Department of Basic Sciences and Environment, University of Copenhagen, Thorvaldsensvej 40, 1871 Frederiksberg C, Denmark.
Org Biomol Chem. 2011 Oct 7;9(19):6832-43. doi: 10.1039/c1ob05729d. Epub 2011 Aug 12.
The development of a highly efficient methodology for solid-phase synthesis of para- and meta-arylopeptoids (oligomeric N-substituted aminomethyl benzamides) with free acids or free amides at the C-terminus is described. The arylopeptoids were synthesised by means of a convenient submonomer protocol in which the arylopeptoid residues were created in an iterative manner on the growing chain using an acylation-substitution cycle. The uronium salt COMU was found to be the most efficient reagent for ensuring fast and clean couplings of the benzoic acid building blocks.
描述了一种高效的固相合成方法,用于合成末端带有游离酸或游离酰胺的对芳基和间芳基肽(寡聚 N-取代氨甲基苯甲酰胺)。通过一种方便的亚单体方法合成了芳基肽,其中使用酰化取代循环在生长链上以迭代方式构建芳基肽残基。发现onium 盐 COMU 是确保苯甲酸砌块快速且清洁偶联的最有效试剂。