Cedarburg Pharmaceuticals, Inc.

Inspyr Therapeutics, Inc.

Genspera, Inc.

Kevin Kunnen

Richard J Pariza

Nathan W Stehle

Xiong Fu

Jeff Hutchison

John K Lynch

Scot W Weis

John M Pascone

Scott G Van Ornum

Paul Zizelman

Provided herein are methods of making the compound of Formula I: and certain intermediates involved in such process.

Methods of producing cancer targeting compounds

Methods of producing cancer treating compounds

Provided herein are methods of making the compound of Formula I: 

Methods of producing cancer compounds

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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Plymouth, IN, United States of America

Kevin Kunnen