Horn Thomas, Lee Byoung-Chul, Dill Ken A, Zuckermann Ronald N
Chiron Corporation, 4560 Horton Street, Emeryville, California 94608, USA.
Bioconjug Chem. 2004 Mar-Apr;15(2):428-35. doi: 10.1021/bc0341831.
A simple route to the introduction of a number of chemoselective functional groups into peptoids (oligo(N-substituted glycines)) by an extension of the standard solid-phase submonomer method is reported. The following groups were introduced: aminooxyacetamide, N-(carbamoylmethyl)acetohydrazide, mercaptoacetamide, 2-pyridinesulfenylmercaptoacetamide, and aldehyde-terminated peptoids. The method uses commercially available reagents, is fully compatible with standard peptoid submonomer synthesis conditions, is easily automated, and generates the desired functionalized peptoid in high yield and purity. Peptoids with suitable pairs of chemoselective ligation groups were joined in high yield.
报道了一种通过扩展标准固相亚单体方法，将多种化学选择性官能团引入类肽（寡聚（N-取代甘氨酸））的简单途径。引入了以下基团：氨氧基乙酰胺、N-（氨甲酰基甲基）乙酰肼、巯基乙酰胺、2-吡啶亚磺酰基巯基乙酰胺和醛基末端类肽。该方法使用市售试剂，与标准类肽亚单体合成条件完全兼容，易于自动化操作，并能以高收率和纯度生成所需的功能化类肽。具有合适化学选择性连接基团对的类肽能高产率地连接起来。
