Papadopoulos Giorgos N, Kokotos Christoforos G
Laboratory of Organic Chemistry, Department of Chemistry, National and Kapodestrian University of Athens, Panepistimiopolis, 15771, Athens, Greece.
Chemistry. 2016 May 10;22(20):6964-7. doi: 10.1002/chem.201600333. Epub 2016 Apr 1.
An efficient one-pot synthesis of hydroxamic acids from aldehydes and hydroxylamine is described. A fast, visible-light-mediated metal-free hydroacylation of dialkyl azodicarboxylates was used to develop the subsequent addition of hydroxylamine hydrochloride. A range of aliphatic and aromatic aldehydes were employed in this reaction to give hydroxamic acids in high to excellent yields. Application of the current methodology was demonstrated in the synthesis of the anticancer medicine vorinostat.
描述了一种从醛和羟胺高效一锅法合成异羟肟酸的方法。利用二烷基偶氮二羧酸酯的快速、可见光介导的无金属氢酰化反应来实现随后盐酸羟胺的添加。该反应中使用了一系列脂肪族和芳香族醛,以高至优异的产率得到异羟肟酸。当前方法在抗癌药物伏立诺他的合成中得到了验证。