肽脂质(N~+C_5 Gly2C_(16))的合成改进

针对肽脂质(N+C5G ly2C16)的合成中分离纯化过程复杂,产率太低的问题,对它的合成过程尤其是产物纯化方法进行了改进。对每一步反应都进行了使产率明显提高的改进,尤其是叔丁氧甲酰甘氨酰双十六烷基胺油状物不经纯化即进行分解生成甘氨酰双十六烷基胺三氟乙酸盐。完全用重结晶取代了层析方法进行各步产物的纯化,使合成过程简捷、高效,肽脂质合成规模可以不受纯化方式的限制,合成总产率由2%提高到了23%。

Improvement on Peptide Lipid(N+C 5Gly2C 16) Synthesis

The study was made to solve the questions for lightening the onerous purification work and improving the very low yield of synthesis.Methods of recrystallization were used in preparation of the peptide lipid(N~+C_5Gly2C_(16)) instead of column chromatography completely.Simpler as well as more efficient synthesis course was obtained by the improvements on every step of the reaction,especially to make the oily N,N-dihexadecyl-N~α-(tbutoxylcarbonyl)glycinamide directly decomposed to form N,N-dihexadecylglycinamide trifluoroacetate without purification.Therefore the synthesis scale of the peptide lipid is not limited,and the yield of peptide lipid(N~+C_5Gly2C_(16)) increases from 2% to 23%.