The development of a semi-preparatory scale supercritical-fluid chromatograph for high-throughput purification of 'combi-chem' libraries

J Biochem Biophys Methods. 2000 Jul 5;43(1-3):87-111. doi: 10.1016/s0165-022x(00)00084-1.

Abstract

A unique separator was developed which allowed automatic separation and peak collection using semi-preparative supercritical fluid chromatography (SFC). A peak detector switched the effluent between waste and special collection cassettes. Up to 50 mg of various solutes were injected onto a 21-mm I.D. Cyano column. The entire flow path was contained and no aerosols were generated. Collection efficiency was as high as 95%. Peak purity was often greater than 99. 9%. Typical run times were less than 10 min. An analytical SFC was used to screen the performance of a wide range of mobile and stationary phases for the elution of more than 60 miscellaneous small drug compounds. The best 'universal' gradient employed 0.4% isobutyl or isopropylamine dissolved in methanol, then mixed from 5 to 55% into carbon dioxide at 10%/min. Flow rate was 50 ml/min. The analytical SFC was shown to be a good predictor of the semi-prep instrumental performance.

MeSH terms

  • 4-Aminobenzoic Acid / chemistry
  • Antipyrine / isolation & purification
  • Benzamides / chemistry
  • Butylamines / chemistry
  • Carbon Dioxide / chemistry
  • Chromatography / instrumentation*
  • Chromatography / methods*
  • Combinatorial Chemistry Techniques / methods
  • Imipramine / isolation & purification
  • Methanol / chemistry
  • Peptide Library*
  • Procaine / isolation & purification
  • Propylamines / chemistry
  • Time Factors
  • para-Aminobenzoates

Substances

  • Benzamides
  • Butylamines
  • Peptide Library
  • Propylamines
  • para-Aminobenzoates
  • Carbon Dioxide
  • isobutylamine
  • Procaine
  • benzamide
  • 4-aminobenzamide
  • Imipramine
  • 2-propylamine
  • Antipyrine
  • 4-Aminobenzoic Acid
  • Methanol