The invention discloses a method for the effective synthesis of optically active oxazoline-2-ketone derivative. The optically active oxazoline-2-ketone derivative has a structure represented by the formula (I), wherein, R is phenyl, para-methoxyphenyl, para-chlorophenyl, para-fluorophenyl, ortho-chlorophenyl, ortho-methoxyphenyl, meta-bromophenyl, 1-naphthyl, para-bromophenyl, para-nitrophenyl, para-methylphenyl or 3,4-difluorophenyl; R is phenyl, para-methylphenyl, para-methoxyphenyl, para-fluorophenyl, para-chlorophenyl, para-bromophenyl or 2-furyl. Such compounds can be obtained by means of high diastereoselectivity and high enantioselectivity of tandem reaction of organically catalytic C2 symmetrical chiral sulfur ylide and nitroolefin.