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

US5530124A · kind A · utility

Assignee

• The DuPont Merck Pharmaceutical Company · US

Inventors

• Lilian A. Radesca · Newark, US
• Gregory D. Harris · Wilmington, US
• Edward K. W. Wat · Wilmington, US
• Robert E. Waltermire · Fryeburg, US

Key dates

• Filing date: Jun 30, 1994
• Grant date: Jun 25, 1996
• Expiry date: Jun 30, 2014

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07C223/02
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

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.