Three synthetic methods for the preparation of (3S, 4S)-3-methoxy-4-methylaminopyrrolidine , an important intermediate in the synthesis of the novel quinolone antitumor agent, AG- 7352, have been developed. By one route, an efficient and large-scale preparation of the chiral pyrrolidine could be achieved through resolution of (±)-1-Boc-3-benzylamino-4- hydroxypyrrolidine, which is prepared from either 3-pyrroline or 1, 4-dichloro-2-butene.