Department of Medicinal Chemistry, School of Pharmacy, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing 210009, PR China.
Steroids. 2010 Jan;75(1):53-6. doi: 10.1016/j.steroids.2009.09.013. Epub 2009 Oct 14.
An efficient and practical scheme to synthesize 2-methoxyestradiol has been developed. The key step was the copper-mediated methoxylation using ethyl acetate as a co-catalyst to introduce a methoxyl group. These synthetic procedures of four steps from 17beta-estradiol as starting material gave 2-methoxyestradiol with a 61% overall yield.
已经开发出一种高效实用的合成 2-甲氧基雌二醇的方案。关键步骤是使用乙酸乙酯作为共催化剂进行铜介导的甲氧基化反应，引入甲氧基。以 17β-雌二醇为起始原料，经过四步合成反应，总收率为 61%，得到 2-甲氧基雌二醇。
