C - Chemistry – Metallurgy – 08 – B
Patent
C - Chemistry, Metallurgy
08
B
C08B 37/16 (2006.01) A61K 47/48 (2006.01) C07H 1/00 (2006.01)
Patent
CA 2240413
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.
En régulant la basicité de la réaction, il est possible d'effectuer de préférence l'alkylation des groupes hydroxyles secondaires de cyclodextrines. Ces groupes hydroxyles entourent l'entrée principale et large donnant accès à la cavité des cyclodextrines et, de cette manière, leur substitution par des substituants convenablement choisis peut améliorer la formation de complexes d'inclusion. Selon les procédés de l'invention, il est possible d'obtenir des dérivés de cyclodextrines substitués par des noyaux 1,4-dioxane condensés. Si l'on utilise un réactif doté d'une fraction alkylante, on forme un mélange d'éthers de cyclodextrine. Les procédés de cette invention permettent de diriger jusqu'à 96 % de la substitution sur les groupes hydroxyles secondaires.
Norton Rose Or S.e.n.c.r.l. S.r.l./llp
Pitha Josef
Roquette Freres
LandOfFree
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