The Synthesis Of Several Kinds Of Phosphatide Compounds

Phospholipids are the most important material to build liposome. In recent years, liposome,as the fourth generation of pharmaceutical formulation, is widely used in the field of medical preparations. High purity phosphatidylcholine (PC), phosphatidylserine (PS) and Methoxy polyethylene glycol 2000-distearoyl Phosphoethanolamine (mPEG2000-DSPE) are key materials in the preparation of liposome. soybean lecithin and lecithin are two widely used natural phospholipid, but the purity is low. they are unfit for the liposome membrane material. However,the purity of synthetic phospholipids is high,they are difficult to be oxidized, stabe to keep and suitable for preparing liposome.they should be of high economic value.The paper focus on the synthesis of phosphatidylcholine(PC), phosphatidylserine(PS) and Methoxy polyethylene glycol 2000-distearoyl Phosphoethanolamine (mPEG2000-DSPE), the purity can reach 98%.The highlights of this paper include:(1) in the synthesis of phosphatidylcholine, Diacylglycerol as the raw material, reacts with 2-bromoethyl phosphorodichloridate, then is hydrolyzed under alkaline conditions, trimethylamine gas is piped in. finally the phosphatidylcholine were obtained. This route has short steps, high yield, operates easily, avoids column chromatography. thus indicates a high prospect of industrial production; (2) in the synthesis of phosphatidylserine, Diacylglycerol reacts with phosphorus oxychloride, then L-serine which has been protected is added, finally hydrolyzed, deprotected, gives phosphatidyl serine. this method has short steps, easy to get raw materials, and can apply to industry. (3) in the synthesis of mPEG2000-DSPE, first, mPEG2ooo is activated by 4-Nitrophenyl chloroformate, then distearoyl Phosphoethanolamine(DSPE) reacts with this intermediate, gives the Methoxy polyethylene glycol 2000-distearoyl Phosphoethanolamine (mPEG2ooo-DSPE)?...