Abstract
Various compounds related to the hypocholesterolemic alkaloid eritadenine (I) were synthesized for the evaluation of structure-activity relationships in this series. 6-Sub-stituted purine analogs were prepared by reacting the 6-chloro-purine intermediate (II) with the corresponding nucleophilic reagents. 2, 6-Di-substituted purine derivatives were prepared by utilizing a route involving an imidazole ring closure step, starting from the appropriately substituted pyrimidine precursors and the amino-acid (VI). The preparation of 6, 8-di-substituted purine analogs was achieved by cyclization of the 5-amino-pyrimidine intermediate (XXIX) derived for the synthesis of I.
