Synthesis of azaspirocycles and their evaluation in drug discovery

Abstract

(Figure Presented). Make It spirol Readily synthesized heteroatom- substituted spiro[3.3]heptanes generally show higher aqueous solubility than their cyclohexane analogues, and show a trend towards higher metabolic stability. The novel framework can be mounted onto scaffolds of druglike structures, such as fluoroquinolones, to afford active compounds with similar or even improved metabolic stability. © 2010 Wiley-VCH Verlag GmbH & Co. KGaA.