Compositions of (-)-e-10-oh-nt and methods for their...

Details Compositions of (-)-e-10-oh-nt and methods for their... Compositions of (-)-e-10-oh-nt and methods for their...

C - Chemistry, Metallurgy

07

C

C07C 215/42 (2006.01) A61K 31/135 (2006.01) A61P 25/00 (2006.01) A61P 25/04 (2006.01) A61P 29/00 (2006.01) C07C 35/37 (2006.01) C07C 213/02 (2006.01)

Patent

CA 2685395

This present disclosure provides compositions comprising E-10-0H-NT metabolites of AT and NT, methods for their synthesis and methods for their use In one embodiment, the compound (-)-E-5-(y-bromo.rho.ropylidene)-10,11-d.iota.hydro-IO-hydroxy-5H-dibenzo[a,d]- cycloheptene. Is prepared by reducing E-5-(y-bromopropylidene)-10,11d.iota.hydro-IO-oxo-5H-d.iota.benzo[a,d] ?cycloheptene in the presence of a crural-specific oxazaborolidine catalyst In another embodiment, method for inhibiting uptake of norepinephrine comprising contacting a norepinephrine transporter with a composition comprising E-IO-OH-NT that is enriched in the (-) enantiomer Is described

L'invention concerne des compositions comprenant des métabolites E-10-OH-NT de AT et NT, des procédés pour leur synthèse et des procédés pour leur utilisation. Dans un mode de réalisation, le composé (-)-E-5-(y-bromopropylidène)-10,11-dihydro-IO-hydroxy-5H-dibenzo[a, d]-cycloheptène est préparé en réduisant le (-)-E-5-(y-bromopropylidène)-10,11-dihydro-IO-oxo-5H-dibenzo[a, d]-cycloheptène en présence d'un catalyseur d'oxazaborolidine spécifique crurale. Dans un autre mode de réalisation, le procédé pour inhiber l'absorption de norépinéphrine comprenant la mise en contact d'un transporteur de norépinéphrine avec une composition comprenant E-10-OH-NT qui est enrichie en énantiomère (-) est décrit.

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