Krauß Jürgen, Plesch Eva, Clausen Sabine, Bracher Franz
Department of Pharmacy - Center for Drug Research, Ludwig-Maximilian-University, Butenandtstr. 5-13, 81377 Munich, Germany.
Sci Pharm. 2014 Mar 13;82(3):501-17. doi: 10.3797/scipharm.1401-19. Print 2014 Jul-Sep.
Ortho-hydroxy-anilides are part of natural products like the new antibiotics platencin (A) and platensimycin (B). An important step in the total synthesis of these antibiotics or their derivatives is the preparation of the o-hydroxy-anilide partial structure. The presented method allows the preparation of o-hydroxy-anilides and o-dihydroxy-anilides from 2-nitrophenol esters in a one-step synthesis without protecting the hydroxy group. Aryl- and alkyl-anilides were prepared following this method as simple analogues of platensimycin (A). The resulting compounds were tested in an agar diffusion assay for their antibiotic potency.
邻羟基苯胺类化合物是天然产物的一部分，如新抗生素普拉特烯素（A）和普拉特烯霉素（B）。这些抗生素或其衍生物全合成中的一个重要步骤是邻羟基苯胺部分结构的制备。本文提出的方法能够在不保护羟基的情况下，通过一步合成从2-硝基苯酚酯制备邻羟基苯胺类化合物和邻二羟基苯胺类化合物。按照此方法制备了芳基和烷基苯胺类化合物，作为普拉特烯霉素（A）的简单类似物。对所得化合物进行琼脂扩散试验以检测其抗菌效力。
