Merck Sharp + Dohme Corp.

Wenyong Chen

Donald R Gauthier

Yang Cao

Alan Michael Hyde

Susan L Zultanski

Nadine Kuhl

Jamie M McCabe Dunn

The present invention provides processes for the preparation of sugammadex: (I) In one aspect, there is provided a process for the preparation of sugammadex from 8-per-deoxy-8-bromo-&#x3b3;-cyclodextrin and 3-mercaptopropionic acid. In another aspect, there is provided an alternative process for the preparation of sugammadex from 8-per-deoxy-8-bromo-&#x3b3;-cyclodextrin and disodium 3 -mercaptopropionate. In another aspect, there is provided a process for the preparation of 8-per-deoxy-8-bromo-&#x3b3;-cyclod extrin, which may be used in the production of sugammadex. In one such aspect, there is provided a process for the preparation of 8-per-deoxy-8-bromo-y-cyclodextrin from &#x3b3;-cyclodextrin and a brominating agent. In another such aspect, there is provided a process for the preparation of 8-per-deoxy-8-bromo-&#x3b3;-cyclodextrin comprising, inter alia, reacting &#x3b3;-cyclodextrin with an electrophilic brominating agent, a deoxygenating agent, and an acid in the presence of an organic solvent. 

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Princeton, NJ, United States of America

Wenyong Chen