| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1325773 | Journal of Organometallic Chemistry | 2006 | 7 Pages |
rac-Desmethoxy-sila-venlafaxine (rac-3) is a derivative of the noradrenaline-selective serotonin/noradrenaline reuptake inhibitor rac-sila-venlafaxine (rac-1b), a silicon analogue of the serotonin-selective serotonin/noradrenaline reuptake inhibitor rac-venlafaxine (rac-1a) (rac-1a, rac-1-[2-(dimethylamino)-1-(4-methoxyphenyl)ethyl]cyclohexan-1-ol; rac-1b, rac-1-[2-(dimethylamino)-1-(4-methoxyphenyl)ethyl]-1-silacyclohexan-1-ol). The synthesis and crystal structure analyses of rac-3 and rac-3 · HCl are reported, and the pharmacological properties of rac-1a, rac-1b, rac-2 (a sila-venlafaxine derivative with a silacyclopentanol skeleton instead of a silacyclohexanol framework), and rac-3 are compared (comparison of the pharmacological selectivity profiles with respect to serotonin, noradrenaline, and dopamine reuptake inhibition).
Graphical abstractThe syntheses and crystal structure analyses of rac-desmethoxy-sila-venlafaxine (rac-3) and its hydrochloride rac-3 · HCl are reported. Compound rac-3 is a derivative of rac-sila-venlafaxine (rac-1b), a sila-analogue of the serotonin/noradrenaline reuptake inhibitor rac-venlafaxine (rac-1a). The pharmacological properties of rac-1a, rac-1b, rac-2, and rac-3 are compared.Figure optionsDownload full-size imageDownload as PowerPoint slide
