CYCLISATION SUBSTRATES AND RELATED 11(ALPHA)- EQUATORIALLY-SUBSTITUTED STEROIDS

Novel and biologically active cyclisation substrates and their method of preparation are disclosed of the formula: (I) wherein (a) R1 is H or alkyl of one to four carbon atoms; (b) R2 is H or alkyl of one to four carbon atoms, with the proviso that R1 is H when X2 is alkyl, and with the proviso that R2 is H when R1 is alkyl: (c) R3 is a suitable leaving group selected from the group consisting of hydroxy, alkoxy of one to four carbons, alhoxyalkoxy of two to four carbons, acyloxy of one to about seven carbon atoms, and trialkylsilyloxy of less than fifteen carbons: (d) R4 is hydrocarbyl of one to four carbons, and (e) R5(1) and R5(2) are each H, alkyl of one to eight carbons, or an optionally esterified or etherified hydroxy group selected from the group consisting of hydroxy, alkoxy of one to four carbons, alkoxyalkoxy of two to four carbons, trialkylsilyloxy of one to fifteen carbons, cycloalkoxy of four to eight carbons. acyloxy of one to seven carbons or heterocyclic ether of five to seven atoms and four to six carbons, with the proviso that at least one of R5(1) and R5(2) is hydrogen. A method is disclosed for the cyclisation of the compounds of formula I leading to novel and biologically active compounds of the following formulae:(II) (III) "para" "ortho" having R4 and R5 (one of R5(1) and R5(2) that may or may not be hydrogen) as defined above. with R6 being alkyl of from one to about four carbon atoms.