The Preorganization of Atropisomers to Increase Target Selectivity

  title={The Preorganization of Atropisomers to Increase Target Selectivity},
  author={Christopher Nalbandian and David E. Hecht and Jeffrey L Gustafson},
Atropisomerism is a form of chirality that arises from differential substitution around a bond that renders the rotational isomers enantiomers. Depending on the degree of hindrance to bond rotation, atropisomers can exist as either stable isolable enantiomers or rapidly racemizing atropisomeric mixtures. Many biologically active small molecules exist as rapidly interconverting atropisomers, however, only one of the possible atropisomers possesses the desired activity. The presence of the… CONTINUE READING