The present invention discloses an improved synthesis of ethyl N-[(2-Boc-amino)ethyl]glycinate and its hydrochloride salt. The synthesis is based on the reductive alkylation of Boc-ethylenediamine with ethyl glyoxylate hydrate and furnishes the title compound in near quantitative yield and high purity without chromatography. This compound is suitable, as is, for the synthesis peptide nucleic acid monomers. Further, conversion to the hydrochloride salt provides a stable, non-hygroscopic solid that is a convenient form for handling and storage.
本发明公开了一种改进的合成乙基N-[(2-Boc-
氨基)乙基]甘
氨酸及其盐酸盐。该合成基于Boc-
乙二胺与乙酰
甘醇水合物的还原烷基化反应,并以接近定量产率和高纯度提供了标题化合物,无需色谱分离。该化合物适合直接用于合成肽核酸单体。此外,转化为盐酸盐提供了一种稳定的、不吸湿的固体形式,便于处理和储存。