Preparations of 2,4-Disubstituted Oestradiols

Abstract

2,4-Dibromoestra-1,3,S(10)-triene-3,17 β- diol 3-(2'-hydroxyethyl) ether (8) undergoes reaction with copper(11) chloride/sodium methoxide to afford a 4-bromo [2,3]- dioxan derivative (9) as the major product together with a minor amount of a 2-bromo [3,4]- dioxan derivative (10). These compounds were used to prepare a number of 2,4-disubstituted oestradiol derivatives.   Alternative routes to other 2,4-disubstituted oestradiols are described.