N-(间马来酰亚胺苯甲酰)二棕榈酰磷脂酰乙醇胺的合成

Synthesis of N-(m-Maleimidobenzoyl)dipalmitoylphosphatidylethanolamine

间氨基苯甲酸与马来酸酐反应生成酰胺化合物,经脱水环合用N-羟基琥珀酰亚胺活化羧基,与二棕榈酰磷脂酰乙醇胺反应生成N-(间马来酰亚胺苯甲酰)二棕榈酰磷脂酰乙醇胺,总收率约29%。可用于制备主动靶向长循环脂质体。

The key amide intermediate was prepared from m-aminobenzoic acid with maleic anhydride, then followed by cyclodehydration, activation with N-hydroxysuccinimide to give N-（m-maleimidobenzoyloxy）- succinimide, finally it was subjected to react with 1,2-dipalmitoylglycero-3-phospho-ethanolamine （DPPE） to the N- （m-maleimidobenzoyl） dipalmitoylphosphatidylethanolamine, a useful excipient for preparing the sterically stabilized immtmoliposome, with an overall yield of about 29 %.