Synthesis and Profiling of a Diverse Collection of Azetidine-Based Scaffolds for the Development of CNS-Focused Lead-like Libraries
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- 作者：Jason T. Lowe ; Maurice D. Lee ; IV ; Lakshmi B. Akella ; Emeline Davoine ; Etienne J. Donckele ; Landon Durak ; Jeremy R. Duvall ; Baudouin Gerard ; Edward B. Holson ; Adrien Joliton ; Sarathy Kesavan ; Berenice C. Lemercier ; Haibo Liu ; Jean-Charles Mari茅 ; Carol A. Mulrooney ; Giovanni Muncipinto ; Morgan Welzel-O鈥橲hea ; Laura M. Panko ; Ann Rowley ; Byung-Chul Suh ; Meryl Thomas ; Florence F. Wagner ; Jingqiang Wei ; Michael A. Foley ; Lisa A. Marcaurelle
- 刊名：The Journal of Organic Chemistry
- 出版年：2012
- 出版时间：September 7, 2012
- 年：2012
- 卷：77
- 期：17
- 页码：7187-7211
- 全文大小：714K
- 年卷期：v.77,no.17(September 7, 2012)
- ISSN：1520-6904
文摘
The synthesis and diversification of a densely functionalized azetidine ring system to gain access to a wide variety of fused, bridged, and spirocyclic ring systems is described. The in vitro physicochemical and pharmacokinetic properties of representative library members are measured in order to evaluate the use of these scaffolds for the generation of lead-like molecules to be used in targeting the central nervous system. The solid-phase synthesis of a 1976-membered library of spirocyclic azetidines is also described.