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TRI-(ADAMANTYL)PHOSPHINES AND APPLICATIONS THEREOF

In one aspect, phosphine compounds comprising three adamantyl moieties (PAd3) and associated synthetic routes are described herein. Each adamantyl moiety may be the same or different. For example, each adamantyl moiety (Ad) attached to the phosphorus atom can be independently selected from the group consisting of adamantane, diamantane, triamantane and derivatives thereof. Transition metal complexes comprising PAd3 ligands are also provided for catalytic synthesis including catalytic cross-coupling reactions.

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Synthesis of Some Potential Antihypertensive Phthalazinyl- and Quinoxalinylguanidines

A series of phthalazinyl- and quinoxalinylguanidines has been synthesized and evaluated for potential antihypertensive activity.Unsubstituted guanidines were prepared by treating the appropriate intermediate chloro compounds with guanidine free base.Substituted guanidines were prepared by treating the cyanamides 9 and 16 with the appropriate amine; with hydrazines, cyanamide 9 gave the triazoles 14 and 15.Moderate falls in blood pressure were observed with compounds 10, 11, 14, and 15.The triazole 15 caused a 25percent fall in heart rate.Some of the compounds (10, 11, 13, and 18) displayed weak alpha-adrenoceptor antagonist properties in vitro, and this activity was confirmed in the pithed rat (in vivo).

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DNA topoisomerase II inhibition has the activity of modulating kui analogue and its preparation method and application (by machine translation)

The invention discloses a DNA topoisomerase II inhibition activity of modulating kui analogs, its optical isomers, non-enantiomer or a racemic mixture, or its pharmaceutically acceptable salt, solvate, or a prodrug thereof, intermediate or metabolites thereof, the structure of the general formula (I) as shown: Wherein R1 , R2 , R3 , R4 , R5 And Ar in every one of the as defined in this invention. The invention also discloses a process for their preparation, their use as medicament and their application in treating tumors. The compounds of this invention curative effect is precise, small toxic side effect, enriched with the topoisomerase II technology is used for the expression of the drug for the treatment of diseases caused by abnormal inhibitors of types, it is expected to become therapeutic index higher can be used for clinical medicine. (by machine translation)

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Positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4). Part II: Challenges in hit-to-lead

This Letter describes the synthesis and SAR of two mGluR4 positive allosteric modulator leads, 6 and 7. VU001171 (6) represents the most potent (EC50 = 650 nM), efficacious (141% Glu Max) and largest fold shift (36-fold) of any mGluR4 PAM reported to date. However, this work highlights the challenges in hit-to-lead for mGluR4 PAMs, with multiple confirmed HTS hits displaying little or no tractable SAR.

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Regioselective Synthesis of 3-Aminoimidazo[1,2- a ]pyrimidines with Triflic Anhydride

The regioselective synthesis of 3-aminoimidazo[1,2- a ]pyrimidines via triflic anhydride mediated amide activation and intramolecular cyclisation is reported. The nature of the added pyridine base allows access to both regioisomers from a simple common precursor. The method tolerates a range of functional groups and provides access to novel heterocyclic scaffolds.

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About 3d-Metal-Complexes of 2-Hydrazinoquinoxalines

Some complexes of 3d-metals and 2-hydrazinoquinoxalines were synthesized and characterized spectrometrically.These compounds probably exist in solution as tetragonal distorted octahedrons.The organic ligands are to be found at the quadratic base, and anions or solvent-molecules, respectively, at the tops of the octahedron.The existence of chelates can be concluded from i.r. spectra.Together with u.v./vis-spectra back donation can be assumed.An assignment of the u.v./vis-bands is suggested and the ligand-field parameters Dq are estimated.

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Studies on the synthesis of 2-phenylsulphonyl-3-styrylquinoxalines

o-Phenylenediamine 1 is condensed with pyruvic acid or sodium pyruvate to yield 3-methylbenzo-1H-dihydropyrazine-2-one 2. The latter on condensation with aromatic aldehydes give 3-styrylquinoxaline-1H-2-one 3. Reaction of 3 with POCl3 in the presence of catalytic amount of DMF yields 2-chloro-3-styrylquinoxaline 4, which on reaction with thiophenol in the presence of triethylamine in methanol gives 2-phenylthio-3-styrylquinoxaline 5. Oxidation of 5 with H2O2 in the presence of acetic anhydride affords 2-phenylsulphonyl-3-styrylquinoxaline 6. 6 has also been prepared directly from 4 by reaction with sodium benzenesulphinate under phase transfer conditions. In an alternate approach to the synthesis of title compound. 2 is treated with POCl3 in DMF to obtain the known 2-chloro-3-methylquinoxaline 7. Reaction of 7 with thiophenol in the presence of triethylamine in methanol gives 2-methyl-3-phenylthioquinoxaline 8. Oxidation of 8 with H2O2 in Ac2O affords 2-methyl-3-phenylsulphonylquinoxaline 9. 9 was also prepared in an alternate method from 7 by reaction with sodium benzenesulphinate, 9 on reaction with aromatic aldehydes yields the title compounds 6.

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Triselenium dicyanide (TSD) as a new cyanation reagent: Synthesis of cyano pterins and quinoxalines along with library of cyano N-heterocyclic compounds

Triselenium dicynide (TSD) has been reported for the first time to be a novel cyanation reagent for the microwave-assisted one-pot synthesis of a series of various types of cyano N-heterocycles such as pterin, deazapterin, quinoxaline, naphthyridine, and pyridine in good yields. Copyright Taylor & Francis Group, LLC.

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Synthesis and antimicrobial activity of some new thioether derivatives of quinoxaline

2-Chloro-3-methylquinoxaline was selected as nucleus around which the molecular manipulations were carried out to get new compounds expected to possess better anti microbial activity. Various quinoxaline derivatives have been synthesized by replacing the chlorine at C-2 with a thioether linkage, which in turn attached to 2-(N-(substituted phenyl)acetamides. The synthesized compounds (5) were tested for their antimicrobial activity. Compounds 5b, 5c, 5d and 5i were found most active (comparable to the standard antibacterial Ciprofloxacin) amongst them. The structure of the compounds was confirmed on the basis of their spectral data.

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QUINOALINYL ESTERS OF CARBAMIMIDOTHIOIC ACIDS

The compounds of this invention are designated as quinoxalinyl esters of carbamimidothioic acids and exhibit the pharmacological properties of preventing gastric ulcers, reducing gastric secretions and lowering blood pressure. The compounds have the following structural formula: STR1 in which Q is hydrogen or nitro;

A is hydrogen, methyl, ethyl, propyl, isopropyl, n-butyl, carbomethoxy, carbethoxy, carbopropoxy, carbisopropoxy, carbobutoxy, carbisobutoxy, or carbo-t-butoxy; and< P>

R 1, R 2, and R 3 are, independently, hydrogen, methyl, ethyl, propyl, isopropyl, n-butyl, isobutyl, t-butyl, allyl, or R. sup.1 and R 3 may be concatenated with a carbon chain having 4 carbon atoms with R 2 then being hydrogen; except that, when A and Q are hydrogen, R 1, R 2, and R. sup.3 may not all be hydrogen; and with the further exception that, where A is methyl and R 1, R 2, and Q are all hydrogen, R 3 may not be ethyl;

or a pharmaceutically acceptable salt thereof.

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