Facile (triazolyl)methylation of MACOS-derived benzofused sultams utilizing ROMP-derived OTP reagents

ACS Comb Sci. 2012 Apr 9;14(4):268-72. doi: 10.1021/co2001839. Epub 2012 Mar 5.

Abstract

A combination of MACOS scale-out and ROMP-derived oligomeric triazole phosphates (OTP(n)) have been successfully utilized for the preparation of a 106-member library of triazole containing benzothiaoxazepine-1,1-dioxides. This report demonstrates the utilization of a suite of soluble OTP(n) reagents for facile (triazolyl)methylation of 10 MACOS-derived sultam scaffolds in purification-free process for parallel synthesis of small molecule collections for HTS.

Publication types

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

MeSH terms

  • Benzothiadiazines / chemical synthesis*
  • Benzothiadiazines / chemistry
  • Combinatorial Chemistry Techniques
  • Methylation
  • Microwaves*
  • Molecular Structure
  • Oxides / chemical synthesis*
  • Oxides / chemistry
  • Phosphates / chemistry*
  • Small Molecule Libraries / chemical synthesis*
  • Small Molecule Libraries / chemistry
  • Stereoisomerism
  • Triazoles / chemistry*

Substances

  • Benzothiadiazines
  • Oxides
  • Phosphates
  • Small Molecule Libraries
  • Triazoles