| abstract |
The invention relates to an active targeting phospholipid and a synthesis process thereof, belonging to the technical field of chemical drug synthesis. The present invention uses raw material compound 1 (N'-nitro-L-arginine methyl ester hydrochloride), compound 2 (N-Boc-N'-Cbz-L-lysine), compound 5 (Fmoc-β ‑Cyclohexyl‑L‑alanine), compound 8 (tert-butyl glycine hydrochloride), compound 11 (Boc‑L‑aspartic acid‑4‑benzyl ester), DSPE‑PEG‑NHS were the starting points for the synthesis The material is subjected to amide condensation, cyclization, and deprotection group, and finally the active targeting phospholipid with the structural formula shown in formula A is prepared; A. The active targeting phospholipid with the structural formula represented by the formula A has a high grafting rate in the synthesis process; when the active targeting phospholipid having the structural formula represented by the formula A is loaded with an antitumor drug with poor water solubility, the drug The slow release of the drug is good. |