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Microwave Assisted Aza-michael Additions towards p-amino Acids

机译：微波辅助Aza-michael对p-氨基酸的添加

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摘要

Background: p-amino acids are non-natural amino acids, where the amino group is attached to the p-carbon instead of the a-carbon. Peptides containing p-amino acids present with particular secondary structures and remarkable chemical and biological properties. p-peptides are used as peptidomimetics, based on the resistance to hydrolysis in vivo, with various important applications in the field of Medicine. Methods: Several synthetic methods have appeared in recent years, with the Aza- Michael conjugate addition reactions, being a very effective approach towards p-amino acids. Microwave irradiation mediated reactions have also attracted much interest since they significantly improve the reaction yields while reducing the reaction time and avoiding by-products formation. The aim of this project has been the development of a reliable and general synthetic methodology towards β2 and β3 amino acids with the use of conjugate additions of N-nucleophiles to substituted acrylate derivatives. The application of effective catalysts has been also examined here. Results: The results show that the acrylate precursors of p2 and p3 amino acids with side chains corresponding to Phe, Asp, Ile, Leu, Val, and Tyr have been synthesized successfully by using a one-pot Horner-Wadsworth-Emmons reaction, and they have been used for the addition of N-nucleophiles, with a study on conditions and yields optimization. Conclusion: With the main challenge for β-amino acid synthesis being that there is still no general method to synthesize different types of β-amino acids corresponding to all-natural a-amino acids, the proposed synthetic methodology may offer this possibility.
机译：背景:p-amino酸是天然的氨基酸酸的氨基相连p-carbon而不是碳。包含p-amino酸特别礼物二级结构和化学和显著生物属性。peptidomimetics,基于阻力水解体内,与各种重要在医学领域中的应用。几种合成方法已经出现在最近年,阿扎-迈克尔共轭加成反应,是一种非常有效的方法对p-amino酸。介导的反应也吸引了很多因为他们显著提高兴趣反应的产量,同时减少反应时间和避免副产物的形成。这个项目的发展可靠的和一般的合成方法对β2、β3氨基酸的使用共轭N-nucleophiles的添加代替丙烯酸酯衍生品。还研究了有效的催化剂在这里。的p2和p3氨基酸前体对应链板式换热器、Asp、Ile低浓缩铀,Val,和酪氨酸合成成功使用一个锅Horner-Wadsworth-Emmons反应,他们已经使用了的N-nucleophiles,和研究条件产量优化。挑战β氨基酸酸合成的仍然没有一般合成方法不同类型的β相对应的胺基酸纯天然a-amino酸,该合成方法可能提供这种可能性。

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