School of Chemistry, University of Nottingham, University Park, Nottingham NG7 2RD, UK.
Sygnature Discovery Ltd, BioCity, Pennyfoot Street, Nottingham NG1 1GF, UK.
Bioorg Med Chem. 2018 Feb 15;26(4):791-797. doi: 10.1016/j.bmc.2017.12.012. Epub 2017 Dec 8.
A spirocyclic, sp-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.
通过金催化的丙炔醇重排，仅两步就合成了一个具有螺环、富 sp 原子的氧杂环丁烷骨架。关键的金环化反应可以在 40 克规模上进行，从而可以为欧洲先导化合物工厂（European Lead Factory）基于该骨架制备 419 种类似 lead 的化合物。
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