- Preparation method of 1-(2,5-dimethoxy phenyl)-2-aminoethanol
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The invention provides a preparation method of hydrochloric acid midodrine intermediate 1-(2,5-dimethoxy phenyl)-2-aminoethanol, comprising the steps of adopting 2,5-dimethoxy benzaldehyde as the raw material to condense with nitromethane under the effect of alkali to obtain 1-(2,5-dimethoxy phenyl)-2-nitroethanol, reducing 1-(2,5-dimethoxy phenyl)-2-nitroethanol with a boron reductant to obtain 1-(2,5-dimethoxy phenyl)-2-aminoethanol. The preparation method of 1-(2,5-dimethoxy phenyl)-2-aminoethanol has the advantages of being mild in reaction conditions, simple in the operation process, high in yield, environment-friendly and low in production cost, and is applicable to industrial production.
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Paragraph 0032; 0035; 0036
(2017/03/08)
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- Asymmetric hydrogenation of α-primary and secondary amino ketones: Efficient asymmetric syntheses of (-)-arbutamine and (-)-denopamine
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Two ss-receptor agonists (-)-denopamine and (-)-arbutamine were prepared in good yields and enantioselectivities by asymmetric hydrogenation of unprotected amino ketones for the first time by using Rh catalysts bearing electron-donating phosphine ligands. A series of α-primary and secondary amino ketones were synthesized and hydrogenated to produce various 1,2-amino alcohols in good yields and with good enantioselectivies. This Rh electron-donating phosphine-catalyzed asymmetric hyderogenation repI resents one of the most promising and convenient approaches towards the asymmetric synthesis of chiral amino alcohols.
- Shang, Gao,Liu, Duan,Allen, Scott E.,Yang, Qin,Zhang, Xumu
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p. 7780 - 7784
(2008/04/03)
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- Synthesis of midodrine HCI from a novel intermediate 1-(2′,5′-dimethoxyphenyl)-2-azidoethanone
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Midodrine hydrochloride, ±1-(2′,5′-dimethoxyphenyl)-2-glycineamido-ethanol-(1)-HCl, is prepared from a novel intermediate, 1-(2′,5′-dimethoxyphenyl)-2-azidoethanone.
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- USE OF ALPHA1A-SELECTIVE ADRENOCEPTOR AGONISTS FOR THE TREATMENT OF URINARY INCONTINENCE
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The present invention provides a method of treating urinary incontinence in a subject which comprises administering to the subject a therapeutically effective amount of a compound having the following structure: STR1 wherein each of the substiutents for the compound is as defined in the specification.
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- Synthesis and adrenergic properties of new duplicated analogs of methoxamine
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New duplicated analogs of the α1-selective agonist methoxamine and of its cyclic derivative 5,8-dimethoxy-1,2,3,4-tetrahydro-2-naphthylamine have been synthesized and tested for their adrenergic properties. All the compounds prepared, presenting a polymethylene spacer of varying length between two units of the active structure, turned out to be completely devoid of any α-stimulating activity. Surprisingly, some of them showed a marked β-adrenergic agonistic effect, being the most interesting compound active at nanomolar concentration.
- Perez,Rosell,Mauleon,Carganico
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p. 1155 - 1166
(2007/10/02)
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- Conformational Effects on the Activity of Drugs. 10. Synthesis, Conformation, and Pharmacological Properties of 1-(2,5-Dimethoxyphenyl)-2-aminoethanols and Their Morpholine Analogues
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In order to obtain a better understanding of the effects that structural parameters have on the changes of adrenergic activity when 1-aryl-2-aminoethanol derivatives are converted into their corresponding 2-arylmorpholine cyclic analogues, we synthesized 1-(2,5-dimethoxyphenyl)-2-aminoethanol derivatives 5-7 and their morpholine analogues 8-10.The preferred conformations of amino alcohols and their cyclic analogues have been determined through an 1H NMR and IR study.Compounds 5 and 6 showed both α-stimulating and α-blocking activity on rat vas deferens, the effect depending on the concentration employed; on the same isolated tissue, N-isopropyl derivative 7 and the morpholine analogues 8-10 exhibited only α-blocking activity.As for the β-adrenergic activity, only the open-chain compound 7 possessed a moderate blocking effect on isolated guinea pig atria.The results of this work seem to indicate that the changes of pharmacological activity involved in the transformation of the adrenergic drugs into their morpholine analogues are influenced more by characteristic features of the aromatic moiety than by the ethanolamine or propanolamine structure of the drug.
- Epifani, E.,Lapucci, A.,Macchia, B.,Macchia, F.,Tognetti, P.,et al.
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p. 254 - 259
(2007/10/02)
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