Cyclizations of substituted benzylidene-3-alkenylamines: synthesis of the tricyclic core of the martinellines

J Org Chem. 2000 Feb 11;65(3):655-66. doi: 10.1021/jo990843c.

Abstract

The martinellines (1 and 2) are natural products that possess both interesting biological activity and chemical structure. During the investigation of a hetero Diels-Alder route to these molecules, alternate Lewis acid-dependent cyclizations of (2'-amino-N'-tert-butoxycarbonyl-5'-chlorobenzylidene)-3-butenylamine (10) were observed. The reaction of a variety of imines with TMSOTf or TiCl(4) led to the formation of different heterocycles including iminodibenzo[b,f][1,5]diazocines, hexahydropyrido[1, 2-c]quinazolin-6-ones, tetrahydropyrrolo[1,2-c]quinazolin-5-ones, 2-arylpiperidines, and 2-arylpyrrolidines. Tetrahydropyrrolo[1, 2-c]quinazolin-5-one 54, obtained via this new methodology, was used as an intermediate in the synthesis of the tricyclic ring system (65) of the martinellines.

Publication types

  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Amines / chemistry*
  • Benzylidene Compounds / chemistry*
  • Molecular Structure
  • Pyrroles / chemical synthesis*
  • Pyrroles / chemistry
  • Quinolines / chemical synthesis*
  • Quinolines / chemistry
  • Spectrum Analysis

Substances

  • Amines
  • Benzylidene Compounds
  • Pyrroles
  • Quinolines
  • martinelline