23/03/2006 · Original Article

The solution hydronaut in a suitable equipment, using up to 30% (weight/weight) of a hydrogenation catalyst such as palladium on charcoal, moistened with water, or palladium on calcium carbonate, hydrated with water, or one of similar catalysts containing platinum, mixture of CIS (+) sertraline and TRANS (-) sertraline.

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Arene amination is achieved by site-selective C–H zincation followed by copper-catalyzed coupling with -benzoylhydroxylamines under mild conditions. Key to this success is -zincation mediated by lithium amidodiethylzincate base that is effective for a wide range of arenes, including nonactivated arenes bearing simple functionalities such as fluoride, chloride, ester, amide, ether, nitrile, and trifluoromethyl groups as well as heteroarenes including indole, thiophene, pyridine, and isoquinoline. An analogous C–H azidation is also accomplished using azidoiodinane for direct introduction of a useful azide group onto a broad scope of arenes and heteroarenes. These new transformations offer rapid access to valuable and diverse chemical space of aminoarenes. Their broad applications in organic synthesis and drug discovery are demonstrated in the synthesis of novel analogues of natural product (−)-nicotine and antidepressant sertraline by late-stage amination and azidation reactions.

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Received sertraline hydrochloride moistened with solvent, can be used directly for further processing or, if necessary, storage, dried at a temperature of less than 80oWith, either at atmospheric or at reduced pressure.If the solvent in the hydrogenation reactions using toluene, sertraline mandelate can be obtained by mixing the filtrate obtained after the hydrogenation, from 0.9 to 1.5 equivalents of D-(-) is Uspenie/solution in ethanol.

Bupropion-SR, Sertraline, or Venlafaxine-XR after Failure of SSRIs for Depression
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23.03.2006 · Original Article

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