A VERSATILE APPROACH TO THE SYNTHESIS OF COMBRETASTATINS

A new and versatile synthesis of combretastatins has been developed. Starring from commercially available materials, 2-phenyl-2-benzyl-1,3-dithianes were easily prepared and used as intermediates in the synthesis of several families of combretastatins. This approach facilitates the preparation of representative intermediates in a few steps, with or without an oxygenated function in the ethylenic residue. Many different analogues suitable for pharmacological evaluation can also be obtained from some of these intermediates.