Several pyrazolo [3, 4-d] pyrimidine analogues of the potent antitumor agent N-{4-[2-(2- amino-4 (3H)-oxo-7H-pyrrolo [2, 3-d] pyrimidin-5-yl) ethyl] benzoyl}-L-glutamic acid (LY231514, 5) have been prepared. A principal synthetic step proved to be a palladium- catalyzed C C coupling of the 5-halo-substituted pyrazolo [3, 4-d] pyrimidines 12–15 with dimethyl 4-ethynylbenzoyl-L-glutamate (16). An additional pyrazolo [3, 4-d] pyrimidine ...