Faculty of Chemistry, University of Warsaw, Pasteura 1, 02-093, Warsaw, Poland.
Mol Divers. 2010 Feb;14(1):97-108. doi: 10.1007/s11030-009-9151-y. Epub 2009 Jun 16.
The Pictet-Spengler reaction is known as a useful tool for the synthesis of constrained analogs of tryptophan. Herein, we present the further cyclization of 1,2,3,4-tetrahydro-beta-carboline-3-carboxylic acid methyl esters with 1-(1'-aminoalkyl) side chain. These transformations lead to heterocyclic structures which can find useful applications in medicinal chemistry as peptide mimetics.
Pictet-Spengler 反应是合成色氨酸约束类似物的有用工具。在此,我们介绍了具有 1-(1'- 氨基烷基)侧链的 1,2,3,4-四氢-β-咔啉-3-羧酸甲酯的进一步环化。这些转化生成的杂环结构在药物化学中可以作为肽模拟物找到有用的应用。