The United States of America as Represented by the Department of Health

Josef Pitha

Bengt Lindberg

C Trinadha Rao

A process for producing monosubstituted alpha-, beta-, and gamma-cyclodextrins includes the step of condensing an excess of a cyclodextrin with an epoxide under alkaline conditions. A process for increasing the solubility of cyclodextrins includes the step of reacting a cyclodextrin with an amine under heterogenous catalytic conditions, or subjecting the cyclodextrin to sulfatation. Compositions useful in these processes include one containing at least one cyclodextrin, ammonia and Raney nickel, and a second composition containing at least one cyclodextrin, chlorosulfonic acid and pyridine.

Preparation of specifically substituted cyclodextrins

A method for obtaining a desired pattern of substitution of hydroxyalkyl groups on cyclodextrins which comprises controlling the basicity of a reaction mixture comprising epoxide and cyclodextrins and a suitable solvent. Through the proper control of basicity with, e.g., sodium hydroxide, hydroxyalkyl substitution may be directed either toward the narrow or wide opening of the cavity of cyclodextrins.

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Stockholm, Sweden

Bengt Lindberg