CAS: 112101-74-3; (R)-N-(1-(4-Methoxy-3-Sulfamoylphenyl)Propan-2-yl)Acetamide

该化合物是一种化学化合物,具有特定结构特征,包括磺酰胺组和乙酰胺酸盐.该化合物通常具有与全氟辛烷磺酸和氨化物相关的特性,例如极地溶剂中潜在的溶性以及由于功能组的存在而形成氢结联的能力.甲基氧基组助长其水利恐惧性,而磺酰胺组则可能加强其生物活动,使其对药用化学感兴趣.由(2R)配置显示的立体化学学学表明,该化合物可能具有可影响其药效效应的气质特性.

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116091-63-5 112101-81-2 119714-13-5

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CAS号86073-42-9 Acetamide, N-[(... | CAS号112101-81-2 R-(-)-5-(2-氨基丙基...

合成工艺路线路线简述

    📜(E)-N-(1-(4-Methoxyphenyl)Prop-1-En-2-yl)Acetamide置于氯磺酸,[rh(Nbd)((S,S,S,S)-Wingphos)]Bf4,氨,氢气体系中,用 二氯甲烷,水,乙腈 用作溶剂,50.0 °C,5.0 Mpa 条件下,反应 18.08H,反应生成N-[(1R)-2-(3-氨基磺酰基-4-甲氧基)-1-甲基]乙酰胺
    参考文献:N-乙酰(e)-β-丙烯酰胺的实用合成
    标题:N-乙酰(e)-β-丙烯酰胺的实用合成
    摘要:摘要 通过用铁还原相应的肟,开发了一种简便实用的制备(e)-β-芳基酰胺[(e)-N-(1-芳基丙-1-烯-2-基]乙酰胺]的方法(II)乙酸盐作为还原剂发现使用六甲基磷酰胺作用作溶剂对高e / Z选择性至关重要,该方法已用于通过不对称氢化有效合成坦索罗辛的关键手性中间体. 通过用铁还原相应的肟,开发了一种简便实用的制备(e)-β-芳基酰胺[(e)-N-(1-芳基丙-1-烯-2-基]乙酰胺]的方法(II)乙酸盐作为还原剂发现使用六甲基磷酰胺作用作溶剂对高e / Z选择性至关重要,该方法已用于通过不对称氢化有效合成坦索罗辛的关键手性中间体.
    Doi:10.1055/s-0033-1339976

    海关参考信息

    专利信息


    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 ).

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    主要参考文献

    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.

    合成参考文献


    参考文献:10.1055/s-0033-1339976
    摘要:Tang W, Cai Z, Liu G, Jiao G, Senanayake C. Practical Syntheses of N-Acetyl (E)-β-Arylenamides. Synthesis. 2013 Oct 14;45(24):3355–60. doi: 10.1055/s-0033-1339976.
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