Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Carbohydrate doai
Patent
1997-10-24
1999-08-10
Ramsuer, Robert W.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Carbohydrate doai
536 186, 536103, 536124, A61K 31715, C08B 3716
Patent
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.
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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.
Hendricks Glenna
Oswecki Jane C.
Ramsuer Robert W.
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