The present invention provides a process for preparing a modified lipid of the formula
comprising reacting
(I) a compound of the formula; and
(ii) a compound of the formula
wherein component (ii) is formulated as a liposome; wherein B is a lipid; wherein A is a moiety of interest (MOI) and is a hydrocarbyl group; wherein X is an optional linker group;
wherein R
1
is H or a hydrocarbyl group; and
wherein R
2
is a lone pair, H or a hydrocarbyl group.
The moiety of interest A may be selected from a carbohydrate moiety, a polymer, a peptide, a glycoprotein, a small biomolecule (such as a folic acid derivative) and a bioconjugate linker.
本发明提供了一种制备修改脂质的方法,其中包括反应(I)化合物的公式; 和(ii)的化合物的公式其中组分(ii)被构造为一个脂质体; 其中B是一种脂质; 其中A是一个感兴趣的基团(
MOI)且是一个烃基团; 其中X是一个可选的连接基团;其中R1是H或一个烃基团; 和其中R2是一个孤对,H或一个烃基团。感兴趣的基团A可以选择自
碳水化合物基团、聚合物、肽、糖蛋白、小
生物分子(如叶酸衍
生物)和
生物共轭连接剂。