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Ortho-mcneil Pharmaceutical Corp.

Walter E Stalzer

Cynthia Anne Maryanoff

William R Dolbier, Jr

Penina Feibush

Thomas W Adkins

Xiao X Rong

Charles F Cicco

Donald A Koch

The present invention is directed to a continuous process for the preparation of fructopyranose sulfamate derivatives of the general formula (I) 

Continuous process for the preparation of fructopyranose sulfamate derivatives

A method of making TFPX using an S,2 type nucleophilic displacement reaction. The method includes reacting a nucleophilic fluorine molecule with a nonfluorinated-tetrahalo-p-xylene molecule. Exemplary nucleophilic fluorine molecules include, but are not limited to, CsF, KF, NaF and LiF. The nonfluorinated-tetrahalo-p-xylene molecules may include, &agr;,&agr;,&agr;&prime;,&agr;&prime;-tetrachloro-p-xylene, &agr;,&agr;,&agr;&prime;,&agr;&prime;-tetrabromo-p-xylene or &agr;,&agr;,&agr;&prime;,&agr;&prime;-tetraiodo-p-xylene. The reaction may be carried out in an open or closed container. Furthermore, the reaction may be carried out in the presence of a phase transfer catalyst. In certain embodiments, the reaction is carried in a substantially solvent-free environment.

TFPX synthesis

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Mentor, OH, United States of America

Walter E Stalzer