-throughput screening collections is reported. Utilizing a microwave-assisted, continuous-flow organic synthesis platform (MACOS), scale-out of core benzothiaoxazepine-1,1´-dioxide scaffolds has been achieved on multigram scale using an epoxide opening/SNAr cyclization protocol. Diversification of these sultam scaffolds was attained via a microwave-assisted intermolecular SNAr reaction with a variety of amines. Overall, a facile, two-step protocol generated a collection of benzothiaoxazepine-1,1´-dioxides possessing stereochemical complexity in rapid fashion, where all eight stereoisomers were accessed from commercially available starting materials.
microwave-assisted, continuous-flow organic synthesis (MACOS) ” F. Ullah , Q. Zang , S. Javed , P. Porubsky , B. Neuenswander , G. H. Lushington , P. R. Hanson , M. G. Organ Synthesis 2012 , 44 , 2547 – 2554 .
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to the 12th century: Excerto do pacto de Gomes Pais e Ramiro Pais (IAN/TT, Mitra de Braga, maço 1, n. 26/A) date: between 1173 and 1175; cf. SOUTO CABO, J. A.: Documentos Galego-portugueses dos séculos XII e XIII . Coruña 2008 - and Notĩcia de
. Cosford Journal of Flow Chemistry 2011 , 1 , 28 – 31 .
“ Accessing stereochemically rich sultams via microwave-assisted, continuous-flow organic synthesis (MACOS) scale-out ” M. G. Organ , P. R. Hanson , A. Rolfe , T. B
Authors:Anja Dörschug, Julian Schwanbeck, Andreas Hahn, Anke Hillebrecht, Sabine Blaschke, Uwe Groß, Markus M. Heimesaat, Hagen Frickmann, and Andreas E. Zautner
sum testing and binary logistic regression. Those calculations were performed applying the software Stata/IC 15.1 for macOS 64-bit Intel (College Station, Texas, USA). Specificity of the serological assays was determined with the serum samples from the