Dupont Pharmaceuticals Company

Bristol-myers Squibb Pharma Company

The Dupont Merck Pharmaceutical Company

Robert E Waltermire

Luigi Anzalone

Gregory D Harris

Joseph M Fortunak

Benjamin R P Stone

Ioannis I Valvis

Hui-Yin Li

Lilian Alicia Radesca

Edward Koon Wat

Preparation of asymmetric cyclic ureas through a monoacylated diamine intermediate

Processes for the preparation of R-.alpha.-propyl-piperonyl amine and its analogs, such compounds being useful intermediates in the preparation of elastase inhibitors, and intermediates useful for making R-.alpha.-propyl-piperonyl amine are described.

Asymmetric synthesis of R-.alpha.-propyl-piperonyl amine and its analogs

This invention provides improved synthetic processes for the preparation of hydroxy-protected cyclic urea compounds of Formula (IX), ##STR1## which are useful as intermediates for the preparation of cyclic urea human immunodeficiency virus (HIV) protease inhibitors, from N-protected aminoaldehydes. The processes of the present invention provide high yields, can be conducted on multikilogram scale, and eliminate the need for chromatographic purification of intermediates or final product.

Method for preparing cyclic ureas and their use for the synthesis of HIV

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Wilmington, DE, United States of America

Robert E Waltermire