Organic Chemistry Department, Universidad Autónoma de Madrid, 28049 Madrid (Spain) www.uam.es/jose.aleman.
Instituto Universitario de Bio-Orgánica, "Antonio González" (IUBO-AG), Centro de Investigaciones Biomédicas de Canarias (CIBICAN), Universidad de La Laguna, 38206 La Laguna (Spain).
Chemistry. 2015 May 26;21(22):8237-41. doi: 10.1002/chem.201500660. Epub 2015 Apr 23.
An asymmetric synthesis of diheteroarylalkanals through one-pot dienamine and Friedel-Crafts reaction is presented. The reaction tolerates a large variety of substituents at different positions of the starting aldehyde and also in the indole nucleophile, and a range of diheterocyclic alkanals can be achieved. Furthermore, we have studied the antiproliferative activity of these new compounds in representative cancer tumor cell lines.
本文报道了一种通过一锅法烯胺和傅克反应不对称合成二杂芳基链醛的方法。该反应对起始醛和吲哚亲核试剂的不同位置以及各种取代基具有良好的耐受性,可以得到一系列二杂环链醛。此外,我们还研究了这些新化合物在代表性的肿瘤细胞系中的抗增殖活性。