- Improved industrial synthesis of antidepressant sertraline
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(cis-1S)-4-(3,4-Dichlorophenyl)-1,2,3,4-tetrahydro-N-methyl-1-naphthalenamine hydrochloride, or sertraline hydrochloride, is a very effective antidepressant. This report presents a novel industrial synthesis of sertraline hydrochloride that is in many respects more advantageous than processes reported thus far. N-[4-(3,4-Dichlorophenyl)-3,4-dihydro-1(2H)-naphthalenylidene]-methanamine N-oxide is used as intermediate in our process, which is a stable compound in normal conditions. It can be obtained in a simple reaction from the corresponding tetralone in good yield, using acceptable reagents with regard to environmental and safety respects. Its reduction to the desired cis-racemic amine is stereoselective, and thus it provides sertraline hydrochloride with a purity required for pharmaceutical ingredients.
- Vukics, Krisztina,Fodor, Tamas,Fischer, Janos,Fellegvari, Iren,Levai, Sandor
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- An ortho-substituted BIPHEP ligand and its applications in Rh-catalyzed hydrogenation of cyclic enamides
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Matrix presented An ortho-substituted BIPHEP ligand, o-Ph-hexaMeO-BIPHEP (1), is designed and synthesized. Compared with chiral biaryl phosphines without ortho substituents such as BINAP and MeO-BIPHEP, o-Ph-hexaMeO-BIPHEP shows higher enantioselectivitie
- Tang, Wenjun,Chi, Yongxiang,Zhang, Xumu
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p. 1695 - 1698
(2007/10/03)
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