Taiwan Biotech Co., Ltd.

Well-being Biochemical Corp.

Wei Min Chang

Shwu Chen Tsay

Subhasish K Chakraborty

Asish R Das

Chin Kun Lu

Kuen Wang Sheu

Ru Hwu Jih

Balaachary Magendran

Chun Mei Shu

The present invention discloses a new process for the synthesis of tamsulosin and its aralkylamine derivatives, especially (R)-(&#x2212;)-5-{2-[2-(2-alkoxyphenoxy) ethylamino]propyl}-2-alkoxybenzenesulfonamides having the following formula 1 (where Rand Rrepresent C-Calkyl groups) and their hydrochloride thereof, and other various pharmaceutical used salts.  Tamsulosin hydrochloride (R=Et, R=Me, in its hydrochloride salt form) is an antagonist of &#x3b1;-A adrenoceptors in the prostate. Tamsulosin&#x2022;HCl occurs as white crystals, which melt with decomposition at approximately 230&#xb0; C. It is sparingly soluble in water and in methanol, slightly soluble in glacial acetic acid and in ethanol, and practically insoluble in ether.

Process for preparation of tamsulosin and its aralkylamine derivatives

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Taoyuan, Taiwan

Wei Min Chang