KO<i>t</i>-Bu-promoted selective ring-opening <i>N</i>-alkylation of 2-oxazolines to access 2-aminoethyl acetates and <i>N</i>-substituted thiazolidinones
作者:Qiao Lin、Shiling Zhang、Bin Li
DOI:10.3762/bjoc.16.44
日期:——
2-methyl-2-oxazoline or 2-(methylthio)-4,5-dihydrothiazole with benzyl halides under basic conditions is described for the first time. The method provides a convenient and practical pathway for the synthesis of versatile 2-aminoethyl acetates and N-substituted thiazolidinones with good functional group tolerance and selectivity. KOt-Bu not only plays an important role to promote this ring-opening N-alkylation
首次描述了碱性条件下2-甲基-2-恶唑啉或2-(甲硫基)-4,5-二氢噻唑与苄基卤化物的有效且简单的KO t -Bu促进的选择性开环N-烷基化。该方法为合成具有良好官能团耐受性和选择性的通用2-氨基乙酸乙酯和N-取代的噻唑烷酮提供了方便实用的途径。KO t -Bu不仅在促进该开环N-烷基化中起重要作用,而且还充当氧供体。
2-Thiazolidinone derivatives, pharmaceutical compositions containing them, process for preparing same, and use
The present invention relates to novel 2-thiazolidinone derivatives of the general formula (I), ##STR1## wherein A stands for hydrogen, halogen or a C.sub.1-4 alkyl, C.sub.1-4 alkoxy or nitro group; and n is 0 or 1. The compounds according to the invention show a cytoprotective and gastric acid secretion-inhibiting effect and thus, may be used in the therapy of gastric and duodenal ulcers.