Ejt. Dasilva et al., NOVEL-APPROACH TO THE SYNTHESIS OF THE AROMATASE INHIBITOR 4-HYDROXYANDROST-4-ENE-3,17-DIONE (4-OHA), Journal of the Chemical Society. Perkin transactions. I, (14), 1996, pp. 1649-1650
A straightforward synthesis of the title compound is achieved through
a novel approach, comprising the oxidation of the easily available 5 a
lpha-androst-3-en-17-one 1 in two sequential steps to yield the kineti
c diosphenol 4, which gives the desired 4-OHA 5 by base-catalysed isom
erization.