Sukhanova Anna A, Prezent Mikhail A, Minyaev Mikhail E, Zavarzin Igor V
N. D. Zelinsky Institute of Organic Chemistry, Russian Academy of Sciences, 47 Leninsky Prosp., 119991, Moscow, Russian Federation.
National Research University Higher School of Economics (HSE University), 20 Myasnitskaya Str., 101000, Moscow, Russian Federation.
Chem Asian J. 2024 Dec 2;19(23):e202400595. doi: 10.1002/asia.202400595. Epub 2024 Oct 29.
A preparation method for steroid-based difluoroboron complexes has been developed using lumiestrone as a steroid example. Previously inaccessible lumiestrone-based difluoroboron complexes annulated at positions 16 and 17 of the D ring have been prepared. Such difluoroboron complexes may have large synthetic potential for heterofunctionalization of steroids at the D ring. An application of a borylation mixture AcO-BF⋅OEt significantly simplify the preparation of steroid "dimers" bearing two estrone moieties connected at positions 2 and 2' via a linker. Crystal structures of key representatives have been determined by X-ray diffraction.
以鲁米雌酮作为甾体示例，开发了一种基于甾体的二氟硼配合物的制备方法。此前难以获得的在D环16位和17位稠合的基于鲁米雌酮的二氟硼配合物已被制备出来。此类二氟硼配合物在甾体D环的杂官能化方面可能具有巨大的合成潜力。硼酸化混合物AcO - BF⋅OEt的应用显著简化了通过连接基在2位和2'位连接两个雌酮部分的甾体“二聚体”的制备。关键代表物的晶体结构已通过X射线衍射确定。
