Assuntos
Proteínas de Transporte/química , Ésteres do Colesterol/sangue , Glicoproteínas , Propanolaminas/síntese química , Proteínas de Transporte/antagonistas & inibidores , Proteínas de Transporte/sangue , Proteínas de Transferência de Ésteres de Colesterol , Cristalografia por Raios X , Humanos , Técnicas In Vitro , Propanolaminas/sangue , Propanolaminas/química , EstereoisomerismoRESUMO
Using a combination of solid phase synthesis for the preparation of N-substituted-N-acylglycines 7 followed by solution-phase ring transformation of trifluoromethylacyl munchnone intermediate 8, a library of 200 trisubstituted-5-trifluoromethylketo (TFMK) imidazoles 9 was prepared. In a sublibrary, bromoacetate resin 4 was treated with 5 amines in parallel to give N-substituted glycines 5 followed by acylation with 12 acid chlorides to provide, upon cleavage from the resin, 60 individual N-substituted-N-acylglycines 7. The glycines 7 were converted to munchnones 8 by treatment with trifluoroacetic anhydride followed by reaction with benzamidine to give trisubstituted-5-TFMK-imidazoles 9. The structural content of the library was analyzed using PlateView of the LCMS results, and individual members were isolated by automated preparative LCMS.
