Exemestane and Its Intermediates and Methods of Making the Same

摘要

A method is provided for preparing an aromatase inhibitor of formula (I) wherein each of R₁, R₂, R₃, R₄, independently, is hydrogen, halogen or C₁-C₆ alkyl. In one form, the aromatase inhibitor is exemestane wherein each of R₁, R₂, R₃, R₄ is hydrogen. In the method, a compound of formula (II) wherein R₁, R₂, R₃, R₄ are as defined above and R is alkylene, is reacted with a deprotonating agent and a compound of the formula R₅SO₂X wherein R₅ is C₁-C₅ alkyl and X is halogen so as to obtain a compound of formula (III) wherein R₁, R₂, R₃, R₄, R₅ are as defined above. The compound of Formula (III) is then reacted with a base to form an aromatase inhibitor of formula (I).