An efficient, practical synthesis of 2-methoxyestradiol
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Updated: Jun 19, 2026

Synthesis of Esters Via a Greener Steglich Esterification in Acetonitrile
Published on: October 30, 2018
Minhang Xin1, Qidong You, Hua Xiang
1Department of Medicinal Chemistry, School of Pharmacy, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing 210009, PR China.
Abstract:
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.
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