已合成了36个二取代的,单取代的和两个三取代的磺酰胺,并研究了它们在碱中的电离平衡(方案1-3)。许多磺酰胺是新材料。在Hammett和Taft图中,已将每个系列获得的p K a值关联起来。对于邻近氢的电离获得的哈米特ρ值约为。2.3。用于“远程”氢离子化获得的Taftρ*值为1.68。六元环状磺酰胺比其无环类似物的酸性大约高出约2。2.5 p ķ一个单元和五元环sulphamides是CA。4 p K a单元比模型开放链对应单元酸性更高。硫d-轨道参与和环应变被认为是这种“增强酸”作用的可能来源。
[EN] PREPARATION OF R-5-(2-(2-ETHOXYPHENOXYETYLAMINO)PROPYL)-2- METHOXYBENZENESULPHONAMIDE HYDROCHLORIDE OF HIGH CHEMICAL<br/>[FR] PREPARATION DE R-5-(2-(2-ETHOXYPHENOXYETYLAMINO)PROPYL)-2- METHOXYBENZENESULPHONAMIDE CHLORHYDRATE A PURETE CHIMIQUE ELEVEE
申请人:LEK PHARMACEUTICALS
公开号:WO2005063702A1
公开(公告)日:2005-07-14
In the present invention, the process for the preparation of tamsulosin hydrochloride and subsequent purification with thermal crystallisation to provide essentially pure tamsulosin hydrochloride is disclosed.
Graf, Chemische Berichte, 1959, vol. 92, p. 509,513
作者:Graf
DOI:——
日期:——
Kirsanow; Solotow, Zhurnal Obshchei Khimii, 1958, vol. 28, p. 343,346;engl.Ausg.S.340,342
作者:Kirsanow、Solotow
DOI:——
日期:——
PREPARATION OF R-5-(2-(2-ETHOXYPHENOXYETHYLAMINO)PROPYL)-2-METHOXYBENZENESULPHONAMIDE HYDROCHLORIDE OF HIGH CHEMICAL PURITY
申请人:LEK Pharmaceuticals d.d.
公开号:EP1708990A1
公开(公告)日:2006-10-11
Preparation of R-5- (2-(2-Ethoxyphenoxyetylamino) -2-Methoxybenzen-Sulphonamide Hydrochloride of High Chemical
申请人:Furlan Borut
公开号:US20080033207A1
公开(公告)日:2008-02-07
In the present invention, the process for the preparation of tamsulosin hydrochloride and subsequent purification with thermal crystallisation to provide essentially pure tamsulosin hydrochloride is disclosed.