An efficient, practical synthesis of 2-methoxyestradiol.
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.
Xin
Minhang
M
Department of Medicinal Chemistry, School of Pharmacy, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing 210009, PR China.
You
Qidong
Q
Xiang
Hua
H
D000077584:2-Methoxyestradiol; D000085:Acetates / Q000737:chemistry; D001965:Bromides / Q000737:chemistry; D002384:Catalysis; D003300:Copper / Q000737:chemistry; D004958:Estradiol / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry*; D009682:Magnetic Resonance Spectroscopy; D008956:Models, Chemical; D015394:Molecular Structure
D000085:Acetates; D001965:Bromides; C408079:cupric bromide; D004958:Estradiol; D000077584:2-Methoxyestradiol; C007650:ethyl acetate; D003300:Copper; C029892:cupric chloride