Alkylations of cyclodextrins leading to derivatives which have a

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Carbohydrate doai

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536 186, 536103, 536124, A61K 31715, C08B 3716

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active

059359412

ABSTRACT:
By controlling basicity of the reaction, is possible to alkylate preferentially the secondary hydroxyls of cyclodextrins. These hydroxyls surround the principal, wide, entry into the cyclodextrin cavity and, thus, their substitution by suitably chosen substituents can improve the formation of inclusion complexes. By methods of the invention, cyclodextrin derivatives substituted with fused 1,4-dioxane ring(s) can be obtained. If a reagent with one alkylating moiety is used, a mixture of ethers of cyclodextrin is formed. Using methods of this invention, up to 96% of the substitution can be directed to the secondary hydroxyls.

REFERENCES:
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patent: 4870060 (1989-09-01), Muller
patent: 5096893 (1992-03-01), Pitha et al.
patent: 5710268 (1998-01-01), Wimmer
Remington, "Pharmaceutical Sciences" 15th Mack Publishing Company, Easton, PA; p. 230, 1975.
Rao et al., "Substitution in .beta.-cyclodextrin Directed by Basicity: Org. Chem., 1991, 56, pp. 1327-1329.

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