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Steroids

An efficient, practical synthesis of 2-methoxyestradiol.


PMID 19835898

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.