A simple, inexpensive apparatus for performance of preparative scale solution phase multiple parallel synthesis of drug analogs. I. Preparation of a retrospective library of quinolone antiinfective agents.
A simple inexpensive apparatus is described consisting of conveniently commercially available components which is suitable for the solution phase multiple parallel synthesis of 24-72 analogs of drug-like molecules. The use of the apparatus is illustrated by preparation of a retrospective library of over 100 analogs of antimicrobial fluoroquinolones prepared in 0% to quantitative yields. Each analog was prepared in up to 150 mg quantity and each was analyzed by NMR and mass spectrometric techniques to verify its purity and identity.
Frank
K E
KE
Department of Medicinal Chemistry, Kansas University, Lawrence 66045-2506, USA.
Jung
M
M
Mitscher
L A
LA
D000890:Anti-Infective Agents / Q000032:analysis* / Q000138:chemical synthesis* / Q000737:chemistry; D002626:Chemistry, Pharmaceutical / Q000295:instrumentation* / Q000379:methods; D024841:Fluoroquinolones; D009682:Magnetic Resonance Spectroscopy; D013058:Mass Spectrometry
D000890:Anti-Infective Agents; D024841:Fluoroquinolones