PROCESS-DEVELOPMENT OF A PLATELET-AGGREGATION INHIBITOR

A practical and efficient method for N-amination of piperazine via a n itrosoamine, suitable for a large scale synthesis, is described. This method involved the temporary transformation of an in situ prepared am inopiperazine to a hydrazone, allowing efficient separation of zinc sa lt byproducts from the system. Acylation and deprotection with hydroxy lamine directly afforded FR062732 in satisfactory quality for pharmaco logical evaluation. These methods solved the operational problems usua lly inherent in zinc reduction of nitrosoamines.