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■ Synthesis and Crystallographic Studies of New Acridinic Esters and Amides: An Efficient Synthetic Route to 4-Methyl Functionalized Acridines

Julien Chiron* and Jean-Pierre Galy

*UMR 6009, Laboratoire de Valorisation de la Chimie Fine, case 552, Facluté des Sciences et Techniques de Saint Jérôme, Avenue l'Escardille Normandie Niemen, 13397 Marseille Cedex 20, France

Abstract

In order to open a new way in antitumor drugs research, an efficient synthetic route to mono functional 4-substitued acridine derivatives has been developed on the basis of direct electrophilic substitution of acridine. This method leads to a wide range of simple acridinic patterns that can be linked to various side chains. We present here the synthesis of two new families of acridine ester and amide derivatives, obtained from acridinic alcohol and amine respectively, with high yields. Some crystallographic aspects of one representative compound of each family are discussed.