3-硝基苯甲醚置于palladium 10% On Activated Carbon,Potassium Tert-Butylate,氢气,溶剂黄146体系中,用 N,N-二甲基甲酰胺 作为反应溶剂,化学反应 14.0H,反应生成 4-甲氧基吲哚 参考文献:Dissecting Metabolic Puzzles Through Isotope Feeding: A Novel Amino Acid In The Biosynthetic Pathway Of The Cruciferous Phytoalexins Rapalexin A And Isocyalexin A 标题:Dissecting Metabolic Puzzles Through Isotope Feeding: A Novel Amino Acid In The Biosynthetic Pathway Of The Cruciferous Phytoalexins Rapalexin A And Isocyalexin A 摘要:理解植物的防御途径对于开发抗病农作物至关重要,这是可持续农业的重要组成部分.因此,天然植物防御物质,如植物抗毒素(参与保护植物免受微生物病原体侵害),具有巨大的生物技术吸引力.十字花科植物是具有重要经济价值的植物,在全球范围内作为油料,高营养价值的蔬菜甚至保健品产生影响.值得注意的是,在独特的十字花科植物抗毒素(如芸薹素a和异硫氰酸酯a)的生物合成途径中所涉及的中间体仍未知.为此,我们利用大量氘代化合物确立了这些独特植物抗毒素的可能前体,并首次提出了它们的详细生物合成途径.该途径涉及多种中间体和一种作为这一复杂拼图核心的新型氨基酸.这项工作为发现具有独特骨架的十字花科植物对抗毒素生物合成途径的酶和基因奠定了基础. DOI:10.1039/c2Ob27076E
专利号:US-7598399-B2 优先权日:2005-11-30 标 题 :Methods for synthesis of 3-amino-1-arylpropyl indoles 发明人:CONNOLLY TERRENCE JOSEPH; FARRELL ROBERT P; HUMPHREYS ERIC ROY; LYNCH STEPHEN M; SARMA KESHAB 权利人:ROCHE PALO ALTO LLC 摘要:A method comprising:n hydrogenating an indole propionamide compound of formula h nn nwith vitride, to form an aminopropyl indole compound of formula in n nwherein m, Ar, R 1 and R 2 are as defined herein. The compounds prepared by the method of the invention are useful as monoamine reuptake inhibitors useful for treatment of CNS indications.
专利号:WO-9966934-A1 优先权日:1998-06-22 标 题 :CYCLIC AMINO ACID COMPOUNDS, PHARMACEUTICAL COMPOSITIONS COMPRISING SAME, AND METHODS FOR INHIBITING β-AMYLOID PEPTIDE RELEASE AND/OR ITS SYNTHESIS BY USE OF SUCH COMPOUNDS 发明人:AUDIA JAMES E; DRESSMAN BRUCE A; SHI QING 权利人:ELAN PHARM INC; LILLY CO ELI; AUDIA JAMES E; DRESSMAN BRUCE A; SHI QING 摘要:Disclosed are compounds which inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits β-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
专利号:US-6696438-B2 优先权日:1998-06-22 标题:Cyclic amino acid compounds, pharmaceutical compositions comprising same, and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds 发明人:AUDIA JAMES E; DRESSMAN BRUCE A; SHI QING 权利人:ELAN PHARM INC; LILLY CO ELI 摘要:Disclosed are compounds which inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits β-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
专利号:WO-2004083202-A1 优先权日:2003-03-19 标 题:A process for the preparation of indolymaleimides 发明人:RAMAKRISHNA VENKATA SATYA NIRO; KAMBHAMPATI RAMA SASTRI; SHIRSATH VIKAS SHREEKRISHNA; JASTI VENKATESHWARLU 权利人:SUVEN LIFE SCIENCES LTD; RAMAKRISHNA VENKATA SATYA NIRO; KAMBHAMPATI RAMA SASTRI; SHIRSATH VIKAS SHREEKRISHNA; JASTI VENKATESHWARLU 摘要:The present invention relates to an improved method of synthesis for indolylmaleimides, such as symmetrical and non-symmetrical bis-indolylmaleimides as well as indolylmaleimides. The process of the present invention has advantages such as shorter reaction time along with fewer amounts of impurity. The yield and purity of the product are good and thus the process has wider industrial applicability.
专利号:WO-2005113580-A1 优先权日:2004-05-21 标题 :Anticoronviral compounds and compositions, their pharmaceutical uses and materials for their synthesis 发明人:HOFFMAN ROBERT LOUIS; KANIA ROBERT STEVEN; NIEMAN JAMES ANDREW; PLANKEN SIMON PAUL; SMITH GEORGE JOSEPH III 权利人:PFIZER; HOFFMAN ROBERT LOUIS; KANIA ROBERT STEVEN; NIEMAN JAMES ANDREW; PLANKEN SIMON PAUL; SMITH GEORGE JOSEPH III 摘要:The invention relates to methods of inhibiting SARS-related coronavirus viral replication activity comprising contacting a SARS-related coronavirus protease with a therapeutically effective amount of a SARS 3C like protease inhibitor of formula (I), and compositions comprising the same.
专利号:ES-2368416-T3 优先权日:2005-11-30 标题:PROCEDURE FOR THE SYNTHESIS OF 3-AMINO-1-ARILPROPIL-INDOLES.
[参考文献]: Jung Min Song, Et Al. Intranasal Delivery Of Liposomal Indole-3-Carbinol Improves Its Pulmonary Bioavailability. Int J Pharm. 2014 Dec 30;477(1-2):96-101. [参考文献]: Tien-Yuan Wu, Et Al. Pharmacokinetics And Pharmacodynamics Of 3,3'-Diindolylmethane (Dim) In Regulating Gene Expression Of Phase Ii Drug Metabolizing Enzymes. J Pharmacokinet Pharmacodyn. 2015 Aug;42(4):401-8.
合成参考文献
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