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Dienamine and Friedel–Crafts One‐Pot Synthesis,and Antitumor Evaluation of Diheteroarylalkanals
Authors:María Frías  Dr José M Padrón  Dr José Alemán
Institution:1. Organic Chemistry Department, Universidad Autónoma de Madrid, 28049 Madrid (Spain) www.uam.es/jose.aleman;2. Instituto Universitario de Bio‐Orgánica, ?Antonio González“ (IUBO‐AG), Centro de Investigaciones Biomédicas de Canarias (CIBICAN), Universidad de La?Laguna, 38206 La?Laguna (Spain)
Abstract: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.
Keywords:aldehydes  antiproliferation  asymmetric synthesis  nitrogen heterocycles  organocatalysis
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