11α-Nitroxy group was introduced into 17α-ethynylestradiol-3,17-diacetate using a scheme of synthesis involving the oxidative nitration by cerium ammonium nitrate and the inversion of the configuration at C11 by the reduction of 11-nitrated 9α,11β-dihydroxy derivative of the initial steroid with sodium borohydride. The obtained 11α-nitroxy analog of ethynylestradiol exhibits antiestgrogen activity.