Faculty of Pharmaceutical Sciences, Teikyo University, 2-11-1 Kaga, Itabashi, Tokyo 173-8605, Japan; AMED-CREST, The Japan Agency for Medical Research and Development (AMED), 1-7-1 Otemachi, Chiyoda-ku, Tokyo 100-0004 Japan.
Faculty of Pharmaceutical Sciences, Teikyo University, 2-11-1 Kaga, Itabashi, Tokyo 173-8605, Japan.
J Steroid Biochem Mol Biol. 2019 Dec;195:105477. doi: 10.1016/j.jsbmb.2019.105477. Epub 2019 Sep 18.
During our ongoing studies of vitamin D, we focused on the vitamin D side-chain 24-position, which is the major metabolic site of human CYP24A1. In order to inhibit the metabolism of vitamin D, 24,24-difluorovitamin Danalogues are important candidates. In this paper, we report the practical introduction of the difluoro-unit to the 24-position to synthesize 24,24-difluoro-CD ring (1) and 24,24-difluoro-25-hydroxyvitamin D (2).
在我们正在进行的维生素 D 研究中,我们专注于维生素 D 的侧链 24 位,这是人类 CYP24A1 的主要代谢位点。为了抑制维生素 D 的代谢,24,24-二氟维生素 D 类似物是重要的候选物。在本文中,我们报告了将二氟单元实际引入 24 位以合成 24,24-二氟-CD 环(1)和 24,24-二氟-25-羟基维生素 D(2)。