Effective use of preparative chiral HPLC in a preclinical drug synthesis.
Access to a key 3-aryl-delta-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.
Nelson
Todd D
TD
Department of Process Research, Merck Research Laboratories, Merck & Co., Rahway, NJ 07065, USA.
Welch
Christopher J
CJ
Rosen
Jonathan D
JD
Smitrovich
Jacqueline H
JH
Huffman
Mark A
MA
McNamara
James M
JM
Mathre
David J
DJ
D000577:Amides / Q000138:chemical synthesis / Q000737:chemistry; D002851:Chromatography, High Pressure Liquid; D025924:Chromatography, Supercritical Fluid; D015195:Drug Design; D004952:Esters / Q000138:chemical synthesis / Q000737:chemistry; D007202:Indicators and Reagents; D007783:Lactones / Q000138:chemical synthesis / Q000737:chemistry; D009682:Magnetic Resonance Spectroscopy; D004364:Pharmaceutical Preparations / Q000138:chemical synthesis* / Q000737:chemistry*; D013237:Stereoisomerism
D000577:Amides; D004952:Esters; D007202:Indicators and Reagents; D007783:Lactones; D004364:Pharmaceutical Preparations