1493792-45-2Relevant academic research and scientific papers
An efficient and epimerization free synthesis of C-terminal arylamides derived from α-amino acids and peptide acids via T3P activation
Madhu, Chilakapati,Nageswararao, Panguluri,Narendra,Sureshbabu, Vommina V.
, p. 353 - 363 (2014/08/18)
A high yield and rapid synthesis of enantiomerically pure N α -protected amino/peptide acid arylamides using n-propylphosphonic anhydride (T3P) in presence of N-methylmorpholine is described. The generality of the reaction has been studied for various N α -protected amino acids with diverse range of aromatic amines and coumarin derivatives.
An efficient synthesis of Nα-protected amino and peptide acid aryl amides via iodine-mediated oxidative acylation of N α-protected amino and peptide thioacids
Madhu, Chilakapati,Vishwanatha,Sureshbabu, Vommina V.
, p. 2727 - 2736 (2013/10/21)
Thioacids derived from N-protected amino or dipeptide and tripeptide acids undergo facile N-acylation with aromatic amines to afford N-protected amino or peptide aryl amides in good to excellent yields and enantiopurities. The method also furnishes difficult-to-prepare N-Fmoc amino acid 4-nitroanilides in good yields. This simple oxidative Nα-acylation of thioacids with aromatic amines proceeds in the presence of iodine, 1-hydroxybenzotriazole and N,N-diisopropylethylamine at room temperature in tetrahydrofuran. Georg Thieme Verlag Stuttgart New York.
