Enamine Ltd., Chervonotkatska 78, 02094 Kyiv, Ukraine.
J Org Chem. 2021 Oct 15;86(20):14061-14068. doi: 10.1021/acs.joc.1c00977. Epub 2021 Jun 24.
photochemical addition of propellane to diacetyl allowed construction of the bicyclo[1.1.1]pentane (BCP) core in a 1 kg scale within 1 day. Haloform reaction of the formed diketone in batch afforded bicyclo[1.1.1]pentane-1,3-dicarboxylic acid in a multigram amount. Representative gram scale transformations of the diacid were also performed to obtain various BCP-containing building blocks-alcohols, acids, amines, trifluoroborates, amino acids, .-for medicinal chemistry.
在 1 公斤规模内，经过 1 天时间，丙二炔与二乙酰的光化学反应可以构建二环[1.1.1]戊烷（BCP）核心。形成的二酮的卤仿反应以多克数量提供二环[1.1.1]戊烷-1,3-二羧酸。还进行了二酸的代表性克级转化，以获得各种含 BCP 的建筑块-醇、酸、胺、三氟硼酸盐、氨基酸等，用于药物化学。
