CAS: 387-43-9; 4-Fluoroindole

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4-氟吲哚-2-甲酸置于n-甲基吡咯烷酮,铜体系中,用58%的收率获得产物4-氟吲哚
参考文献:Synthesis And Structure Of Fluoroindole Nucleosides
标题:Synthesis And Structure Of Fluoroindole Nucleosides
摘要:化学修饰碱基常用于稳定核酸,研究核酸结构形成的驱动力以及调整 Dna 和 Rna 杂交条件.核苷类似物是研究氢键,碱基堆积和溶解这三种导致核酸稳定性的主要作用力的化学手段.为了更深入地了解这些相互作用对 Rna 稳定性的贡献,我们决定合成一些新型核酸类似物,用氟化吲哚取代核碱基.氟化吲哚可与氟化苯并咪唑进行比较,以确定氮在五元环系统中的作用.本文报告了氟吲哚核糖核苷的合成以及所有合成的氟吲哚核糖核苷的 X 射线晶体结构.这些化合物也可能成为多种具有生物活性的 Rna 类似物的构建基块.
DOI:10.1139/v07-020

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-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-9493461-B2
优先权日:2013-02-07
标 题 :Tetracyclic heterocycle compounds and methods of use thereof for the treatment of hepatitis C
发明人：DAI XING; LIU HONG; PALANI ANANDAN; HE SHUWEN; LAI ZHONG; NARGUND RAVI; MARCANTONIO KAREN; XIAO DONG; BROCKUNIER LINDA L; ZORN NICOLAS; DANG QUN; PENG XUANJIA; LI PENG
权利人:MERCK SHARP & DOHME
摘要:The present invention relates to compounds of formula I that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.

专利号:US-9242998-B2
优先权日:2013-02-07
标题 :Tetracyclic heterocycle compounds and methods of use thereof for the treatment of hepatitis C
发明人：HE SHUWEN; DAI XING; PALANI ANANDAN; NARGUND RAVI; LAI ZHONG; ZORN NICOLAS; XIAO DONG; DANG QUN; MCCOMAS CASEY C; LI PENG; PENG XUANJIA; SOLL RICHARD
权利人:HE SHUWEN; DAI XING; PALANI ANANDAN; NARGUND RAVI; LAI ZHONG; ZORN NICOLAS; XIAO DONG; DANG QUN; MCCOMAS CASEY C; LI PENG; PENG XUANJIA; SOLL RICHARD; MERCK SHARP & DOHME
摘要:The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.

专利号:US-9243002-B2
优先权日:2013-02-07
标题 :Tetracyclic heterocycle compounds and methods of use thereof for the treatment of hepatitis C
发明人：DAI XING; LIU HONG; PALANI ANANDAN; HE SHUWEN; BROCKUNIER LINDA L; NARGUND RAVI; MARCANTONIO KAREN; ZORN NICOLAS; XIAO DONG; PENG XUANJIA; LI PENG; GUO TAO
权利人:MERCK SHARP & DOHME
摘要:The present invention relates to compounds of formula I that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.