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PHOSPHORUS Pentoxide for Amide and Peptide Bond Formation with Minimal By-products
Tetrahedron Letters ( IF 1.5 ) Pub Date : 2019-10-23 , DOI: 10.1016/j.tetlet.2019.151311
Venkataramana Erapalapati , Umatai A. Hale , Nandita Madhavan

Phosphorus pentoxide and DMAP are used for amide bond formation from carboxylic acids and amines. Dipeptides and amides have been synthesized using this reagent in 42-77% yields and >99% ees. The protocol is attractive as it occurs at ambient temperature, the formation of organic by-products is minimal and the reagent can be readily quenched using water. Furthermore, excellent enantioselectivities are observed without the use of harsh triazole based additives.



中文翻译:

五氧化二磷可形成酰胺和肽键,副产物最少

五氧化二磷和DMAP用于由羧酸和胺形成酰胺键。使用该试剂已合成了二肽和酰胺,产率为42-77%,ee大于99%。该方案具有吸引力,因为它在环境温度下发生,有机副产物的形成极少,并且试剂可以很容易地用水淬灭。此外,在不使用苛刻的三唑基添加剂的情况下,观察到优异的对映选择性。

更新日期:2019-10-24
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