摘要：

The exceptional conformational rigidity conferred on proline by its cyclic system has been the keystone for the control of tridimensional structure of peptides and proteins.1 Moreover, proline analogues are of special interest since they are common structural elements found in natural products with important medicinal activity that have been targets for many syntheses.2 The amino acid proline has been extensively used as an organocatalyst and several methodologies have been explored for the synthesis of unnatural prolines.3 However, to the best of our knowledge few methods have been explored for the synthesis of arylprolines, in particular 5-arylprolines for which there are no reports in the literature. Efforts in our laboratory have focused on the applications of Heck arylation for the synthesis of building blocks for biological actives compounds as well as organocatalysts. In this way, we report herein an efficient and stereoselective approach to the synthesis of 5-arylprolines employing the Heck arylation methodology as a key strategy.

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