CAS: 399-52-0; 5-Fluoro-1H-Indole

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CAS号399-76-8 5-氟吲哚-2-甲酸 | CAS号408355-23-7 7-溴-5-氟-1H-吲哚 | CAS号32989-58-5 trans-5-fluoro-... | CAS号371-40-4 4-氟苯胺 | CAS号127-17-3 丙酮酸 | CAS号371-14-2 4-氟苯肼 | CAS号348-36-7 5-氟吲哚-2-甲酸乙酯 | CAS号1073-06-9 间溴氟苯 | CAS号700-36-7 2-溴-4-氟-1-硝基苯 | CAS号1093066-72-8 1-叔丁基二甲基硅基-5氟吲哚-4-硼酸 | CAS号101349-12-6 5-氟色醇 | CAS号321-69-7 5-氟靛红酸酐 | CAS号310886-79-4 5-氟-1H-吲哚-3-羧酸甲酯 | CAS号149669-43-2 5-氟-3-(4-哌啶)-吲哚 | CAS号443-73-2 5-氟吲哚-3-乙酸 | CAS号446-08-2 2-氨基-5-氟苯甲酸 | CAS号392-13-2 5-氟-3-甲基吲哚 | CAS号198474-05-4 PF-06840003 | CAS号205114-16-5 3-溴-6-氟喹啉

5-氟吲哚-2-酮置于bis(Trimethylsilyl)Amide Yttrium(Iii),频那醇硼烷体系中,用 甲苯 作为反应溶剂,化学反应 36.0H,以92%的收率获得产物5-氟吲哚
参考文献:钇配合物的同质双(三甲基甲硅烷基)酰胺催化酰胺的硼氢化还原.
标题:钇配合物的同质双(三甲基甲硅烷基)酰胺催化酰胺的硼氢化还原.
摘要:均一的镧系元素络合物y [n(tms)2] 3是一种高效的均相催化剂,可用于将硼化的仲酰胺和叔酰胺还原为相应的胺.发现一系列含有不同官能团如氰基,硝基和乙烯基的酰胺具有非常好的耐受性.该转化也已经很好地应用于吲哚和吡哌贝地的合成.详细的同位素标记实验,对照实验和动力学研究为阐明反应机理提供了累积的证据.
DOI:10.1021/acs.Orglett.9B04606

专利信息

专利号:US-11873305-B2
优先权日:2020-06-30
标题 :Processes for synthesis of substituted indole intermediates for the synthesis of serd compounds
发明人：ZHANG HAIMING; XU JIE; WUITSCHIK GEORG; ANGELAUD REMY; HEROLD SEBASTIAN; STUTZ ALFRED; BRUETSCH TOBIAS; BURKHARD JOHANNES
权利人:GENENTECH INC; HOFFMANN LA ROCHE
摘要:Provided herein are processes for the preparation of indolyl intermediates using Wenker Synthesis for the total synthesis of SERD compounds useful in the treatment of cancer.

专利号:US-12024731-B2
优先权日:2017-05-03
标 题 :Methods and enzyme catalysts for the synthesis of non-canonical amino acids
发明人：BOVILLE CHRISTINA E; BRINKMANN-CHEN SABINE; BULLER ANDREW R; ROMNEY DAVID K; PRIER CHRISTOPHER K; KOCH PHILIPP; SCHEELE REMKES A
权利人:CALIFORNIA INST OF TECHN
摘要:The present disclosure provides methods for preparing β-substituted tryptophan compounds. The methods include: combining i) an unsubstituted indole or a substituted indole, ii) a β-substituted serine, and iii) a tryptophan synthase β-subunit (i.e., a TrpB); and maintaining the resulting mixture under conditions sufficient to form the β-substituted tryptophan. The TrpB contains at least one amino acid mutation which promotes formation of an amino-acrylate intermediate. New TrpB variants and new β-substituted tryptophan analogs are also described.

专利号:US-10730906-B2
优先权日:2002-08-01
标题:Multi-step synthesis of templated molecules
发明人：PEDERSEN HENRIK
权利人:PEDERSEN HENRIK; NUEVOLUTIONS AS
摘要:Disclosed is a method for the manufacture of a library of complexes. The complexes comprise templated molecules attached to the template which directed the synthesis thereof. The templated molecules are produced in a step-by-step fashion which provides for a high local concentration of reactive groups involved in the formation of connections between the individual components of the template molecule.

专利号:US-2023220001-A1
优先权日:2020-06-09
标 题:Method for synthesis of thioether-containing peptides
发明人：GRUSS HENDRIK; LUTZ CHRISTIAN; SÃœSSMUTH RODERICH; Yao guiyang; KNITTEL CAROLINE; KOSOL SIMONE; MAINZ ANDI
权利人:HEIDELBERG PHARMA RES GMBH
摘要:The present invention relates to a method of formation of a sulphur bridge between tryptophan and cysteine in solid phase peptide synthesis under iodine treatment. The invention also relates to the resulting compounds of the method and their respective use.

专利号:US-7371769-B2
优先权日:2004-12-07
标 题 :Tetrahydropyridin-4-yl indoles with a combination of affinity for dopamine-D2 receptors and serotonin reuptake sites
发明人：HES ROELOF VAN; SMID PIETER; KRUSE CORNELIS G; TULP MARTINUS TH M
权利人:SOLVAY PHARM BV
摘要:The present invention relates to a group of novel tetrahydropyridin-4-yl indoles with a dual mode of action: serotonin reuptake inhibition and affinity for dopamine-D 2 receptors, to methods for the preparation of these compounds and to novel intermediates useful for the synthesis of said tetrahydropyridin-4-yl indoles. The invention also relates to the use of a compound disclosed herein for the manufacture of a medicament giving a beneficial effect. n The invention relates to novel tetrahydropyridin-4-yl indoles of the formula. n nand tautomers, stereoisomers, prodrugs, N-oxides, pharmacologically acceptable salts, hydrates and solvates thereof,n nwherein:n R 1 is hydrogen, halogen, alkyl(C 1-3 ) or alkoxy(C 1-3 ), CN or CF 3 , R 2 is hydrogen or alkyl(C 1-3 ), R 3 is hydrogen or alkyl(C 1-3 ), Z is hydrogen or alkyl(C 1-3 ), alkoxy(C 1-3 ) or alkylthio(C 1-3 ), A is hydrogen or alkyl(C 1-3 ), or A and Z together form a saturated or (partly) unsaturated 5- or 6-membered ring which may be substituted with halogen, alkyl (C 1-3 ) or phenyl, in which ring Z represents carbon, sulfur of nitrogen.

专利号:US-9365494-B2
优先权日:2008-12-18
标 题 :Process for synthesis of amino-methyl tetralin derivatives
发明人：DURKIN KIERAN; FISHER LAWRENCE EMERSON; MEILI ARTHUR; SCALONE MICHAELANGELO; SHI XIANQING; VITALE JUSTIN
权利人:DURKIN KIERAN; FISHER LAWRENCE EMERSON; MEILI ARTHUR; SCALONE MICHAELANGELO; SHI XIANQING; VITALE JUSTIN; ROCHE PALO ALTO LLC
摘要:Methods for producing a compound of formula k1 or k2 n nby reducing a dihydronapthalene amide compound of formula in n nwith hydrogen gas in the presence of a ruthenium catalyst of formula j1 or j2n nRu(Z) 2 (L)  j1;n nRu(E)(E′)(L)(D)  j2;n nwherein m, n, Ar, Y, R 1 E, E′, D, Z and L are as defined herein.