Organic Process Research & Development

Process Development of a Platelet Aggregation Inhibitor

A Zanka

Index: Zanka, Atsuhiko Organic Process Research and Development, 1998 , vol. 2, # 6 p. 418 - 421

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Citation Number: 3

Abstract

A practical and efficient method for N-amination of piperazine via a nitrosoamine, suitable for a large scale synthesis, is described. This method involved the temporary transformation of an in situ prepared aminopiperazine to a hydrazone, allowing efficient separation of zinc salt byproducts from the system. Acylation and deprotection with hydroxylamine directly afforded FR062732 in satisfactory quality for pharmacological evaluation. These methods solved ...