Equilin and its derivatives are important active ingredients of conjugated estrogens, extracted from pregnant horse urine. However, they are still challenge synthetic targets due to the presence of an unstable non-conjugated double bond.Equilin(7), 17β-dihydroequilin(8) and 17α-dihydroequilin(9) were efficiently synthesized from commercially available 19-hydroxyandrost-4-ene-3,17-dione via retro-aldol aromatization with the overall yields of 32%, 37% and 25%, respectively.
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