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8722316 
Journal Article 
Synthesis of azaspirocycles and their evaluation in drug discovery 
Burkhard, JA; Wagner, B; Fischer, H; Schuler, F; Müller, K; Carreira, EM 
2010 
Yes 
Angewandte Chemie (International Edition)
ISSN: 1433-7851
EISSN: 1521-3773 
49 
20 
3524-3527 
English 
20544904 
(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. 
Amines; Drug design; Heterocycles; Metabolism; Spiro compounds