CAS: 478-94-4; (+)-Lysergamide

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    (+)-Isolysergic Acid Amide 2889-26-1
    麦角酸 D-Lysergic Acid 82-58-6

    合成工艺路线路线简述

      📜麦角酸置于n-羟基-7-氮杂苯并三氮唑,N,N'-二叔丁基碳二亚胺,三氟乙酸体系中,用 N-甲基吡咯烷酮,N,N-二甲基甲酰胺 作为反应溶剂,化学反应 1.0H,反应生成 麦角酰胺
      参考文献:新型麦角肽作为腺苷和多巴胺受体的双重配体.
      标题:新型麦角肽作为腺苷和多巴胺受体的双重配体.
      摘要:多价配体是有前途的药理学工具,对多种疾病的治疗可能比高度选择性的单靶标药物更为有效.目前正在评估使用多巴胺能激动剂和腺苷能拮抗剂的联合疗法,以治疗帕金森氏病.[(a)kanda,T .; 等.经验值 神经元.2000,162,321-327.(b)詹纳,体育专家.投资.药物,2005,14,729-738.(c)kase,H .;等.neurology 2003,61(suppl 6),S97-S100.]在这里,我们通过基于麦角蛋白优先结构的组合方法制备了作用于腺苷和多巴胺受体的双重配体.这些新化合物的效力和功效通过放射性配体结合研究和表达腺苷和多巴胺受体的细胞内细胞内camp产生测定来确定.选定的化合物表现出双重多巴胺激动剂和腺苷拮抗剂活性.具有这种药理学特征的分子对于研究中枢神经系统中的多巴胺-腺苷串扰以及测试多价药物对帕金森氏病的治疗潜力具有潜在的实用性.
      DOI:10.1021/jm060947X

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      专利信息


      专利号:US-3929796-A
      优先权日:1974-08-02
      标 题:Synthesis of penniclavine and elymoclavine
      发明人:KORNFELD EDMUND C; BACH NICHOLAS J
      权利人:LILLY CO ELI
      摘要:Synthesis of penniclavine and of elymoclavine, intermediates useful therein, and novel compounds producible therefrom.

      专利号:US-5843682-A
      优先权日:1995-11-20
      标题 :N-1-carboxyalkyl derivatives of LSD
      发明人:SIGLER GERALD F; ROUHANI RIAZ; DAVOUDZAHEH DAVID
      权利人:BOEHRINGER MANNHEIM CORP
      摘要:Novel derivatives of LSD having the formula wherein R1 is an alkyl, cycloalkyl or aryl group having 1 to 10 carbon atoms, preferably an alkyl group having 1 carbon atom; R2 is a bond or wherein R3 is alkyl, cycloalkyl or aryl group having 2 to 10 carbon atoms, preferably an alkyl group having 2 or 5 carbon atoms; Z is an immunogenic carrier substance, an enzyme donor polypeptide or a label selected from the group consisting of an enzyme, a substance having fluorescent or luminescent properties and a radioactive substance; and n is 1 to p where p equals MW of Z/1000. The derivatives include maleimide conjugates of an immunogenic poly(amino acid), an enzyme donor polypeptide or a labeling substance such as an enzyme, a fluorescent substance or a radioactive substance. Novel activated hapten intermediates useful in the preparation of the conjugates and methods for synthesis of the hapten intermediates and their conjugate derivatives are also disclosed.

      专利号:US-3923812-A
      优先权日:1974-08-02
      标题:Synthesis of elymoclavine
      发明人:BACH NICHOLAS J; KORNFELD EDMUND C
      权利人:LILLY CO ELI
      摘要:Elymoclavine is prepared by oxidation of D-6-methyl-8hydroxymethyl-10 Alpha -methoxy-8-ergolene to the corresponding D-8-aldehyde followed by reduction with an active metal in acid medium.

      专利号:EP-0354945-B1
      优先权日:1988-01-13
      标 题 :Process for the enhancement of enzyme activities and synthetic efficiency in microorganisms and higher plants
      发明人:FIEDLER FRANZ; ZENK MEINHART H; GUNDLACH HEIDRUN; WEBER ALFRED; KENNECKE MARIO
      权利人:SCHERING AG
      摘要:In the process disclosed, the organisms are brought into contact witn inactivated elicitor-containing microorganisms, fragments of the latter, or excretions of elicitor-containing microorganisms. Only inactivated elicitor-containing bacteria, fragments of the latter, or excretions of elicitor-containing bacteria may be used to activate enzymes and promote synthesis in non-microbial organisms. The process can be used, for example, to promote synthesis in microorganisms or plants which produce pigments, antibiotics, alkaloids or phytoalexins or to activate enzymes in microorganisms capable of transforming steroids.

      专利号:US-2009011476-A1
      优先权日:2005-08-19
      标 题 :Gene cluster and method for the biosynthesis of terrequinone a
      发明人:HOFFMEISTER DIRK; KELLER NANCY P
      权利人:WISCONSIN ALUMNI RES FOUND
      摘要:The present invention provides a novel gene cluster containing five genes (tdiA-E) involved in indole alkaloid synthesis. Disruption of tdiB, encoding an enzyme with prenyltransferase activity, transferring dimethylallylpyrophosphate to C-2 of an indole structure, eliminated the production of the antitumor compound terrequinone A, a metabolite not known from A. nidulans . The invention further provides a method for expressing terrequinone A in a host cell and isolating purified terrequinone A therefrom.

      专利号:EP-3137618-A1
      优先权日:2014-04-29
      标 题 :Improved methods for making and using polynucleotide sequences in the synthesis of alkaloid compounds

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      合成参考文献


      摘要:Psychotropic Drugs and Related Compounds, 2nd ed., Usdin, E., and D.H. Efron, Washington, DC, 1972, -(97), 1972
      摘要:21 CFR Sections 1308.11-1308.15
      参考文献:doi.org/10.3390/pharmacy13040098
      摘要:doi:doi.org/10.3390/pharmacy13040098
      参考文献:10.1007/bf01902441
      摘要:de Mello WC, Chang YC. Neuromuscular transmission inElectrophorus electricus (L.). Cellular and Molecular Life Sciences. 1966 Oct;22(10):680–1. doi: 10.1007/bf01902441.
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