Novartis Institutes for Biomedical Research, Cambridge, MA 02139, USA.
Chem Commun (Camb). 2012 Jul 7;48(53):6735-7. doi: 10.1039/c2cc32538a. Epub 2012 May 29.
The first TiCl(4)-mediated condensation of secondary amides with aldehydes and ketones has been achieved. The reaction proceeds at room temperature and is complete within 5 h in most cases. The optimized procedure used 5 equiv of an amine base hinting that the in situ activation of both the amide and the Lewis acid is required. The reaction affords polysubstituted (E)-enamides.
首次实现了 TiCl(4)介导的二级酰胺与醛酮的缩合反应。该反应在室温下进行,大多数情况下在 5 小时内即可完成。优化后的反应条件使用了 5 当量的胺碱,这表明需要同时原位激活酰胺和路易斯酸。该反应得到了多取代的(E)-烯酰胺。