Expanding the Balz-Schiemann Reaction: Organotrifluoroborates Serve as Competent Sources of Fluoride Ion for Fluoro-Dediazoniation
作者:Tharwat Mohy El Dine、Omar Sadek、Emmanuel Gras、David M. Perrin
DOI:10.1002/chem.201803575
日期:2018.10.9
The Balz–Schiemann reaction endures as a method for the preparation of (hetero)aryl fluorides yet is eschewed due to the need for harsh conditions or high temperatures along with the need to isolate potentially explosive diazonium salts. In a departure from these conditions, we show that various organotrifluoroborates (RBF3−s) may serve as fluorideion sources for solution‐phase fluoro‐dediazoniation
Synthetic Fosmidomycin Analogues with Altered Chelating Moieties Do Not Inhibit 1-Deoxy-D-xylulose 5-phosphate Reductoisomerase or Plasmodium falciparum Growth In Vitro
作者:René Chofor、Martijn Risseeuw、Jenny Pouyez、Chinchu Johny、Johan Wouters、Cynthia Dowd、Robin Couch、Serge Van Calenbergh
DOI:10.3390/molecules19022571
日期:——
Fourteen new fosmidomycin analogues with altered metal chelating groups were prepared and evaluated for inhibition of E. coli Dxr, M. tuberculosis Dxr and the growth of P. falciparum K1 in human erythrocytes. None of the synthesized compounds showed activity against either enzyme or the Plasmodia. This study further underlines the importance of the hydroxamate functionality and illustrates that identifying effective alternative bidentate ligands for this target enzyme is challenging.