Automated synthesis of a library of triazolated 1,2,5-thiadiazepane 1,1-dioxides via a double aza-Michael strategy

ACS Comb Sci. 2012 Aug 13;14(8):456-9. doi: 10.1021/co300049u. Epub 2012 Aug 1.

Abstract

The construction of a 96-member library of triazolated 1,2,5-thiadiazepane 1,1-dioxides was performed on a Chemspeed Accelerator (SLT-100) automated parallel synthesis platform, culminating in the successful preparation of 94 out of 96 possible products. The key step, a one-pot, sequential elimination, double-aza-Michael reaction, and [3 + 2] Huisgen cycloaddition pathway has been automated and utilized in the production of two sets of triazolated sultam products.

Publication types

  • Letter
  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Automation
  • Aza Compounds / chemistry*
  • Azepines / chemical synthesis*
  • Azepines / chemistry
  • Combinatorial Chemistry Techniques*
  • Molecular Structure
  • Small Molecule Libraries / chemical synthesis*
  • Small Molecule Libraries / chemistry
  • Sulfur / chemistry*

Substances

  • 1,4-diazepane
  • Aza Compounds
  • Azepines
  • Small Molecule Libraries
  • Sulfur