CAS: 19764-32-0; (R)-2-Acetamido-3-(4-Hydroxyphenyl)Propanoic Acid

该化合物是氨基酸乙酰乙酰胺的衍生物,其特点是氨基氨基氮原子中添加了乙酰基体,与母体化合物相比,这一改变增强了其在水中的溶解性和稳定性,是白到白的晶状粉,通常在水和甲醇等极地溶剂中溶解.N-乙酰D-硫磺经常用于生物化学研究和营养补充,因为它是...

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CAS号64896-33-9 2-乙酰基-3-(4-羟基苯基)-丙烯酸 | CAS号556-02-5 D-酪氨酸 | CAS号108-24-7 乙酸酐 | CAS号23525-90-8 l-N-acetyl tyro... | CAS号22862-76-6 茴香霉素

合成工艺路线路线简述

    📜(Z)-α-Acetamido-P-Hydroxycinnamic Acid置于rhodium(I)-(S,S)-Skewphos Complexes 氢气体系中,用 四氢呋喃 用作溶剂,化学反应生成N-乙酰-D-酪氨酸
    参考文献:Asymmetric Synthesis. Asymmetric Catalytic Hydrogenation Using Chiral Chelating Six-Membered Ring Diphosphines
    标题:Asymmetric Synthesis. Asymmetric Catalytic Hydrogenation Using Chiral Chelating Six-Membered Ring Diphosphines
    摘要:
    Doi:10.1021/ja00399A023

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    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:US-9783800-B2
    优先权日:2014-02-03
    标 题:Method for producing peptides having azole-derived skeleton
    发明人:SUGA HIROAKI; GOTO YUKI; KATO YASUHARU
    权利人:UNIV TOKYO
    摘要:Object of the present invention is to develop an artificial synthesis system of various peptides having an azole derivative structure and develop a library of such peptides. The present invention provides a method of producing a peptide having, in the backbone thereof, an azole derivative structure comprising the step of: synthesizing a substrate peptide of an azoline structure introducing enzyme having, in the modified region thereof, at least any one of the following amino acids, n n[in any of the compounds,n X 1 represents a group selected from the group consisting of SH, OH, NH 2 , SR 1 , OR 1 , NHR 1 , and N 3 (R 1 represents a protecting group), X 2 represents an easily eliminable group; and X 3 represents hydrogen or a substituted or unsubstituted alkyl or aryl group having from 1 to 10 carbon atoms]; reacting the substrate peptide with an azoline structure introducing enzyme to obtain a peptide having an azoline derivative structure; and converting the azoline derivative structure of the resulting peptide into an azole derivative structure by inducing an HX 2 elimination reaction of X 2 group.

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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:10.1021/jm00027a027
    摘要:Ye QZ, Johnson LL, Nordan I, Hupe D, Hupe L. A recombinant human stromelysin catalytic domain identifying tryptophan derivatives as human stromelysin inhibitors. J Med Chem. 1994 Jan 07;37(1):206–9. doi: 10.1021/jm00027a027.
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