116091-63-5Relevant articles and documents
Method of resolving tamsulosin enantiomer
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Paragraph 0152-0156, (2017/08/29)
The invention relates to a method of resolving tamsulosin enantiomer, and in particular, relates to a method of resolving tamsulosin, represented as the formula (I), into an R-enantiomer and an S-enantiomer. The method includes the steps of: (a) dissolving a solid mixture of (R)-tamsulosin free alkali and (S)-tamsulosin free alkali in a solvent and performing a reaction to the free alkalis with camphor-10-sulfonic acid to form a solution containing a pair of diastereomeric camphor-10-sulfonates of tamsulosin, and then preferentially precipitating one diastereomeric camphor-10-sulfonate of the tamsulosin from the solution containing a pair of the diastereomeric camphor-10-sulfonates of tamsulosin, thereby forming a precipitate, in which one diastereomer is enriched, and a solute, in which the other one diastereomer is enriched; and (b) from one of the precipitate and the solute, releasing tamsulosin free alkali to obtain optical-rotation-enriched tamsulosin free alkali. The method has excellent technical performance.
A METHOD OF PREPARATION OF (R)-(-)-5(2-AMINOPROPYL)-2-METHOXYBENZENESULFONAMIDE
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Page/Page column 9, (2008/06/13)
A method of preparation of (R)-(-)-5-(2-aminopropyl)-2-methoxybenzenesulfonamide of formula I and its use for production tamsulosin. A protective group is introduced to N-[(1R)-2-(4-methoxyphenyl)-1-methylethyl]-N- [(1 R)-1-phenylethyl)]amine and the resulting amide of formula IX is chlorosulfonated and the resulting sulfochloride is converted to a sulfonamide of formula X, from which the compound of formula I is obtained by hydrogenation.
TAMSULOSIN DERIVATIVE
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Page/Page column 17, (2008/06/13)
The optically active compound, R (-)-5-[2-[[2-(2-ethoxyphenoxy)ethyl] amino] propyl]-2-hydroxybenzenesulfonamide in good chemical and optical purity, a metabolite of the α1-adrenergic blocking agent tamsulosin, and methods for the preparation thereof. Pharmaceutical compositions including the optically active compound and methods of treatment comprising direct administration of an effective α1-adrenergic antagonistic amount of such compositions to mammals.