Bozzola Tiago, Nilsson Ulf J, Ellervik Ulf
Centre for Analysis and Synthesis, Department of Chemistry, Lund University P.O. Box 124 SE-221 00 Lund Sweden
RSC Adv. 2022 Apr 19;12(19):11992-11995. doi: 10.1039/d2ra01576e. eCollection 2022 Apr 13.
A direct one-step nucleophilic substitution of the 4-OAc of acetyl protected Neu5Ac is presented. Previously published methods for direct substitution of the 4-OAc are limited to cyclic secondary amines. Here we present conditions that allow for a much wider range of nitrogen nucleophiles as well as thiols and cyanide, to be used. The present investigation significantly broadens the scope of 4-aminations and allows for the introduction of a wide variety of different nucleophiles.
本文介绍了一种对乙酰基保护的Neu5Ac的4-OAc进行直接一步亲核取代的方法。先前发表的直接取代4-OAc的方法仅限于环状仲胺。在此，我们提出了一些条件，使得范围更广的氮亲核试剂以及硫醇和氰化物都能被使用。本研究显著拓宽了4-胺化反应的范围，并允许引入多种不同的亲核试剂。
