NOVEL POSITIVELY CHARGED LIPIDS AND LIPOSOMES COMPRISING THE POSITIVELY CHARGED LIPIDS

摘要

PURPOSE: A method for preparing a cationic lipid using glutamate, a method for preparing a cationic lipid KE-DM, cationic lipids prepared by the methods, a liposome containing the cationic lipid and a DNA-liposome complex containing the liposome are provided, to improve the DNA delivery efficiency of a liposome. CONSTITUTION: The cationic lipid is prepared by preparing a compound of the formula III by esterification of an amino group-protected glutamate (I) and an alcohol (II); removing R1 at the compound of the formula III to obtain a compound of the formula IV; coupling the compound of the formula IV and an activated compound of the formula V to obtain a compound of the formula IV; and removing R3 at the compound of the formula VI and forming its salt to obtain a cationic lipid of the formula VII (See the reaction scheme 1), wherein R1 and R3 are a benzyl carbamate, p-methoxybenzyl carbamate, 9-fluoromethyl carbamate, t-butyl carbamate or 1-adamantyl carbamate group; R2 is H, an alkyl group of C10-C18 or an alkenyl group of C10-C18; and X is F, Cl, Br, I, CF3CO2, HSO4 or NH3.