Process for preparation of tamsulosin and its aralkylamine...

Organic compounds -- part of the class 532-570 series – Organic compounds – Amino nitrogen containing

Reexamination Certificate

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C564S084000

Reexamination Certificate

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11179568

ABSTRACT:
The present invention discloses a new process for the synthesis of tamsulosin and its aralkylamine derivatives, especially (R)-(−)-5-{2-[2-(2-alkoxyphenoxy) ethylamino]propyl}-2-alkoxybenzenesulfonamides having the following formula 1 (where R1and R2represent C1-C4alkyl groups) and their hydrochloride thereof, and other various pharmaceutical used salts.Tamsulosin hydrochloride (R1=Et, R2=Me, in its hydrochloride salt form) is an antagonist of α-A adrenoceptors in the prostate. Tamsulosin•HCl occurs as white crystals, which melt with decomposition at approximately 230° C. It is sparingly soluble in water and in methanol, slightly soluble in glacial acetic acid and in ethanol, and practically insoluble in ether.

REFERENCES:
patent: 2006/0036113 (2006-02-01), Xie
patent: WO2004/087623 (2004-10-01), None

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