AI Article Synopsis

  • A new method is introduced for the cascade oxidation and halogenoaminocyclization of trifluoromethylated homoallylic N-acylhydrazines, which simplifies the preparation of CF-containing pyrazoline compounds.
  • The process is efficient, yielding a variety of these compounds under mild conditions, and does not require additional additives or catalysts.
  • The resulting pyrazolines can be easily transformed into more complex derivatives by modifying the leftover halogen atom.

Article Abstract

An efficient and practical cascade oxidation/halogenoaminocyclization of trifluoromethylated homoallylic N-acylhydrazines is developed. The protocol enables an efficient access to various biologically interesting CF-containing pyrazoline compounds from readily accessible trifluoromethylated homoallylic N-acylhydrazines in good to excellent yields under mild conditions without any other additives or catalysts. The produced pyrazoline compounds can be further manipulated to other more complicated derivatives through transformation of residual halogen atom.

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http://dx.doi.org/10.1021/acs.joc.7b02934DOI Listing

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