Synthesis of some 2-arylpropionic acid amides as prodrugs

AKGUN H. , Tozkoparan B. , ERTAN M. , AKSU F. , INAN S.

ARZNEIMITTEL-FORSCHUNG/DRUG RESEARCH, cilt.46, sa.9, ss.891-894, 1996 (SCI İndekslerine Giren Dergi) identifier identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 46 Konu: 9
  • Basım Tarihi: 1996
  • Sayfa Sayıları: ss.891-894


The synthesis of amide prodrugs of some 2-arylpropionic acids (ibuprofen, naproxen, diclofenac and ketorolac) and the enantiomeric separation of these compounds are reported in this paper. The compounds were prepared from the corresponding 2-arylpropionic acids and (R-(-)-2-amino-1-butanol in the presence of N,N'-dicyclohexylcarbodiimide (DCC). Enantiomers were separated by preparative chromatography or crystallisation. The structure were confirmed by infrared, nuclear magnetic resonance and elementary analysis. The compounds prepared in the study have significant analgesic activity.