专利号:WO-2012101648-A1 优先权日:2011-01-24 标题:Novel process for the synthesis of enantiomerically pure 2-methoxy-5-[(2r)-2-(4-alkylpiperazin-l-yl)propyl]-benzenesulfonamide 发明人:HAVALDAR FREDDY H; DABHOLKAR BHUSHAN VASANT; MULE GANESH BABAN 权利人:HAVALDAR FREDDY H 摘要:Where R is C1-C3 alkyl, alkenyl A novel process for synthesis of compound of Formula 1 comprising steroselective catalytic reduction of compound of Formula IV under hydrogen gas pressure to obtain an intermediate compound of Formula II, which on coupling in presence of coupling agent and base in presence of organic solvent to obtain compound of Formula X, Formula X on reacting with deprotecting agent in presence of organic solvent results in formation of compound of Formula XI, condensation of Formula XI with alkyl halide results in formation of compound of Formula I.
专利号:US-7619116-B2 优先权日:2003-12-17 标 题:Intermediates for the synthesis of (R)-tamsulosin and of its pharmaceutically acceptable salts and process for their preparation 发明人:DAMBRIN VALERY; LENOIR JEAN-YVES; SCHNEIDER JEAN-MARIE; GUILLAMOT GERARD; FOLLET MICHEL; BECKER ABRAM 权利人:PRODUCTS CHIMIQUES AUXILIAIRES 摘要:A subject matter of the present invention is novel intermediates for the synthesis of (R)-tamsulosin and of its pharmaceutically acceptable salts, and also the associated preparation process.
专利号:US-7538246-B2 优先权日:2003-12-29 标 题:Synthesis of optically pure(r)-5-(2-amynopropyl)-2-methoxybenzenesulphonamide 发明人:MOHAR BARBARA 权利人:LEK PHARMACEUTICALS 摘要:The present invention relates to a new process for the preparation of optically pure(R)-5-(2-aminopropyl)-2-methoxybenzenesulphonamide, which is an intermediate in the synthesis of tamsulosin.
专利号:US-7282606-B2 优先权日:2005-07-13 标题:Process for preparation of tamsulosin and its aralkylamine derivatives 发明人:JIH RU HWU; TSAY SHWU CHEN; MAGENDRAN BALAACHARY; CHAKRABORTY SUBHASISH K; DAS ASISH R; SHEU KUEN WANG; SHU CHUN MEI; LU CHIN KUN; CHANG WEI MIN 权利人:TAIWAN BIOTECH CO LTD 摘要: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. n n n n n n n n n n 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.
专利号:EP-1734036-B1 优先权日:2005-06-14 标 题:Process for preparation of tamsulosin and its derivatives 发明人:JIH RU HWU; MAGENDRAN BALAACHARY; CHAKRABORTY SUBHASISH K; DAS ASISH R; TSAY SHWU CHEN; SHEU KUEN WANG; SHU CHUN MEI; LU CHIN KUN; CHANG WEI MIN 权利人:WELL BEING BIOCHEMICAL CORP; TAIWAN BIOTECH CO LTD 摘要:The present invention discloses a new process for the synthesis of tamsulosin derivatives of formula 1 (where R 1 and R 2 represent C 1 -C 4 alkyl groups) and their hydrochlorides and other pharmaceutically acceptable salts, comprising reacting the hydrochloride of sulphonamide 2 (where R represents C 1 -C 4 alkyl) with the ether compound 21 (where R' represents C 1 -C 4 alkyl and R' represents MeC 6 H 4 SO 2 or MeSO 2 ).
专利号:US-2006148046-A1 优先权日:2004-12-31 标题 :Enzymatic process for the preparation of an intermediate compound and use thereof for the synthesis of tamsulosin hydrochloride
参考标题:Process For Preparation Of Tamsulosin And Its Aralkylamine Derivatives 摘要: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.