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 R
1
and R
2
represent C
1
-C
4
alkyl groups) and their hydrochloride thereof, and other various pharmaceutical used salts.
Tamsulosin hydrochloride (R
1
=Et, R
2
=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.
本发明公开了一种合成
坦洛新及其芳基胺衍
生物的新工艺,特别是具有以下
化学式1的(R)-(−)-5-2-[2-(2-烷氧基苯氧基)乙基
氨基]丙基}-2-烷氧基苯磺酰胺(其中R1和R2代表C1-C4烷基基团)及其盐酸盐,以及其他各种药用盐。
坦洛新盐酸盐(R1=Et,R2=Me,在其盐酸盐形式中)是前列腺α-A
肾上腺素受体的拮抗剂。
坦洛新•HCl呈白色晶体,约在230°C左右分解熔化。它在
水和
甲醇中溶解度较低,在
冰乙酸和
乙醇中稍溶,在醚中几乎不溶。