Abbott Laboratories Corporation

Weijang Zhang

Anthony Ralph Haight

Bikshandarkoil A Narayanan

Margaret Chi-Ping Hsu

Matthew John Peterson

An efficient arylation technique for use in the synthesis of erythromycin derivatives, involving a modified Heck reaction which employs less than six mole percent of palladium catalyst and no phosphine is disclosed. With this modified Heck reaction, an O-alkenylaryl macrolide can be obtained in a much shorter reaction time than under conventional Heck reaction conditions. The modified Heck reaction can be utilized in a method for phosphine-free arylation of an O-allylic erythromycin derivative, in a method for preparing an O-alkenylaryl erythromycin A derivative, or in a method for preparing a 2', 4&#x2033;-hydroxyl protected 6-O-alkenylaryl erythromycin A derivative.

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Grayslake, IL, United States of America

Weijang Zhang