Solid-phase synthesis of libraries generated from a 4-phenyl-2-carboxy-piperazine scaffold. Academic Article uri icon

start page

  • 546

end page

  • 553

abstract

  • Strategies for finding novel structures of therapeutical interest are discussed. The rationale for the selection of the two scaffolds N4-(m-aminophenyl)-piperazine-2-carboxylic acid E and N4-(o-aminophenyl)-piperazine-2-carboxylic F is described. The synthesis of the appropriate precursors to scaffold E and F and their use in solid-phase chemistry are described. A 160-member library was produced combining these novel piperazine scaffolds with eight sulfonyl chlorides/acid chlorides and 10 amines. The compound library prepared was analyzed using LC-MS, showing the expected base peak in all wells at an average purity of 82%.

PubMed Identifier

  • 11703150

volume

  • 3

number

  • 6

keywords

  • Calcium Channel Blockers
  • Chemistry, Pharmaceutical
  • Combinatorial Chemistry Techniques
  • Dihydropyridines
  • Piperazines
  • Structure-Activity Relationship