Vysoka Skola Chemicko-technologicka V Praze

Vyzkumny Ustav Veterinarniho Lekarstvi, V.v.i.

Apigenex S.r.o.

Elissa Bartheldyova

Ladislav Droz

Jaroslav Turanek

Miroslav Ledvina

Roman Effenberg

Josef Masek

Frantisek Hubatka

New aminooxylipids of general formula I, wherein n=5-30 and X is polymethylene linker of the general formula II where n=2-10, or X is polyethylene glycol linker of the general formula III, wherein n=1-14 are provided. A method of preparation of the aminooxylipids of general formula I characterized in that the acylation of N-tert-butoxycarbonyl-polymethylenediamine {(CH)C&#x2014;O&#x2014;(C&#x2550;O)&#x2014;HN&#x2014;(CH)&#x2014;NH, n=2-13}, or N-tert-butoxycarbonyl-polyethyleglycoldiamine {(CH)C&#x2014;O&#x2014;(C&#x2550;O)&#x2014;HN&#x2014;(CH)&#x2014;[O&#x2014;(CH)]&#x2014;O&#x2014;(CH)NH, n=1-14} with in position C(2) symmetrically branched fatty acids of general formula IV, wherein n=5-30, in the presence of condensation reagent, or from acid of general formula IV derived acylchloride of general formula V wherein n=5-30, produces N-Boc-aminolipids of general formula VI, wherein n=5-30 a X is polymethylene linker of the general formula II or X is polyethylene glycol linker of the general formula III.

Aminooxylipids for the construction of self-assembling liposomal systems enabling their subsequent modification by biologically functional molecules

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Unin, Czechia

Elissa Bartheldyova