A simple, inexpensive apparatus for performance of preparative scale solution phase multiple parallel synthesis of drug analogs. I. Preparation of a retrospective library of quinolone antiinfective agents

Comb Chem High Throughput Screen. 1998 Jun;1(2):73-87.

Abstract

A simple inexpensive apparatus is described consisting of conveniently commercially available components which is suitable for the solution phase multiple parallel synthesis of 24-72 analogs of drug-like molecules. The use of the apparatus is illustrated by preparation of a retrospective library of over 100 analogs of antimicrobial fluoroquinolones prepared in 0% to quantitative yields. Each analog was prepared in up to 150 mg quantity and each was analyzed by NMR and mass spectrometric techniques to verify its purity and identity.

Publication types

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

MeSH terms

  • Anti-Infective Agents / analysis*
  • Anti-Infective Agents / chemical synthesis*
  • Anti-Infective Agents / chemistry
  • Chemistry, Pharmaceutical / instrumentation*
  • Chemistry, Pharmaceutical / methods
  • Fluoroquinolones
  • Magnetic Resonance Spectroscopy
  • Mass Spectrometry

Substances

  • Anti-Infective Agents
  • Fluoroquinolones