Effective use of preparative chiral HPLC in a preclinical drug synthesis

• Published in: Chirality (New York, N.Y.) Vol. 16; no. 9; pp. 609 - 613
• Main Authors: Nelson, Todd D., Welch, Christopher J., Rosen, Jonathan D., Smitrovich, Jacqueline H., Huffman, Mark A., McNamara, James M., Mathre, David J.
• Format: Journal Article
• Language: English
• Published: Hoboken Wiley Subscription Services, Inc., A Wiley Company 2004
• Subjects: Amides - chemical synthesis; Amides - chemistry; automated chiral SFC screening; Chromatography, High Pressure Liquid; Chromatography, Supercritical Fluid; Drug Design; drug discovery/synthesis; Esters - chemical synthesis; Esters - chemistry; Indicators and Reagents; Lactones - chemical synthesis; Lactones - chemistry; Magnetic Resonance Spectroscopy; Pharmaceutical Preparations - chemical synthesis; Pharmaceutical Preparations - chemistry; preparative chiral HPLC; Stereoisomerism; δ-lactone
• ISSN: 0899-0042; 1520-636X
• DOI: 10.1002/chir.20081

Access to a key 3‐aryl‐δ‐lactone intermediate in enantiopure form using preparative chiral chromatography allowed expedited preparation of an important drug discovery target. A preclinical drug discovery strategy that combines rapid route discovery with effective use of preparative chiral chromatography can result in significant savings of both time and labor. Chirality 16:609–613, 2004. © 2004 Wiley‐Liss, Inc.