Selective alkylations of cyclodextrins leading to derivatives which have a rigidly extended cavity
US5681828A · kind A · utility
Inventor
Key dates
| Filing date | Dec 19, 1995 |
| Grant date | Oct 28, 1997 |
| Priority date | — |
| Expiry date | Dec 19, 2015 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC08B37/0012
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
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.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.