Ötvös Sándor B, Hsieh Chi-Ting, Wu Yang-Chang, Li Jih-Heng, Chang Fang-Rong, Fülöp Ferenc
Institute of Pharmaceutical Chemistry, University of Szeged, Eötvös u. 6, H-6720 Szeged, Hungary.
MTA-SZTE Stereochemistry Research Group, Hungarian Academy of Sciences, Eötvös u. 6, H-6720 Szeged, Hungary.
Molecules. 2016 Mar 7;21(3):318. doi: 10.3390/molecules21030318.
Flow chemistry-based syntheses of deuterium-labeled analogs of important antidiabetic chalcones were achieved via highly controlled partial C≡C bond deuteration of the corresponding 1,3-diphenylalkynones. The benefits of a scalable continuous process in combination with on-demand electrolytic D2 gas generation were exploited to suppress undesired over-reactions and to maximize reaction rates simultaneously. The novel deuterium-containing chalcone derivatives may have interesting biological effects and improved metabolic properties as compared with the parent compounds.
通过对相应的1,3-二苯基炔酮进行高度可控的部分C≡C键氘代反应，实现了基于流动化学的重要抗糖尿病查耳酮氘代类似物的合成。利用可扩展连续过程与按需电解产生D2气体相结合的优势，抑制了不期望的过度反应并同时最大化反应速率。与母体化合物相比，新型含氘查耳酮衍生物可能具有有趣的生物学效应和改善的代谢特性。
