- A new and direct asymmetric synthesis of a hindered chiral amine via a novel sulfinate ketimine derived from N-tosyl-1,2,3-oxathiazolidme-2-oxide: Practical asymmetric synthesis of (R)-sibutramine
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A novel and direct approach for the asymmetric synthesis of (R)-sibutramine via chiral amine 5 using N-tosyl-1,2,3-oxathiazolidine-2-oxide (13) as a recyclable chiral auxiliary is described. Chiral sulfinate imine 16e was obtained by treatment of 13e with
- Han, Zhengxu,Krishnamurthy, Dhileepkumar,Senanayake, Chris H.
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- PHENYLCYCLOBUTYLAMIDE DERIVATIVES AND THEIR STEREOISOMERS, THE PREPARATION PROCESSES AND USES THEREOF
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Phenylcyclobutylamide derivatives and their optical isomers, the preparing processes and the uses thereof, which includes the compounds of formula (I), their pure stereoisomers and their pharmaceutically acceptable salts. In formula (I), R is H, formacyl,
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- PHENYLCYCLOBUTYLAMIDE DERIVATIVES AND THEIR STEREOISOMERS, THE PREPARING PROCESSES AND THE USES THEREOF
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Phenylcyclobutylamide derivatives and their optical isomers, the preparing processes and the uses thereof, which includes the compounds of formula (I), their pure stereoisomers and their pharmaceutically acceptable salts. In formula (I), R is H, formacyl,
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Page/Page column 8
(2010/12/30)
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- DOPAMINE-AGONIST COMBINATION THERAPY FOR IMPROVING SLEEP QUALITY
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The present invention generally to pharmaceutical compositions comprising a dopamine agonist and sedative agent. In a preferred embodiment, the dopamine agonist is optically pure (S)-didesmethylsibutramine. In a preferred embodiment, the sedative agent is
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Page/Page column 90-91
(2008/06/13)
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- A method of manufacturing an amine stereoisomerically
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This invention provides intermediates useful in a method of preparing amine stereoisomers. It also provides a method of preparing sulfoxide and sulfinylamine stereoisomers using certain of the intermediates.
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Page/Page column 53
(2010/02/12)
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- New resolution approach for large-scale preparation of enantiopure didesmethylsibutramine (DDMS)
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An improved synthesis and efficient resolution method to prepare both enantiopures of DDMS using crystallization of enantiomerically pure tartaric acid salts of racemic DDMS are disclosed.
- Han, Zhengxu,Krishnamurthy, Dhileepkumar,Fang, Q. Kevin,Wald, Stephen A.,Senanayake, Chris H.
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p. 3553 - 3556
(2007/10/03)
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- Therapeutic agents
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The present invention provides a method of treating and preventing obesity and related co-morbid conditions comprising the administration of a therapeutically effective amount of one or more monoamine reuptake inhibitors which are serotonin reuptake inhibitors and/or noradrenaline reuptake inhibitors and a 5-HT1A agonist to a patient in need thereof.
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- First application of tunable alkyl or aryl sulfinamides to the stereoselective synthesis of a chiral amine: asymmetric synthesis of (R)-didesmethylsibutramine ((R)-DDMS) using (R)-triethylmethylsulfinamide ((R)-TESA).
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A highly diastereoselective addition of i-BuLi to a triethylmethylsulfinamide derived aldimine was used as the key step in the first asymmetric synthesis of (R)-didesmethylsibutramine, a metabolite of sibutramine for the potential treatment of CNS disorders. [reaction: see text]
- Han, Zhengxu,Krishnamurthy, Dhileepkumar,Pflum, Derek,Grover, Paul,Wald, Stephen A,Senanayake, Chris H
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p. 4025 - 4028
(2007/10/03)
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