Enamine Ltd., Chervonotkatska 78, 02094 Kyiv, Ukraine.
V.P. Kukhar Institute of Bioorganic Chemistry and Petrochemistry NAS of Ukraine, Murmanska 1, 02094 Kyiv, Ukraine.
J Org Chem. 2021 Feb 5;86(3):2200-2209. doi: 10.1021/acs.joc.0c02355. Epub 2020 Nov 19.
A synthetic strategy to fused bicyclic piperidines-building blocks for medicinal chemistry-is developed. The key step was an intramolecular [2 + 2]-photocyclization. The photochemical step was performed on a gram scale. Crystallographic analysis of the obtained compounds revealed that they occupy a novel chemical space and can be considered as elongated analogues of 3-substituted piperidines.
开发了一种融合双环哌啶的合成策略，这是药物化学的构建模块。关键步骤是分子内[2+2]光环化。该光化学步骤在克级规模上进行。获得的化合物的晶体结构分析表明，它们占据了一个新颖的化学空间，可以被认为是 3-取代哌啶的伸长类似物。
