A CONSTRAINED DIKETOPIPERAZINE AS A NEW SCAFFOLD FOR THE SYNTHESIS OFPEPTIDOMIMETICS

As a new scaffold for peptidomimetic synthesis, a highly constrained b ifunctional diketopiperazine, 4, has been prepared by smooth N-alkylat ion with tert-butyl bromoacetate. As a first application, we describe herein the synthesis of new peptidomimetics of the Arg-Gly-Asp (RGD) s equence. The product 30, which shows a selective platelet-aggregation inhibiting activity, can be used as a lead for the preparation of more potent products.