邻乙氧基苯酚,2-氯乙醇置于sodium Hydroxide体系中,用 水 用作溶剂,化学反应 48.0H,以77%的收率获得2-(2-乙氧基-苯氧基)-乙醇 参考文献:Process For Preparation Of Tamsulosin And Its Aralkylamine Derivatives 标题:Process For Preparation Of Tamsulosin And Its Aralkylamine Derivatives 摘要: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230oc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.
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-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:US-2007106079-A1 优先权日:2003-12-17 标题:Novel intermediates for the synthesis of (r)-tamsulosin and of its pharmaceutically acceptable salts and process for their preparation
专利号:WO-2005058810-A1 优先权日:2003-12-17 标题:Novel intermediates for the synthesis of (r)-tamsulosin and of its pharmaceutically acceptable salts and process for their preparation
专利号:EP-1697316-B1 优先权日:2003-12-17 标题 :Novel intermediates for the synthesis of (r)-tamsulosin and of its pharmaceutically acceptable salts and process for their preparation
专利号:EP-1697316-A1 优先权日:2003-12-17 标 题 :Novel intermediates for the synthesis of (r)-tamsulosin and of its pharmaceutically acceptable salts and process for their preparation
参考文献:10.1007/s00253-024-13314-z 摘要:Cinca-Fernando P, Ascaso-Alegre C, Sevilla E, Martínez-Júlvez M, Mangas-Sánchez J, Ferreira P. Discovery, characterization, and synthetic potential of two novel bacterial aryl-alcohol oxidases. Appl Microbiol Biotechnol. 2024 Oct 29;108(1):498.