Konno K, Maki S, Fujishima T, Liu Z, Miura D, Chokki M, Takayama H
Faculty of Pharmaceutical Sciences, Teikyo University, Kanagawa, Japan.
Bioorg Med Chem Lett. 1998 Jan 20;8(2):151-6. doi: 10.1016/s0960-894x(97)10204-9.
A novel and practical route to the A-ring enyne synthon (2), which can be versatile for a variety of A-ring analogs of 1 alpha,25-dihydroxyvitamin D3 (1), was developed. This novel method led to an improved synthesis of the A-ring diastereomers of 1, the compounds 13-15, and synthesis of the new analogs, 2-methyl-1,25-dihydroxyvitamin D3 (4) with its all possible diastereomers. The biological evaluation of the 2-methyl analogs showed the alpha alpha beta-isomer to be more potent than 1.
开发了一种新颖且实用的合成A环烯炔合成子（2）的路线，该合成子可用于多种1α,25 - 二羟基维生素D3（1）的A环类似物。这种新方法改进了1的A环非对映异构体（化合物13 - 15）的合成，并合成了新的类似物2 - 甲基 - 1,25 - 二羟基维生素D3（4）及其所有可能的非对映异构体。对2 - 甲基类似物的生物学评估表明，ααβ - 异构体比1更具活性。
