One-pot multicomponent synthesis of diversely substituted 2-aminopyrroles. A short general synthesis of rigidins A, B, C, and D

Org Lett. 2011 Mar 4;13(5):1118-21. doi: 10.1021/ol103149b. Epub 2011 Jan 26.

Abstract

Privileged medicinal scaffolds based on the structures of tetra- and pentasubstituted 2-aminopyrroles were prepared via one-pot multicomponent reactions of structurally diverse aldehydes and N-(aryl-, hetaryl-, alkylsulfonamido)acetophenones with activated methylene compounds. This methodology was used in a four-step synthesis of alkaloids rigidins A, B, C, and D in overall yields of 61%, 58%, 60%, and 53%, respectively. Of these, rigidins B, C, and D were synthesized for the first time.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Acetophenones / chemical synthesis*
  • Acetophenones / chemistry
  • Alkaloids
  • Biological Products / chemical synthesis*
  • Biological Products / chemistry
  • Combinatorial Chemistry Techniques
  • Marine Biology
  • Molecular Structure
  • Pyrimidines / chemical synthesis*
  • Pyrimidines / chemistry
  • Pyrroles / chemical synthesis*
  • Pyrroles / chemistry

Substances

  • Acetophenones
  • Alkaloids
  • Biological Products
  • Pyrimidines
  • Pyrroles
  • rigidin B