Prodn. of 7-substd. 1,3,5-oestratriene derivs. - via reaction of new 6-organo:sulphonyl-1,3,5,6-oestratetraene derivs. with nucleophile(s)

摘要

Prodn.of 7-substd. 1,3,5(10)-oestratrienes (I), where the substit. is bonded to the 7 posn. through a C atom, is effected by: (a) reacting a 6-organosulphonyl-1,3,5(10),6-oestratetraene deriv. of formula (II) with a cpd. (III) having a nucleophilic C atom; (b) opt. separating 7alpha and 7beta isomers; (c) opt. functionalising the 7-substit.; (d) reductively desulphonylating the prod.; and (e) opt. cleaving the 3-alkoxy gp. (if present): R1 = 1-8C alkyl, 1-10C alkanoyl or aroyl; R2 = 1-10C alkanoyl or aroyl; X = 1-8C alkyl or aryl. Also claimed are cpds. (II). USE - (I) include cpds. with oestrogenic or antioestrogenic activity, e.g, the antioestrogen 7alpha-(10-(N-butyl-N-methylcarbamoyl)-decyl)-1,3,5(10)- -oestratriene-3,17beta-diol (EP138504).