New resolution approach for large-scale preparation of enantiopure didesmethylsibutramine (DDMS)

Z Han, D Krishnamurthy, QK Fang, SA Wald…

Index: Han, Zhengxu; Krishnamurthy, Dhileepkumar; Fang, Q. Kevin; Wald, Stephen A.; Senanayake, Chris H. Tetrahedron Asymmetry, 2003 , vol. 14, # 22 p. 3553 - 3556

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Abstract

Didesmethylsibutramine (DDMS) 1b represents one of the sibutramine 1a metabolites (Fig. 1) 1., 2. and 3. that was reported to be a more potent noradrenaline and serotonin reuptake inhibitor than the parent sibutramine itself. 4 Preliminary studies showed that the two enantiomers of DDMS exhibit different biological activities. 5 In order to support the preclinical studies, larger quantities of both enantiomers of DDMS were required. To meet this requirement, an efficient and ...

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