- COMPOSITIONS AND METHODS FOR CYCLOFRUCTANS AS SEPARATION AGENTS
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The present invention relates to derivatized cyclofructan compounds, compositions comprising derivatized cyclofructan compounds, and methods of using compositions comprising derivatized cyclofructan compounds for chromatographic separations of chemical species, including enantiomers. Said compositions may comprise a solid support and/or polymers comprising derivatized cyclofructan compounds.
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Page/Page column 45-49; 60
(2010/12/31)
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- PROCESS FOR THE PREPARATION OF MIDODRINE, PHARMACEUTICALLY-ACCEPTABLE SALTS THEREOF AND INTERMEDIATES
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The present invention provides for a novel process for the preparation of Midodrine or a pharmaceutically acceptable salt thereof comprising: (a) a step of reacting 2-amino-1-(2’,5’-dimethoxyphenyl) ethanol of formula (I) with an N-protected glycine of formula (II) containing an amino protecting group in the presence of 1,1’-carbonyldiimidazole (CDI); and (b) removing the amino protecting group by deprotection formula (I), formula (II), wherein R1 is a benzyl, triphenylmethyl, tert-butyloxycarbonyl, or a benzyloxycarbonyl group. This results in an unexpectedly efficient and cost-effective process. Additionally, the process is simple and safe as all the intermediates and reagents involved in the process pose no safety risks. Further reaction of Midodrine with a pharmaceutically acceptable acid affords a pharmaceutically acceptable salt thereof. Preferably, the pharmaceutically acceptable salt obtained from the process according to the present invention is Midodrine Hydrochloride.
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- AN IMPROVED PROCESS FOR THE SYNTHESIS OF (±) 2-AMINO-N-[2,(S,5-DIMETHOXYPHENYL)-2-HYDROXYETHYL] ACETAMIDE MONOHYDROCHLORIDE
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This invention relates to an improved process for synthesizing (±) 2-Amino-N-[2,(S,5-dimethoxyphenyl)-2-hydroxyethyl] acetamide monohydrochloride in good yield and in a cost effective manner from 1-(2,5dimethoxyphenyl)-2-bromoethanone by reacting the same
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- Process for the synthesis of (+) 2-amino-n-{2, (2,5-dimethoxy phenyl)-2-hydroxyethyl} acetamide monohydrochloride
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This invention relates to an improved process for synthesizing (±)-2-Amino-N-[2-(2,5-dimethoxyphenyl]-2-hydroxyethyl acetamide monohydrochloride in good yield and in a cost effective manner from 1-(2,5-dimethoxyphenyl)-2-bromoethanone by reacting the same
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- Process for the preparation of Midodrine
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The invention provides a process for the preparation of 2-amino-N-[2-(2,5-dimethoxyphenyl)-2-hydroxyethyl]acetamide of the formula 1 by hydrogenolysis of substituted 2-dibenzylamino-N-[2-(2′,5′-dimethoxyphenyl)-2-hydroxy-ethyl]acetamide having the formula
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- A process for the preparation of midodrine
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The invention provides a process for the preparation of 2-amino-N-[2-(2,5-dimethoxyphenyl)-2-hydroxyethyl]acetamide of the formula 1 by hydrogenolysis of substituted 2-dibenzylamino-N-[2-(2',5'-dimethoxyphenyl)-2-hydroxy-ethyl]acetamide having the formula (5), wherein Ar and Ar' are aryl groups.
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- A Separation Procedure for the Preparation of Enantiomerically Pure Midodrine
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Racemic midodrine chlorohydrate (rac-1) was N-protected to yield the racemic products rac-2a-c. These were converted into the diastereomeric O-acetals 3a-c/4a-c, which can easily be separated by chromatography. After removal of the N- and O-protective gro
- Noe,Knollmüller,G?rtner
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p. 159 - 165
(2007/10/03)
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- Aminoalcohols, III: Preparation of Enantiomerically Pure Pharmacologically Active N-Substituted β-Aminoalcohols
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A synthesis of N-substituted β-aminoalcohols is described starting from enantiomerically pure O-MBF- or O-MBE-protected β-aminoalcohols which can be prepared via LiAlH4 reduction of O-protected cyanohydrines. - Keywords: 1,2-Amino-alcohols, enantiomerically pure; N-Alkylation; Clorprenaline; Propranolol; Midodrine
- Noe, C. R.,Knollmueller, M.,Gaertner, P.,Fleischhacker, W.,Katikarides, E.
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p. 557 - 564
(2007/10/02)
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