- Polyphenol compound containing tetrahydropapaverine-3-methyl carboxylate, preparation method and applications thereof
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The invention discloses a polyphenol compound containing tetrahydropapaverine-3-methyl carboxylate, a preparation method and applications thereof, wherein the polyphenol compound has a structure represented by a formula I, and R is hydrogen, halogen, C1-8 alkyl, C1-8 cycloalkyl, C1-8 halogenated alkyl, C1-8 alkoxy, C1-8 halogenated alkoxy, C2-4 alkenyl, phenyl, halogenated phenyl, nitrophenyl, C1-4 alkyl substituted phenyl, C1-4 halogenated alkyl substituted phenyl, naphthalene or acylamino. According to the invention, the polyphenol compound is novel in structure and generally has relativelygood inhibitory activity on influenza A virus H1N1, and the inhibitory effect of most compounds is superior to the inhibitory effect of a positive control Perimivir, so that the results show that thecompound has obvious inhibiting effect on influenza A virus, can be prepared into anti-influenza A virus medicine to be applied, has good application prospects in prevention and treatment of influenzavirus infection, and expands the application of tetrahydropapaverine structures as anti-influenza virus medicine.
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- Enantioselective Synthesis of Hydantoin and Diketopiperazine-Fused Tetrahydroisoquinolines via Pictet-Spengler Reaction
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An enantioselective synthesis of iso-, isothio-, and isoselenohydantoin and diketopiperazine-fused tetrahydroisoquinolines from l-Dopa was reported. The route consists of an Pictet-Spengler reaction of (S)-2-amino-3-(3,4-dimethoxyphenyl)propanoates with v
- Liu, Shih-I,Haung, Jia-Yun,Barve, Indrajeet J.,Huang, Sheng-Cih,Sun, Chung-Ming
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p. 336 - 344
(2019/03/19)
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- Pd/C-Catalyzed Dehydrogenative [3+2] Cycloaddition for the Synthesis of Functionalized Tropanes
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A Pd/C-catalyzed cascade approach for the synthesis of attractive benzo-fused tropanes was developed. The reaction proceeds through a sequential Pd/C-catalyzed dehydrogenative formation of azomethine ylides from amines and 1,3-dipolar cycloaddition. It allows the generation of structurally complex benzo-fused tropanes in good yields with excellent diastereoselectivities under mild reaction conditions. Preliminary results of asymmetric version of the reaction reveal that the copper catalyst and chiral monophosphoramidite ligand can furnish optically active products with moderate ee.
- Wang, Hai-Jun,Guo, Lei,Zhu, Cheng-Feng,Luo, Yun-Fei,Li, You-Gui,Wu, Xiang
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supporting information
p. 5456 - 5459
(2018/10/20)
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- The preparation method of the levodopa intermediate derivatives
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The invention relates to a preparation method for a levodopa intermediate derivative. The preparation method comprises: in a solvent, reacting 3, 4-dimethoxybenzene phenylalanine shown as formula I with (+)-tartaric acid derivative to obtain the salt of a [(-)-3, 4-dimethoxybenzene phenylalanine]2.(+)- tartaric acid derivative. The solvent includes an alcohol solvent and an ester solvent. The racemization method includes: in the solvent, under the action of an aldehyde or ketone catalyst, reacting the 3, 4-dimethoxybenzene phenylalanine shown as formula I at 0-90DEG C for 0.5-24 h. The preparation method for the levodopa intermediate derivative provided by the invention has simple steps, and the prepared enantiomer has high purity and is low in cost, thus being applicable to industrial production. (reaction formula).
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Paragraph 0070; 0071; 0072; 0073; 0074; 0075
(2017/10/13)
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- PROCESSES AND REAGENTS FOR MAKING DIARYLIODONIUM SALTS
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This disclosure relates to processes and reagents for making diaryliodonium salts, which are useful for the preparation of fluorinated, iodinated, astatinated and radiofluorinated aromatic compounds.
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Paragraph 0411
(2014/05/08)
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- Fixation and recycling of nitrogen monoxide through carbonitrosation reactions
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The removal of nitrogen monoxide from gas streams through complexation to iron(ii) ions in aqueous dimethylsulfoxide can be combined with a new variant of the Meerwein arylation, which incorporates the previously complexed NO into organic compounds to give oximes as final products. The first step of this two-step process has been evaluated regarding the effectiveness of the NO absorption and the sensitivity of the aqueous iron(ii)-DMSO solution towards oxygen from air, in both cases in comparison with the known BioDeNOx process. The subsequent Meerwein arylation, which was designed with the intention to make use of nitrogen monoxide as the simplest nitrogen-centered radical scavenger, is shown to tolerate an exceptionally broad spectrum of substituents on the aromatic core of the diazonium salts including electron-donating as well as electron-withdrawing substituents. Under simple conditions the resulting oximes can be converted to racemic amino acid esters. This journal is the Partner Organisations 2014.
- De Salas, Cristina,Heinrich, Markus R.
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supporting information
p. 2982 - 2987
(2014/06/10)
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- Anticancer activity of ruthenium(II) arene complexes bearing 1,2,3,4-tetrahydroisoquinoline amino alcohol ligands
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Ruthenium complexes offer potential reduced toxicity compared to current platinum anticancer drugs. 1,2,3,4-tetrahydrisoquinoline amino alcohol ligands were synthesised, characterised and coordinated to an organometallic Ru(II) centre. These complexes were evaluated for activity against the cancer cell lines MCF-7, A549 and MDA-MB-231 as well as for toxicity in the normal cell line MDBK. They were observed to be moderately active against only the MCF-7 cells with the best IC50 value of 34 μM for the cis-dia-stereomeric complex C4. They also displayed excellent selectivity by being relatively inactive against the normal MDBK cell line with SI values ranging from 2.3 to 7.4.
- Chelopo, Madichaba P.,Pawar, Sachin A.,Sokhela, Mxolisi K.,Govender, Thavendran,Kruger, Hendrik G.,Maguire, Glenn E. M.
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supporting information
p. 407 - 414
(2013/10/01)
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- Synthesis of aromatic α-aminoesters: Palladium-catalyzed long-range arylation of primary Csp3-H bonds
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Remote control: The title reaction for β-Iζ arylation of α-amino esters with aryl bromides is described. This reaction, which occurs selectively at the terminal position of linear alkyl chains, gives rise to synthetically useful (hetero)arylalanines and homologues after debenzylation (see scheme). Copyright
- Aspin, Sam,Goutierre, Anne-Sophie,Larini, Paolo,Jazzar, Rodolphe,Baudoin, Olivier
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p. 10808 - 10811
(2013/01/15)
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- Electronically rich N-substituted tetrahydroisoquinoline 3-carboxylic acid esters: Concise synthesis and conformational studies
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Recent work in our laboratory has shown that the highly substituted, electronically rich 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid (THIQ3CA) scaffold is a key building block for a novel class of promising anticoagulants.10 The synthesis
- Al-Horani, Rami A.,Desai, Umesh R.
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experimental part
p. 2027 - 2040
(2012/04/04)
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- Designing nonsaccharide, allosteric activators of antithrombin for accelerated inhibition of factor Xa
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Antithrombin is a key regulator of coagulation and prime target of heparins, clinically used anticoagulants. Heparins induce a two-step conformational activation of antithrombin, a process that has remained challenging to target with molecules devoid of t
- Al-Horani, Rami A.,Liang, Aiye,Desai, Umesh R.
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p. 6125 - 6138
(2011/10/30)
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- A general approach to aza-heterocycles by means of domino sequences driven by hydroformylation
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The development of hydroformylative domino reactions of easily accessible vinyl acetamides is described. Extremely regioselective hydroformylation of terminal double bounds provides a transient N-acyliminium that can be trapped by various nucleophiles to give several aza-heterocylic scaffolds in a diastereoselective manner.
- Airiau, Etienne,Spangenberg, Thomas,Girard, Nicolas,Schoenfelder, Angele,Salvadori, Jessica,Taddei, Maurizio,Mann, Andre
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experimental part
p. 10938 - 10948
(2009/11/30)
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- New synthetic amino acids for the design and synthesis of peptide-based metal ion sensors
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The syntheses of two new nonstandard amino acids, Flu (6) and XBp (20), and a new synthesis of Dmd (12) are reported. These residues exhibit fluorescence, metal-coordination, and fluorescence-quenching properties, respectively. These building blocks have been incorporated into peptides via solid phase peptide synthesis to afford the prototype for a photoinduced electron transfer-based metal ion chemosensor. The fluorescence of the peptides is modulated upon metal binding. This results from a metal ion-induced conformational change that brings the side chains of the Flu and Dmd amino acids into proximity, thereby favoring photoinduced electron transfer (PET) fluorescence quenching.
- Torrado, Alicia,Imperiali, Barbara
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p. 8940 - 8948
(2007/10/03)
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