Institute of Biostructures and Bioimages, National Research Council, 80138, Naples, Italy.
Amino Acids. 2011 Oct;41(4):981-90. doi: 10.1007/s00726-010-0798-6. Epub 2010 Nov 11.
A new synthetic strategy to alkylate amino groups under mild conditions has been developed. It utilizes only 4 Å molecular sieves as base in order to promote the N-alkylation reaction, in presence of the appropriate alkyl halide. The methodology was validated by the simple and efficient side-chain N-alkylation of o-Ns-protected Fmoc-amino acid. One of them was introduced as building block into a peptide sequence, thus allowing the preparation of site-specific alkylated peptide molecules.
已经开发出一种在温和条件下烷基化氨基的新合成策略。它仅利用 4 Å 分子筛作为碱，以促进 N-烷基化反应，同时存在适当的卤代烷。该方法通过简单有效的邻-硝基苯磺酰基（o-Ns）保护的 Fmoc-氨基酸的侧链 N-烷基化得到验证。其中之一被引入到肽序列中作为构建块，从而允许制备具有特定位置烷基化的肽分子。
