Diastereoisomeric tetrahydropyrido-(2,3,d) pyrimidine derivatives

US4927828A · kind A · utility

Assignee

• THE TRUSTEES OF PRINCETON UNIVERSITY · US

Inventors

• Edward C. Taylor · Princeton, US
• George P. Beardsley · Essex, US
• Chuan Shih · Carmel, US
• Stephen Robert Fletcher · Hamilton, CA

Key dates

• Filing date: Jun 28, 1988
• Grant date: May 22, 1990
• Expiry date: Jun 28, 2008

Classification

• Technology area (CPC Y): Emerging Cross-Sectional Technologies
• CPC primary: Y02P20/55
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

The diastereoisomeric forms of N-(4-[2-(2-amino-4-hydroxy-5,6,7,8-tetrahydropyrido[2,3-d]-pyrimidin-6-yl) ethyl]benzoyl)-L-glutamic acid are antineoplastic agents. The compounds are prepared by separation of the diastereoisomeric form of the correspondingly protected glutamic derivatives and hydrolytic or hydrogenolytic removal of carboxylic acid and/or amino protecting groups. Typical embodiments are the (R,S) and (S,S) forms of N-(4-[2-(2-amino-4-hydroxy-5,6,7,8-tetrahydropyrido[2,3-d]pyrimidin-6-yl)e thyl]benzoyl)-L-glutamic acid.