Abstract A highly efficient strategy has been developed for the synthesis of the cationic lipid, N-[2-({2, 5-bis [(3-aminopropyl) amino]-1-oxopentyl} amino) ethyl]-N, N-dimethyl-2, 3-bis [(1- oxo-9-octadecenyl) oxy] salt with hydrogen chloride (DOSPA). It involves the linkage of a cationic head group and a hydrophobic moiety in the presence of the standard coupling reagents.