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Densely functionalised spirocyclic oxetane-piperidine scaffolds for drug discovery
Bioorganic & Medicinal Chemistry ( IF 3.5 ) Pub Date : 2017-12-08 , DOI: 10.1016/j.bmc.2017.12.012
Gemma C. Geary , Andrew Nortcliffe , Christopher A. Pearce , Daniel Hamza , Geraint Jones , Christopher J. Moody

A spirocyclic, sp3-atom rich oxetane-containing scaffold was synthesised in just two steps via a gold catalysed propargylic alcohol rearrangement. The key gold cyclisation can be undertaken on a 40 g scale allowing the preparation of 419 lead-like compounds based on the scaffold for the European Lead Factory.



中文翻译:

功能强大的螺环氧杂环丁烷-哌啶骨架用于药物发现

经由金催化的炔丙醇重排仅两步合成了螺环,富含sp 3原子的氧杂环丁烷。关键的金环化反应可以40 g规模进行,从而可以基于欧洲铅厂的支架制备419种铅状化合物。

更新日期:2017-12-08
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