A tunable route for the synthesis of azomethine imines and β-aminocarbonyl compounds from alkenes

J Am Chem Soc. 2012 Oct 3;134(39):16111-4. doi: 10.1021/ja305491t. Epub 2012 Sep 20.

Abstract

Cyclic azomethine imines possessing a β-aminocarbonyl motif are accessed from simple alkene and hydrazone starting materials. A thermal, concerted alkene aminocarbonylation pathway involving an imino-isocyanate intermediate is proposed and supported by DFT calculations. A notable feature of the process is the steric shielding present in the dipoles formed, which allows for facile purification of the products by chromatography or crystallization. In addition, a fluorenone-derived reagent is reported, which provides reactivity with several alkene classes and allows for mild derivatization of the dipoles into β-aminoamides, β-aminoesters, and β-amino acids.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alkenes / chemistry*
  • Azo Compounds / chemistry*
  • Chemistry Techniques, Synthetic
  • Hydrazones / chemistry
  • Imines / chemical synthesis*
  • Imines / chemistry*
  • Ketones / chemistry
  • Thiosemicarbazones / chemistry*

Substances

  • Alkenes
  • Azo Compounds
  • Hydrazones
  • Imines
  • Ketones
  • Thiosemicarbazones
  • azomethine