CAS: 131707-23-8; Ethyl 6-Bromo-4-[(Dimethylamino)Methyl]-5-Hydroxy-1-Methyl-2-(Phenylsulfanylmethyl)Indole-3-Carboxylate,Hydrochloride

上下游产品

ethyl 5-acetyloxy-2-methyl-1H-indole-3-carboxylate 1,2-dimethyl-5-acetoxy-1H-indole-3-carboxylic acid ethyl ester 4-nitro-phenol formaldehyd

5-乙酰氧基-2-甲基吲哚-3-羧酸乙酯置于氨基磺酸,溴,Potassium Carbonate,Sodium Hydroxide,过氧化苯甲酰体系中,用 甲醇,氯仿,水,N,N-二甲基甲酰胺 用作溶剂,化学反应 17.0H,反应生成盐酸阿比朵尔
参考文献:一种盐酸阿比朵尔一水合物的制备方法
标题:一种盐酸阿比朵尔一水合物的制备方法
摘要:本发明公开了一种盐酸阿比朵尔的制备方法,本发明创新性的采用原料廉价易得的对硝基苯酚为原料,经乙酰化,硝基还原,吲哚环反应,甲基化反应,溴代,苯硫酚化和脱保护,Mannich反应,成盐得到盐酸阿比朵尔;整个合成过程反应条件温和,原料来源方便,产品性状好,收率高,副产物少,反应选择性和纯度高,对环境友好,生产成本低,适合工业化生产;避免了现有技术中的选择性差,副产物多,收率较低,避免了使用贵重的催化剂以及环境污染大的试剂的弊端.

专利信息

专利号:US-2016185745-A1
优先权日:2013-08-07
标题:Analogs of vinaxanthone and xanthofulvin, methods of synthesis, and methods of treatments thereof
发明人：SIEGEL DIONICIO; CHIN MATTHEW; ELIASEN ANDERS; AXELROD ABRAM
权利人:UNIV TEXAS
摘要:The present invention relates generally to methods of synthesis of vinaxanthone and xanthofulvin, novel analogs, and methods of use thereof.

专利号:US-11649285-B2
优先权日:2016-08-03
标题 :Identification of VSIG3/VISTA as a novel immune checkpoint and use thereof for immunotherapy
发明人：KALABOKIS VASSILIOS; WANG JINGHUA; WU GUOPING; BAZAN JOSE FERNANDO; VALLEY CHRISTOPHER CARLIN
权利人:BIO TECHNE CORP
摘要:The ligand for VISTA is identified (VSIG3) as well as the use of this ligand and receptor interaction in the identification or synthesis of a VSIG3 agonist or antagonist compounds, preferably antibodies, polypeptides and fusion proteins which agonize or antagonize the effects of VSIG3 and/or VISTA and/or the VSIG3/VISTA interaction. These antagonists may be used to suppress VSIG3/VISTA's suppressive effects on T cell immunity, and more particularly used in the treatment of cancer, or infectious disease. These agonist compounds may be used to potentiate or enhance VSIG3/VISTA's suppressive effects on T cell immunity and thereby suppress T cell immunity, such as in the treatment of autoimmunity, allergy or inflammatory conditions. Screening assays for identifying these agonists and antagonist compounds are also provided.

专利号:WO-2024061972-A1
优先权日:2022-09-20
标 题:Methods and platform for chemical synthesis
发明人：CRONIN LEE; MANZANO SEBASTIÃ?N; ZALESSKIY SERGEY; KITSON PHILIP; WANG HSIN
权利人:UNIV GLASGOW COURT
摘要:The invention relates to a method and apparatus for performing and characterising a chemical synthesis, such as those performed with an automated chemical synthesis platform, including such that are portable platforms, the method comprising the steps of: performing a chemical synthesis in a chemical synthesiser; recording analytical data during the chemical synthesis, and developing a profile for the analytical data recorded over time; and comparing the profile for the chemical synthesis against a reference profile, which reference profile is the analytical data recorded over time for a reference chemical synthesis, wherein the chemical synthesis and the reference chemical synthesis share at least the same reagents and method steps for the same intended product, such as the chemical synthesis and the reference chemical synthesis sharing the same instruction set. The method and apparatus are for intended for use in replication of approved, chemical syntheses based on common reaction platforms.

专利号:US-10065924-B2
优先权日:2014-07-22
标 题 :Preparation and biological evaluation of viridicatumtoxin analogs
发明人：NICOLAOU KYRIACOS C; HALE CHRISTOPHER R H; NILEWSKI CHRISTIAN; IOANNIDOU HERAKLIDIA; EL MARROUNI ABDELLATIF
权利人:UNIV RICE WILLIAM M
摘要:In one aspect, the present invention provides novel derivatives of viridicatumtoxin of the formula wherein the variables are as defined herein. The application also provides compositions, methods of treatment, and methods of synthesis thereof.

专利号:US-10562936-B2
优先权日:2015-09-18
标题 :Ligands for integrin αvβ6, synthesis and uses thereof
发明人：KAPP TOBIAS; KESSLER HORST; MALTSEV OLEG
权利人:UNIV MUENCHEN TECH
摘要:Disclosed are compound exhibiting highly active and selective binding to αvβ6 integrin, which are represented by the following general formula (I): Cyclo-(Arg-X1-Asp-X2-X3-X4-X5-X6-X7) (I) wherein the variables groups X to X have the following meanings X1: Ser, Gly, Thr, X2: Leu, lie, Nle, Val, Phe, X3: Gly, Ala, X4: Leu, He, Nle, Val, Phe, Lys, Tyr, Trp, Arg, X5: D-Pro, N-Me-D-lipophilic amino acids, X6: Pro, N-Me-amino acids, N-Me-Lys, N-Me-Lys(Ac), and X7; Ala, Leu, He, Nle, Val, Phe, Tyr, Trp or wherein the sub-sequence -X5-X6- represents a β-turn mimetic differing from the meanings above, or pharmaceutically acceptable salts, esters, solvates, polymorphs or modified forms thereof represented by the following general formula (II): (X0)n1L(X8)n2 wherein Xo represents the compound of the general formula (I) as specified above (excluding one hydrogen atom to allow bonding to the linker), L represents a linker, X8 represents the effector moiety and wherein n1 and n2 are each independently selected from the range of 1 to 5, wherein n1+n2 represents the number of valencies of the linker and is preferably in the range of from 2 to 6, more preferably 3-5, with the proviso that each of n1 and n2 is at least 1, as well as uses therefore in therapy and imaging.

专利号:US-11332498-B2
优先权日:2017-03-17
标 题:Ligands for integrin αVβ8, synthesis and uses thereof
发明人：KESSLER HORST; KAPP TOBIAS; REICHART FLORIAN; MALTSEV OLEG
权利人:UNIV MUENCHEN TECH
摘要:Disclosed are compounds represented by the following general formula (I): Cyclo-(Arg-Gly-Asp-X1-X2-X3-X4-X5) (I) wherein the variables groups X1 to X5 have the following meanings X1: Leu, Ile, Nle, Val, Tyr, Phe; X2: D-amino acid such as D-Pro, N-Me-D-Phe; X3: Pro, N-Me-amino acid such as N-Me-Lys, N-Me-Lys(Ac); Pro-Rx3, N-Me-Lys-Rx4; X4: Gly, Ala, Ser, Thr; X5: Leu, Ala, Tyr, His, Ile, Nle, Val, Phe wherein Pro-Rx3 represents a proline residue that carries at the C-3, C-4 or C-5 carbon atom and preferably the C-4 carbon atom a functional group selected from —NH2, —OH, —NH—Ac, —NH-hexyne, and wherein Lys-Rx4 represents a lysine residue, wherein the ω-amino nitrogen atom carries a group of the formula -L4-R4, wherein L4 is selected from the group consisting of covalent bond, —C(O)—, and —C(O)—O—, . . . , and wherein R4 is selected from the group consisting of —(CH2)n-C≡CH with n=0, 1, 2, 3, 4, 5, 6, 7 or 8, or wherein the sub-sequence -X2-X3- represents a β-turn mimetic diffeωωring from the meanings above, or pharmaceutically acceptable salts, esters, solvates, polymorphs or modified forms thereof represented by the following general formula (II): (X0)n1L(X8)n2 wherein X0 represents the compound of the general formula (I) as specified above (excluding one hydrogen atom to allow bonding to the linker), L represents a linker, X8 represents the effector moiety and wherein n1 and n2 are each independently selected from the range of 1 to 5, preferably such that each of n1 and n2 represents 1, wherein n1+n2 represents the number of valencies of the linker and is preferably in the range of from 2 to 6, more preferably 2-5, with the proviso that each of n1 and n2 is at least 1, as well as uses therefore in therapy and imaging.