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Cedarburg Pharmaceuticals, Inc.

Scot W Weis

Richard J Pariza

Nathan W Stehle

Kevin Kunnen

John M Pascone

Scott G Van Ornum

Paul Zizelman

John P Maye

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). 

The present invention is directed to solid salts of hop acids and to processes for their production. Preferred are solid sodium and potassium salts of isoalpha acids rho-isoalpha acids, tetrahydroisoalpha acids, hexahydroisoalpha acids and beta acids.

Solid salts of hop acids

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Milwaukee, WI, United States of America

Scot W Weis