Direct AmidationReaction And Its Application In Peptide Synthesis

Amide bond is a kind of stucture which can show high biological activity.Most biological activity matter has amide bond.25%of known drugs have at least an amide bond.Now commonly used methods for peptides synthesis by amidation condensation agent.But these amidation methods are not directly amidation.Hayley Charville and David Jackson found that aryl boric acid catalyst can be effective for simple structure of amidation reaction.And all belong to direct amidation reaction.The reaction yield is high and chiral structure did not change.But,so far,aryl boric acid catalyst was not used in direct amidation of amino acids such as complex structure.Therefore,This topic.is in the past to aryl boric acid catalyst research conducted on the basis of more in-depth research.Discuss whether aryl boric acid kind of catalyst can be used in peptides synthesis process.At first,use single amino acid with a simply ammonia or acid proceed direct amidation.See if can be effective for reaction.After the success to gradually for its research in the dipeptide and tripeptide synthesis.In order to improve the yield and try changing the reaction conditions.For a peptides synthesis evaluation,chiral structure change is vital.So after the synthesis reaction,use HPLC dectection chiral structure.Results show that the method of direct amidation reaction did not cause changes in the amino acid chiral structure of peptide synthesis.