Cedarburg Pharmaceuticals, Inc.

John M Pascone

Richard J Pariza

Nathan W Stehle

Kevin Kunnen

Scot W Weis

Scott G Van Ornum

Paul Zizelman

A method is provided for preparing an aromatase inhibitor of formula (I) wherein each of R, R, R, R, independently, is hydrogen, halogen or C-Calkyl. In one form, the aromatase inhibitor is exemestane wherein each of R, R, R, Ris hydrogen. In the method, a compound of formula (II) wherein R, R, R, Rare as defined above and R is alkylene, is reacted with a deprotonating agent and a compound of the formula RSOX wherein Ris C-Calkyl and X is halogen so as to obtain a compound of formula (III) wherein R, R, R, R, Rare as defined above. The compound of Formula (III) is then reacted with a base to form an aromatase inhibitor of formula (I).

Exemestane and its intermediates and methods of making the same

A method is provided for preparing an aromatase inhibitor of formula (I) wherein each of R, R, R, R, independently, is hydrogen, halogen or C-Calkyl. In one form, the aromatase inhibitor is exemestane wherein each of R, R, R, Ris hydrogen. In the method, a compound of formula (II) wherein R, R, R, Rare as defined above and R is alkylene, is reacted with a deprotonating agent and a compound of the formula RSOX wherein Ris C-Calkyl and X is halogen so as to obtain a compound of formula (III) wherein R, R, R, R, Rare as defined above. The compound of Formula (III) is then reacted with a base to form an aromatase inhibitor of formula (I). 

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Grafton, WI, United States of America

John M Pascone