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Multicapillary Flow Reactor: Synthesis of 1,2,5-Thiadiazepane 1,1-Dioxide Library Utilizing One-Pot Elimination and Inter-/Intramolecular Double aza-Michael Addition Via Microwave-Assisted, Continuous-Flow Organic Synthesis (MACOS).
Journal of Flow Chemistry ( IF 2.0 ) Pub Date : 2012-10-01 , DOI: 10.1556/jfc-d-12-00015
Farman Ullah 1 , Qin Zang , Salim Javed , Aihua Zhou , Christopher A Knudtson , Danse Bi , Paul R Hanson , Michael G Organ
Affiliation  

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.

中文翻译:


多毛细管流动反应器:通过微波辅助连续流有机合成 (MACOS),利用一锅消除和分子间/分子内双氮杂迈克尔加成合成 1,2,5-噻二氮卓 1,1-二氧化物库。



微波辅助连续流有机合成 (MACOS) 方案,用于合成功能化 1,2,5-噻二氮杂卓 1,1-二氧化物库,采用一锅消除和分子间/分子内双氮杂迈克尔加成策略被报道。 MACOS 中的优化方案用于横向扩展,并使用多毛细管流动反应器进一步扩展用于文库生产。以 100 至 300 毫克规模制备了 50 个成员的 1,2,5-噻二氮卓 1,1-二氧化物文库,总收率在 50 至 80% 之间,通过质子核磁共振 (1H -NMR)光谱。
更新日期:2012-10-01
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