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Tetrahedron: Asymmetry

Practical synthesis of (3S, 4S)-3-methoxy-4-methylaminopyrrolidine

Y Tsuzuki, K Chiba, K Mizuno, K Tomita…

文献索引:Tsuzuki, Yasunori; Chiba, Katsumi; Mizuno, Kazuhiro; Tomita, Kyoji; Suzuki, Kenji Tetrahedron Asymmetry, 2001 , vol. 12, # 21 p. 2989 - 2997

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被引用次数: 27

摘要

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.