The invention discloses a kind of methods of enantioselective synthesis for cis-imidazolines and in relation to structure by chiral resolution. A pair of of chiral acid is from a kind of racemic mixture by selective freezing for separating the enantiomer precursor of cis-imidazolines. Two enantiomers can be cyclized into required cis--imidazoline by complementary pathway. Compound can synthesize an enantiomeric excess high as 99% and can be used for treating cancer, kill senile cell, or processing aging-associated condition.