- A convenient synthesis of benz-1,2-oxazine derivatives
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An expedient synthesis of benz-1,2-oxazine derivatives involving nitrene insertion on a methoxy group is described.
- Ghosh, Sukhen Chandra,De, Asish
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- ARYL AND HETEROARYL-CARBOXAMIDE SUBSTITUTED HETEROARYL COMPOUNDS AS TYK2 INHIBITORS
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Novel carboxamide substituted compounds of Formula (I) are disclosed; as well as processes for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Tyrosine Kinase 2 (Tyk2).
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Page/Page column 129
(2021/10/15)
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- A Bu4N[Fe(CO)3(NO)]-Catalyzed Hemetsberger–Knittel Indole Synthesis
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The nucleophilic Fe complex Bu4N[Fe(CO)3(NO)] (TBA[Fe]) catalyzes the direct intramolecular amination of aryl vinyl azides to give the corresponding indole derivatives in good to excellent yields.
- Baykal, Aslihan,Plietker, Bernd
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supporting information
(2020/02/20)
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- Substituted benzene and heterocyclic compound and its preparation method and application
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The invention provides substituted benzoheterocyclic compounds and a preparation method thereof. The compounds have structures shown by formulas I and II. The invention also provides the effects of the compounds shown by formulas I and II in resisting virus, tumor and the like. The invention further provides a medicine composition taking the compounds shown by the formulas I and II as active ingredients, and the anti-virus or anti-tumor effect of the medicine composition. The invention lays a foundation for the future in-depth study and development of the anti-virus or anti-tumor medicine of the compounds.
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Paragraph 0225; 0226; 0227; 0234; 0235; 0236
(2016/10/20)
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- Gold(I)-catalyzed rearrangement of alkynylaziridine indoles for the synthesis of spiro-tetrahydro-β-carbolines
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Functionalized spiro-tetrahydro-β-carbolines were formed by an efficient gold(I)-catalyzed rearrangement reaction of alkynylaziridine indoles. The reaction involved a Friedel-Crafts type intramolecular reaction of alkynylaziridine indoles, following by hydroamination of aminoallene intermediate.
- Yang, Yan-Fang,Li, Lian-Hua,He, Yu-Tao,Luo, Jian-Yi,Liang, Yong-Min
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supporting information
p. 702 - 707
(2014/02/14)
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- Design, synthesis and antiproliferative activity of a novel class of indole-2-carboxylate derivatives
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Based on the chemical structure of Pyrroloquinoline quinone (PQQ), a novel class of indole-2-carboxylate derivatives was designed, synthesized and assayed for antiproliferative activity in cancer cells in vitro. The biological results showed that some der
- Ji, Xing-Yue,Xue, Si-Tu,Zhan, Yue-Chen,Shen, Jia-Jia,Wu, Lin-Tao,Jin, Jie,Wang, Zhen,Li, Zhuo-Rong
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p. 409 - 418
(2014/07/21)
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- Synthesis of chromeno[3,4-b]indoles as Lamellarin D analogues: A novel DYRK1A inhibitor class
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A library of substituted chromeno[3,4-b]indoles was developed as Lamellarin isosters. Synthesis was achieved from indoles after a four-step pathway sequence involving C-3 iodination, a Suzuki cross-coupling reaction, and a one pot deprotection/lactonisation step. Twenty final compounds were tested in order to determine their activity against topoisomerase I and kinases, the two major biological activities of Lamellarins. One newly synthesized derivative exhibited a strong topoisomerase activity comparable to reference compounds such as campthotecin and Lamellarin with only a weak kinase inhibition. Two other lead compounds were identified as new nanomolar DYRK1A inhibitors and several other drugs affected the kinases in the sub-micromolar range. These results will enable us to use the chromeno[3,4-b]indole as a pharmacophore to develop potent treatments for neurological or oncological disorders in which DYRK1A is fully involved.
- Neagoie, Cleopatra,Vedrenne, Emeline,Buron, Frédéric,Mérour, Jean-Yves,Rosca, Sorin,Bourg, Stéphane,Lozach, Olivier,Meijer, Laurent,Baldeyrou, Brigitte,Lansiaux, Amelie,Routier, Sylvain
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experimental part
p. 379 - 396
(2012/04/10)
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- Iron(II) triflate as a catalyst for the synthesis of indoles by intramolecular C-H amination
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A practical iron-catalyzed intramolecular C-H amination reaction and its application in the synthesis of indole derivatives are presented. As a catalyst, commercially available iron(II) triflate is used.
- Bonnamour, Julien,Bolm, Carsten
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p. 2012 - 2014
(2011/06/28)
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- Intramolecular C-H amination reactions: Exploitation of the Rh 2(II)-catalyzed decomposition of azidoacrylates
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Rhodium(II) perfluorobutyrate-mediated decomposition of vinyl azides provides a new, mild entry into Rh2(II) nitrenoid chemistry. This methodology allows rapid access to a variety of complex, functionalized N-heterocycles in two steps from commercially available starting materials. Copyright
- Stokes, Benjamin J.,Dong, Huijun,Leslie, Brooke E.,Pumphrey, Ashley L.,Driver, Tom G.
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p. 7500 - 7501
(2008/02/09)
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- Solvent-free Heck-Jeffery reactions under ball-milling conditions applied to the synthesis of unnatural amino acids precursors and indoles
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The syntheses of various amino- and hydroxy-substituted dehydrophenylalanine derivatives using the Heck-Jeffery protocol under non-solvent conditions in a ball mill are presented. The influences of electron-withdrawing groups and of the location of the heteroatom substituent relative to the halide are discussed. Suitably substituted ortho-amino dehydrophenylalanine derivatives undergo a cyclization-elimination reaction to the corresponding 2-substituted indoles. Georg Thieme Verlag Stuttgart.
- Tullberg, Erik,Schacher, Felix,Peters, Dan,Frejd, Torbjoern
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p. 1183 - 1189
(2007/10/03)
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- INDOLE DERIVATIVES AND DRUGS CONTAINING THE SAME
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An indole derivative represented by the following general formula (1) : wherein at least one of R1, R2, R3, and R4 represents an alkoxy group containing 1 to 20 carbon atoms, and other groups of the R1, R2, R3, and R4 represent hydrogen, an alkyl group containing 1 to 6 carbon atoms, acetyl group, or hydroxyl group; and either one of X and Y represents -(CH2)nOH wherein n is an integer of 0 to 30, and the other one of the X and Y represents hydrogen atom; or a salt thereof; and a drug and an agent for promoting differentiation of a stem cell containing such indole derivative or its salt as an effective component. The indole derivative (1) of the present invention has action of inducing differentiation of neural stem cell specifically into a neuron, and this indole derivative is useful as a prophylactic or therapeutic drug for brain dysfunction or neuropathy caused by loss or degeneration of the neuron.
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Page/Page column 7
(2010/02/11)
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- Effects of indole fatty alcohols on the differentiation of neural stem cell derived neurospheres
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In a search for inducers of neuronal differentiation to treat neurodegenerative diseases such as Alzheimer's disease, a series of indole fatty alcohols (IFAs) were prepared, 13c (n = 18) was able to promote the differentiation of neural stem cell derived neurospheres into neurons at a concentration of 10 nM. Analysis of the expression of the Notch pathway genes in neurospheres treated during the differentiation phase with 13c (n = 18) revealed a significant decrease in the transcription of the Notch 4 receptor.
- Coowar, Djalil,Bouissac, Julien,Hanbali, Mazen,Paschaki, Marie,Mohier, Eliane,Luu, Bang
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p. 6270 - 6282
(2007/10/03)
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- Anti-aids piperazines
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The present invention includes diaromatic substituted heterocyclic compounds (III) STR1 which are useful in treating individuals infected with the HIV virus. The invention includes certain previously generically disclosed anti-AIDS piperazinyl compounds (V) and a method of treating HIV infected individuals with the indoles of formula (V) and the anti-AIDS amines (X).
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- Entry into 6-methoxy-D(+)-tryptophans. Stereospecific synthesis of 1-benzenesulfonyl-6-methoxy-D(+)-tryptophan ethyl ester
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A strategy for the synthesis of optically active ring-A methoxylated indole alkaloids which employs the Moody azide/Schollkopf chiral auxiliary protocol has resulted in the successful preparation of 1-benzenesulfonyl-6-methoxy-D(+)-tryptophan ethyl ester 16. This amino ester is required for the synthesis of Alstonia bisindole alkaloids including macralstonine 2 via an enantiospecific Pictet-Spengler reaction
- Allen,Hamaker,La Loggia,Cook
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p. 2077 - 2102
(2007/10/02)
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- Indoline Analogues of Idazoxan: Potent α2-Antagonists and α1-Agonists
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The synthesis and α-adrenergic activity of a series of substituted 2-imidazolinylindolines are described.Substitution in the indoline ring generated compounds with a spectrum of adrenoceptor antagonist/agonist profiles that proved sensitive to both the nature and position of the substituent.Many of the derivatives possess greater presynaptic antagonist potency that the corresponding benzodioxan 1, dihydrobenzofuran 2, and indan 3 analogues; however, this α2-antagonism is often accompanied by α1-agonist activity.It was not possible to separate α2-antagonist from α1-agonist properties in this series.Compounds of most interest proved to be the N-ethyl 6, 5-chloro-N-methyl 18 and 5-chloro-N-ethyl 23 derivatives, all being potent α2-antagonists and α1-agonists.Substitution at the 4- and 7-position of the indoline ring generally gave compounds with nonselective agonist properties.
- Fagan, Gay P.,Chapleo, Christopher B.,Lane, Anthony C.,Myers, Malcolm,Roach, Alan G.,et al
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p. 944 - 948
(2007/10/02)
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- The Alkaloids of Picrasma javanica
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Extraction of Picrasma javanica Bl. (Simarubaceae) has yielded two new β-carboline alkaloids, 1-ethenyl-4-methoxy-9H-pyrido-indol-5-ol (5-hydroxydehydrocrenatine) (4) and 1-ethyl-4-methoxy-9H-pyridoindol-5-ol (5-hydroxycrenatine) (5), the st
- Arbain, Dayar,Sargent, Melvyn V.
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p. 1527 - 1536
(2007/10/02)
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