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Herein we developed a practical synthetic approach to the previously unknown difluoro-substituted bicyclo[1.1.1]pentanes. The key step was an addition of difluorocarbene to electron-rich bicyclo[1.1.0]butanes by CF₃TMS/NaI system. The obtained difluoro-bicyclo[1.1.1]pentanes are a new generation of saturated bioisosteres of the benzene ring for drug discovery projects.

Herein we developed a practical synthetic approach to the previously unknown difluoro-substituted bicyclo[1.1.1]pentanes. The key step was an addition of difluorocarbene to electron-rich bicyclo[1.1.0]butanes by CF₃TMS/NaI system. The obtained difluoro-bicyclo[1.1.1]pentanes are a new generation of saturated bioisosteres of the benzene ring for drug discovery projects.

ABSTRACT:The interaction of molybdo-phosphoric and molybdo-antimonophosphoric heteropoly acids with aliphatic (tetradecylammonium nitrate and trinonyloctadecylammonium iodide) and heterocyclic (lucigenine and safranine) quaternary ammonium salts immobilized onto silica has been studied using adsorption and spectroscopic methods. It has been shown that the formation of ionassociates between the quaternary ammonium cations and the heteropoly anions is accompanied by their interaction with surface silica groups which accounts for the tight binding of heteropoly acids to the surface. Such interfacial reactions can successfully be applied to the development of spectroscopic and semi-quantitative visual test techniques for detecting trace amounts of phosphorus and antimony.

The phenyl ring is a basic structural element in chemistry, and we learn about it already in school. We have developed an “ideal” saturated bioisoster of the para-substituted phenyl ring, - 2 oxabicyclo[2.2.2]octane. Its incorporation into Imatinib drug led to dramatic improvement of all physicochemical properties. This study opens new horizons in science, given the commonplace of the phenyl ring everywhere.