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2. 发明申请

WO2004087623A2 AN IMPROVED PROCESS FOR THE PREPARATION OF (R) (-) TAMSULOSIN HYDROCHLORIDE 审中-公开
标题翻译：（ - ）三羟甲基纤维素氢氯化物的制备方法的改进方法
公开(公告)号：WO2004087623A2
公开(公告)日：2004-10-14
申请号：PCT/IN2004/000054
申请日：2004-03-05
申请人： ALEMBIC LIMITED , SUHAS, Sohani , DEODHAR, Mandar Manohar , PATEL, Nishant Mahendra , PATEL, Manish K , KANSAL, Vinod Kumar
发明人： SUHAS, Sohani , DEODHAR, Mandar Manohar , PATEL, Nishant Mahendra , PATEL, Manish K , KANSAL, Vinod Kumar
IPC分类号： C07C
CPC分类号： C07C303/40 , C07B2200/07 , C07B2200/13 , C07C311/37
摘要： A process for the preparation of (R)(-) Tamsulosin hydrochloride [(R)(-)-5-[2-[[2-(o-ethoxy-phenoxy)ethyl]amino]-2-methylethyl]-2-methoxybenzenesulfonamide hydrochloride] of formula (III), The (R)(-) Tamsulosin hydrochloride of formula (III) produced by the process has an alpha-adrenergic blocking action and possesses a hypotensive activity and is used mainly for the treatment of benign prostatic hyperplasia (BPH). The process is directed to be high yielding, cost effective, easy to operate at industrial scale and does not involve the use of moisture sensitive, pyrophoric compounds. Importantly, the process would avoid unreacted contaminants in the final product and provide for isolating and obtaining the final product with good yield and purity. Advantageously, the process would not require the handling of hazardous reagents, such as LAH. The process is also selective, industrially favourable in that the same would use less amount of solvent, hence increase the plant capacity and will also require less manpower.
摘要翻译：制备（R）（ - ）盐酸坦索罗辛[（R）（ - ） - 5- [2 - [[2-（邻乙氧基 - 苯氧基）乙基]氨基] -2-甲基乙基] -2- 甲氧基苯磺酰胺盐酸盐]，式（III）的（R）（ - ）盐酸坦索罗辛盐酸盐通过该方法生产，具有α-肾上腺素能阻断作用，具有低血压活性，主要用于治疗良性前列腺增生（BPH）。该方法的目的是高产率，成本有效，易于在工业规模下运行，并且不涉及使用湿气敏感的自燃化合物。重要的是，该方法将避免最终产品中未反应的污染物，并提供分离和获得具有良好产率和纯度的最终产物。有利地，该方法不需要处理危险试剂，例如LAH。该方法也是选择性的，在工业上是有利的，因为同样使用较少量的溶剂，因此增加了设备容量并且也将减少人力。

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