Abstract

This review describes methods for the synthesis of 1-trifluomethylindanes and close structures, which are still quite rare and scarcely available compounds. There are two main approaches to obtain 1-CF3-indanes. The first one is the construction of an indane system from CF3 precursors; the main methods are acid-mediated Friedel–Crafts cyclization, transition metal-catalyzed [3+2] annulation, and free-radical transformations. The second approach is the trifluoromethylation of a ready-made indane core by various CF3 sources, such as Ruppert–Prakash or Togni reagents. Many of these synthetic procedures possess high regio- and stereo-selectivity, allowing the preparation of unique 1-CF3-indane structures. In recent years, great attention has been paid to the synthesis of 1-CF3-indanes, due to the discovery of important biologically active properties for these compounds.

Highlights

  • Organofluorine compounds are widely used and are of great importance in chemistry, biology, medicine, agriculture, materials science, and other fields of science and technology.The presence of fluorine atoms in organic molecules significantly changes their chemical, physical, and pharmokinetic properties

  • The second approach is the trifluoromethylation of a ready-made indane core by various CF3 sources, such as Ruppert–Prakash or Togni reagents

  • The development of novel methods of synthesis of CF3 -indane derivatives and investigation of their biologically active properties is an important goal for chemistry, biology, and medicine

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Summary

Introduction

Organofluorine compounds are widely used and are of great importance in chemistry, biology, medicine, agriculture, materials science, and other fields of science and technology. The development of novel methods of synthesis of CF3 -indane derivatives and investigation of their biologically active properties is an important goal for chemistry, biology, and medicine. These fluorinated derivatives must find broad application in material science and many other fields. F1-trifluoromethyl indanes are extremely promising objects for medicinal chemOMe. μM vestigation of their biologically properties is an important goal for chemistry, biolMeO ogy, and medicine. ΜM vestigation of their biologically properties is an important goal for chemistry, biolMeO ogy, and medicine Cl indanones to show the main approaches to the preparation of these compounds

Discussion
Synthesis
MeAlCl
12. Stereoselective
13. Synthesis
14. Possible
CF3-allyl alcohols 19 in TfOH has been applied in the synthesis of1-CF tuted
Protonation
15. TfOH-promoted
29. Con3 -aminoindanes to cyclic ketimines
20. Synthesis of CFof
25. Stereoselective
26. Synthesis of of 1-CF
27. Synthesis
28. Synthesis using
29. Enantioselective
34. Copper-catalyzed
Conclusions

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