Triethylamine-Promoted Henry Reaction/Elimination of HNO2/Cyclization Sequence of Functionalized Nitroalkanes and 2-Oxoaldehydes: Diversity-Oriented Synthesis of Oxacycles

Org Lett. 2023 Jun 9;25(22):4033-4037. doi: 10.1021/acs.orglett.3c01158. Epub 2023 May 26.

Abstract

The triethylamine-promoted cascade Henry reaction/elimination of HNO2/cyclization reaction of 2-oxoaldehydes with nitroalkanes bearing various remote functionalities is described. Both chiral and achiral nitroalkanes were applicable to this protocol, leading to a variety of oxacycles, such as chromenes, chromanes, cyclic hemiacetals, and polycyclic acetals. An unexpected regioselective photooxygenation occurred without sensitizer during derivatization to convert a derived diene product into a dioxetane by reaction with singlet oxygen, which provided chromen-2-one and benzaldehyde after fragmentation.

MeSH terms

  • Acetals*
  • Benzopyrans*
  • Cyclization

Substances

  • triethylamine
  • Acetals
  • Benzopyrans