Fluorinated Radicamine A and B: Synthesis and Glycosidase Inhibition
作者:Yi-Xian Li、Ren Iwaki、Atsushi Kato、Yue-Mei Jia、George W. J. Fleet、Xuan Zhao、Min Xiao、Chu-Yi Yu
DOI:10.1002/ejoc.201501453
日期:2016.3
Fluorinated derivatives of radicamine A and radicamineB have been synthesized from D-arabinose-derived cyclic nitrone. Structure–activity relationship studies showed that glycosidaseinhibition of these fluorinated derivatives was significantly influenced by the position of the fluorine atom. C-7 or C-11 fluorination of the aromatic ring decreased α-glucosidase inhibition of the derivatives, whereas
已经从 D-阿拉伯糖衍生的环硝酮合成了 radicamine A 和 radicamine B 的氟化衍生物。构效关系研究表明,这些氟化衍生物的糖苷酶抑制受到氟原子位置的显着影响。芳环的 C-7 或 C-11 氟化降低了衍生物对 α-葡萄糖苷酶的抑制作用,而 C-8 或 C-10 氟化保留了糖苷酶抑制活性。
synthesis of fluorinated arenes by the iron-mediated fluorination of potassium aryltrifluoroborates with Selectfluor® and potassiumfluoride is described. The fluorination reaction uses commercially available reagents and without requiring the addition of exogenous ligands. Fluorinated compounds were obtained in moderate to good yields under mild reaction conditions. The synthesis of fluorinated arenes
New Chiral Sulfoxide Ligands Possessing a Phosphano or Phosphanoamino Functionality in Palladium-Catalyzed Asymmetric Allylic Nucleophilic Substitution Reactions
New chiral sulfoxide ligands possessing a phosphano or phosphanoamino functionality as an alternative coordinating element were developed, and their usefulness was demonstrated by applying them to palladium-catalyzedasymmetricallylic nucleophilic substitutionreactions. The structure of the catalyst precursor coordinated by the chiral phosphino sulfoxide was determined by X-ray crystallographic analysis
[3+2]Cycloadditionreaction of lithium trimethylsilyldiazomethane with benzynes, generated from halobenzenes, gave the corresponding 3-trimethylsilylindazoles in good to moderate yields.