Benzotriazole-Mediated Synthesis of Aza-peptides: En Route to an Aza-Leuenkephalin Analogue
作者:Nader E. Abo-Dya、Suvendu Biswas、Akash Basak、Ilker Avan、Khalid A. Alamry、Alan R. Katritzky
DOI:10.1021/jo302251e
日期:2013.4.19
with an ester bond 26b, and a hybrid azatripeptide with an ester bond 28. A new protocol for the synthesis of N-Pg-azatripeptides 33a,b and 35a,b, each containing a natural amino acid at the N-terminus, avoids the low coupling rates of the aza-amino acid residue and enables the solution-phase synthesis of an azaphenylalanine analogue of Leu-enkephalin 40.
新颖ñ - (Ñ -Pg-azadipeptidoyl)苯并三唑20A - ë与α氨基酸有效耦合21A - ë,二肽22A - Ç,氨基羟乙酸23A,depsidipeptide 23B,和α羟基β苯基丙酸27屈服,分别,三氮杂肽24a – g,氮杂三肽25a,b,具有氧酰胺键的杂合氮杂三肽26a,具有酯键的杂合氮杂四肽26b杂化的带有酯键的氮杂三肽28。用于合成N -Pg-氮杂三肽33a,b和35a,b的新方案,每个肽在N-末端均包含天然氨基酸,避免了氮杂氨基酸残基的低偶联率并使溶液相成为可能。亮脑啡肽40的氮杂苯丙氨酸类似物的合成。