Selective alkylations of cyclodextrins leading to derivatives wh

Details Selective alkylations of cyclodextrins leading to derivatives wh Selective alkylations of cyclodextrins leading to derivatives wh

1995-12-19

1997-10-28

Kight, John

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Carbohydrate doai

536103, 536124, A61K 31715, A01N 4304, C08B 3716, C07H 100

Patent

active

056818289

ABSTRACT:
By controlling basicity of the reaction, it 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:
patent: 4764604 (1988-08-01), Muller

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