REACTION OF TRIALKYL PHOSPHITES AND a-HALOKETONES IN APROTIC MEDIA (PERKOW-ARBUZOV REACTION) AND IN PROTIC SOLVENTS

The authors suggest a new reaction mechanism for the Perkow-Arbuzov reaction yielding vinyl phosphates and B-keto phosphonates. For the reaction of a-haloacetophenones and trialkyl phosphites in alcohol or acetic acid giving 3 products a uniform mechanism involving again a common intermediate was assumed. In the course of our work the applicability of Hammett's equation has been extended for studying parallel and braching reactions, as well

Synthesis and Evaluation of Phosphorus Containing, Specific CDK9/CycT1 Inhibitors

International audienceAlthough there is a significant effort in the design of a selective CDK9/CycT1 inhibitor, no compound has been proven to be a specific inhibitor of this kinase so far. The aim of this research was to develop novel and selective phosphorus containing CDK9/CycT1 inhibitors. Molecules bearing phosphonamidate, phosphonate, and phosphinate moieties were synthesized. Prepared compounds were evaluated in an enzymatic CDK9/CycT1 assay. The most potent molecules were tested in cell-based toxicity and HIV proliferation assays. Selectivity of shortlisted compounds against CDKs and other kinases was tested. The best compound was shown to be a highly specific, ATP-competitive inhibitor of CDK9/CycT1 with antiviral activity