Solid-Phase Synthesis of Substituted 2,3-Diketopiperazines from Reduced Polyamides
作者:Adel Nefzi、Marc A. Giulianotti、Richard A. Houghten
DOI:10.1016/s0040-4020(00)00253-2
日期:2000.5
An efficient method for the solid phase synthesis of 1,6-disubstituted 2,3-diketopiperazine and 1,4,5-trisubstituted 2,3-diketopiperazine derivatives is described. The reduction of resin-bound acylated amino acids or resin-bound acylated dipeptides, followed by treatment with oxalyldiimidazole, affords the corresponding diketopiperazines in good yield and high purity. This is an example of a broader
描述了固相合成1,6-二取代的2,3-二酮哌嗪和1,4,5-三取代的2,3-二酮哌嗪衍生物的有效方法。还原树脂结合的酰化氨基酸或树脂结合的酰化二肽,然后用草酰二咪唑处理,以良好的收率和高纯度提供了相应的二酮哌嗪。这是使用肽直接或间接作为起始原料进行单个杂环化合物固相合成的广泛方法的一个例子。