Synthesis and structure of preorganized, C(3)-symmetric trilactam scaffolds with convergently oriented (S)-acetylthiomethyl appendages

Org Lett. 2002 Jun 27;4(13):2273-5. doi: 10.1021/ol0261480.

Abstract

[reaction: see text] Efficient modular synthesis of conformationally preorganized, C(3)-symmetric trilactams is reported. The allyl acetate cyclization substrate was synthesized in five steps from Garner's L-serine-derived aldehyde. After chiral ligand-mediated palladium cyclization, the resulting vinyl hydropyran was transformed into the orthogonally protected amino acids for iterative coupling. The final macrolactamization was accomplished using EDCI/HOBt or HATU/HOAt under high dilution conditions.

Publication types

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

MeSH terms

  • Catalysis
  • Crystallography, X-Ray
  • Cyclization
  • Heterocyclic Compounds, 3-Ring / chemical synthesis*
  • Heterocyclic Compounds, 3-Ring / chemistry
  • Lactams / chemical synthesis*
  • Lactams / chemistry
  • Molecular Structure
  • Stereoisomerism
  • Sulfhydryl Compounds / chemistry

Substances

  • Heterocyclic Compounds, 3-Ring
  • Lactams
  • Sulfhydryl Compounds