521300-99-2

Upstream product

• 35963-20-3 (R)-10-camphorsulfonic acid 
• 94666-07-6 5-[2-[2-(2-ethoxyphenoxy)-ethylamino]-2-methylethyl]-2-methoxybenzenesulfonamide 
• 112244-38-9 (+/-)-5-(2-aminopropyl)-2-methoxybenzenesulfonamide 
• 122-84-9 4-methoxybenzyl methyl ketone 
• 3259-03-8 2-(o-ethoxyphenoxy)-ethyl bromide 
• 80223-79-6 2-methoxy-5-(2-oxopropyl)benzenesulfonyl chloride 
• 116091-63-5 2-methoxy-5-(2-oxopropyl)benzenesulfonamide 
• 6781-16-4 (2-ethoxyphenoxy)methyl cyanide 
• 106463-17-6 (+)-Tamsulosin 
• 106133-20-4 (R)-tamsulosin 

Downstream Products

• 106133-20-4 tamsulosin hydrochloride 

Relevant academic research and scientific papers

Method of resolving tamsulosin enantiomer

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.

Process for the separation of R(-)-and S(+)-5-[2-[[2-(2-ethoxyphenoxy)ethyl]amino]propyl]-2-methoxybenzenesulfonamide

The process for separating the R(?)- and S(+)-5-[2-[[2-(2-ethoxyphenoxy)ethyl]amino]propyl]-2-methoxybenzene-sulfonamide enantiomers comprises (a) reacting a mixture of said enantiomers with an optically active organic acid to form diastereoisomeric salts with said enantiomers, where in said diastereoisomeric salts have different solubility and can be separated by crystallization; (b) separating the diastereoisomeric salt mixture enriched in the salt of one of the enantiomers; and (c) releasing said salts to obtain the R(?)or S(+) enantiomer. The R(?)-5-[2-[[2-(2-ethoxyphenoxy) ethyl]amino]propyl]-2-methoxybenzenesulfonamide enantiomer has α-adrenergic blocking activity and is useful as an antihypertensive agent suitable for the treatment of congestive heart failure and benign prostatic hypertrophy.