CAS: 6548-09-0; 2-Amino-3-(5-Bromo-1H-Indol-3-yl)Propanoic Acid

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CAS号10075-48-6 5-溴-3-甲基吲哚 | CAS号70070-22-3 5-溴-3-甲基-1H-吲哚-... | CAS号622-88-8 4-溴苯肼单盐酸盐 | CAS号151417-95-7 1-(benzenesulfo... | CAS号10075-50-0 5-溴吲哚 | CAS号151417-97-9 diethyl 2-aceta... | CAS号151417-96-8 1-benzenesulfon... | CAS号830-93-3 5-溴芦竹碱 | CAS号67308-26-3 N-叔丁氧羰基-5-溴-DL-色氨酸 | CAS号18813-71-3 6-溴-1-甲基-9h-吡啶并... | CAS号75816-20-5 B°C-L-5-溴色氨酸

合成工艺路线路线简述

    📜5-溴-3-甲基吲哚置于sodium Hydroxide,N-溴代丁二酰亚胺(Nbs),正丁基锂,过氧化氢苯甲酰,硫酸,Sodium Hydride体系中,用 四氯化碳 作为反应溶剂,化学反应 26.0H,反应生成 5-溴-Dl-色氨酸
    参考文献:A New Synthesis Of 5-Bromo-Dl-Tryptophan
    标题:A New Synthesis Of 5-Bromo-Dl-Tryptophan
    摘要:A New Synthesis Of 5-Bromotryptophan,A Potential Antisickling Agent,From 5-Bromo-3-Methylindole Is Described.
    DOI:10.1080/00397919308009861

    海关参考信息

    专利信息


    专利号:US-12351573-B2
    优先权日:2019-05-09
    标 题:Compounds for use in synthesis of peptidomimetics
    发明人:AL-ABED YOUSEF; CHENG KAI FAN
    权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH
    摘要:Synthesis of O-benzotriazole and O-imidazole synthons are described. Uses of synthons in synthesis of azapeptides and other peptidomimetics, azapeptides and other peptidomimetics synthesized from the synthons and uses of azapeptides and other peptidomimetics are also described.

    专利号:US-2023159450-A1
    优先权日:2020-05-08
    标 题 :Dimers for use in synthesis of peptidomimetics
    发明人:AL-ABED YOUSEF; ALTITI AHMAD
    权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH
    摘要:Dimers for use in synthesis of peptidomimetics are described. Uses of dimers as synthons in synthesis of azapeptides and other peptidomimetics, azapeptides and other peptidomimetics synthesized from the dimers and uses of azapeptides and other peptidomimetics are also described.

    专利号:US-2004101523-A1
    优先权日:1989-07-27
    标题:Renal-selective prodrugs for control of renal smpathetic nerve activity in the treatment of hypertension
    发明人:REITZ DAVID B; KOEPKE JOHN P; BLAINE EDWARD H; SCHUH JOSEPH R; MANNING ROBERT E; SMITS GLENN J
    权利人:SEARLE & CO
    摘要:Renal-selective prodrugs are described which are preferentially converted in the kidney to compounds capable of inhibiting synthesis of catecholamine-type neurotransmitters involved in renal sympathetic nerve activity. The prodrugs described herein are derived from inhibitor compounds capable of inhibiting one or more of the enzymes involved in catecholamine synthesis, such compounds being classifiable as tyrosine hydroxylase inhibitors, or as dopa-decarboxylase inhibitors, or as dopamine-β-hydroxylase inhibitors. These inhibitor compounds are linked to a chemical moiety, such as a glutamic acid derivative, by a cleavable bond which is recognized selectively by enzymes located predominantly in the kidney. The liberated inhibitor compound is then available in the kidney to inhibit one or more of the enzymes involved in catecholamine synthesis. Inhibition of renal catecholamine synthesis can suppress heightened renal nerve activity associated with sodium-retention related disorders such as hypertension. Conjugates of particular interest are glutamyl derivatives of dopamine-β-hydroxylase inhibitors, of which N-acetyl-γ-glutamyl fusaric acid hydrazide (shown below) is preferred.

    专利号:WO-9101724-A1
    优先权日:1989-07-27
    标题 :Renal-selective prodrugs for the treatment of hypertension
    发明人:REITZ DAVID B; KOEPKE JOHN P; BLAINE EDWARD H; SCHUH JOSEPH R; MANNING ROBERT E; SMITS GLENN J
    权利人:SEARLE & CO
    摘要:Renal-selective prodrugs are described which are preferentially converted in the kidney to compounds capable of inhibiting synthesis of catecholamine-type neurotransmitters involved in renal sympathetic nerve activity. The prodrugs described herein are derived from inhibitor compounds capable of inhibiting one or more of the enzymes involved in catecholamine synthesis, such compounds being classifiable as tyrosine hydroxylase inhibitors, or as depa-decarboxylase inhibitors, or as dopamine-β-hydroxylase inhibitors. These inhibitors compounds are linked to a chemical moiety, such as a glutamic acid derivative, by a cleavable bond which is recognized selectively by enzymes located predominantly in the kidney. The liberated inhibitor compound is then available in the kidney to inhibit one or more of the enzymes involved in catecholamine synthesis. Inhibition of renal catecholamine synthesis can suppress heightened renal nerve activity associated with sodium-retention related disorders such as hypertension. Conjugates of particular interest are glutamyl derivatives of dopamine-β-hydroxylase inhibitors, of which N-acetyl-Y-glutamyl fusaric acid is preferred.

    专利号:US-2020354404-A1
    优先权日:2019-05-09
    标 题 :Peptidomimetic agents, synthesis and uses thereof
    发明人:AL-ABED YOUSEF
    权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH
    摘要:Compounds for use in synthesis of peptidomimetic agents; synthesis of peptidomimetic agents; peptidomimetic diagnostic and therapeutic agents; and uses of the compounds and peptidomimetic agents in drug discovery, diagnosis, prevention and treatment of diseases are described.

    专利号:WO-2025128985-A1
    优先权日:2023-12-14
    标题 :Sulfoxide and sulfone derivatives of thiocarbazates as synthons for azapeptides synthesis and process of using same
    发明人:AL-ABED YOUSEF
    权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH
    摘要:Provided for herein are sulfoxide and sulfone derivatives of thiocarbazates that have the formula (I): wherein A, R, R 1 , R 2 , and n are defined herein. The compounds may be used as synthons in the synthesis of azaeptides and other aza- amino acid conjugates.

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    合成参考文献


    参考文献:10.1021/np800501m
    摘要:Zou H, Zheng X, Li SM. Substrate promiscuity of the cyclic dipeptide prenyltransferases from Aspergillus fumigatus ( section sign). J Nat Prod. 2009 Jan;72(1):44–52. doi: 10.1021/np800501m.
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