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Erythromycin A one lactone antibiotic derivatives, preparation method and application thereof (by machine translation)

The present invention discloses a series of formula I shown containing substituted quinoline or isoquinoline erythromycin A one lactone antibiotic derivatives, their preparation and use, each compound side chain intermediates and synthetic method. The key point of the present invention is characterized in that: the formula I compounds are shown broad spectrum antibiotics has the effect and at the same time inhibiting gram positive and gram negative bacteria outstanding antibacterial activity and anti-drug-resistant bacteria. The invention provides a compound can be used as a broad spectrum antibiotic, has at the same time inhibiting gram positive and gram negative bacteria antibacterial, anti-virus activity. (by machine translation)

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An efficient synthesis of the potent dopamine D1 agonist dinapsoline by construction and selective reduction of 2?-azadimethoxybenzanthrone

8,9-Dihydroxy-2,3,7,11b-tetrahydro-1H-naphth[1,2,3-de]isoquinoline (dinapsoline, 1) is a potent dopamine D1 receptor agonist with potential antiparkinsonian activity. A new synthesis was developed with the fully aromatic compound 2 as the key intermediate. The synthesis herein described is suitable for a larger scale preparation of dinapsoline compared to the previously known methods. Furthermore, the unproductive protection/deprotection step of the nitrogen is circumvented by maintaining a high oxidation state of the isoquinoline moiety throughout the synthesis. The construction of the framework was accomplished by Friedel-Crafts acylation and a Suzuki cross-coupling reaction between the commercially available 4-bromoisoquinoline and aryl boronic acid 5, the latter demanding the transformation of the lithiation-directing amide back to a carboxylic acid functionality. The selective reduction was carried out stepwise with sodium borohydride and sodium cyanoborohydride. The new synthesis is high yielding and reduces the number of transformations in the previously reported methods.

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IMIDAZOLE DERIVATIVES AND THEIR USE AS MODULATORS OF CYCLIN DEPENDENT KINASES

The invention provides compounds of the formula (I): and salts, tautomers, solvates and N-oxides thereof; wherein Q is CH or N; X is N, N+-O- or CR3; Y is N, N+-O- or CR3a; R1 and R2 are independently selected from hydrogen and various substituents as defined in the claims; or R1 and R2 together with the atoms to which they are attached, link to form an optionally substituted carbocyclic or heterocyclic aromatic or non-aromatic ring of 4 to 7 members; R3 is selected from hydrogen and various substituents; and R3a is selected from hydrogen and various substituents as defined in the claims. Also provided are pharmaceutical compositions containing the compounds of formula (I), processes for making the compounds and the medical uses of the compounds. The compounds of formula (I) have activity as inhibitors of CDK kinases and are useful in the treatment of inter alia proliferative diseases such as cancers.

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One of the major reasons for studying chemical kinetics is to use measurements of the macroscopic properties of a system, Application In Synthesis of 4-Bromoisoquinoline, such as the rate of change in the concentration of reactants or products with time.In a article, mentioned the application of 1532-97-4, Name is 4-Bromoisoquinoline, molecular formula is C9H6BrN

Cesium carbonate-promoted synthesis of aryl methyl sulfides using: S -methylisothiourea sulfate under transition-metal-free conditions

In the presence of cesium carbonate, an efficient synthesis of aryl methyl sulfides by the reactions of aryl halides with commercially available S-methylisothiourea sulfate is developed. This odourless and highly crystalline solid can be used as the substitute for malodorous methanethiol. The gram-scale reaction also proceeds smoothly without the use of column chromatography separation. Similarly, 2-(dimethylamino)ethylthio and cyclopropylmethylthio groups can be easily introduced into the aromatic rings from the corresponding S-[2-(dimethylamino)ethyl]isothiourea dihydrochloride and S-cyclopropylmethylisothiourea hydrobromide. The possible reaction mechanism is proposed. It is believed that this route to aryl alkyl sulfides is well competitive with currently known methods due to its wide substrate scope, excellent yields, easy operation and transition-metal-free conditions.

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Reactions of 3-Benzoyl-3,4-dihydro-2-methyl-4-quinazolinecarbonitrile (2-Methylquinazoline Reissert Compound) with Acid, Base, Sodium Hydride, and Electrophiles

Acid hydrolysis of 3-benzoyl-3,4-dihydro-2-methyl-4-quinazolinecarbonitrile (11, 2-methylquinazoline Reissert compound) resulted in the formation of the oxazole (13).Alkaline hydrolysis gave 2-methylquinazoline (12) and banzoic acid (8).The anion (D1), generated from 11 and NaH in dimethylformamide (DMF), underwent decomposition to give the ketone (14) and the cyanoquinazoline (15) together with by-products 12 and O-benzoylbenzoin (9).Compound 11 reacted with aromatic aldehydes (10a-c) in the presence of NaH to give the benzoates (16a-c) and by-products 12 and 15.Alkylation (or arylation) with alkyl (or aryl) halides (11a, b) afforded the corresponding 4-substituted derivatives (19a, b) and a by-product 14.The reactivities of 11 and 3-benzoyl-3,4-dihydro-4-quinazolinecarbonitrile (21, quinazoline Reissert compound) are compared. Keywords—Reissert compound; quinazoline; hydrolysis; Reissert compound anion; rearrengement; aromatization; electronic effect; electrophilic substitution

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Related Products of 1532-97-4, Catalysts function by providing an alternate reaction mechanism that has a lower activation energy than would be found in the absence of the catalyst. In some cases, the catalyzed mechanism may include additional steps.In a article, 1532-97-4, molcular formula is C9H6BrN, introducing its new discovery.

Micellar catalysis of Suzuki-Miyaura cross-couplings with heteroaromatics in water

(Chemical Equation Presented) Pd-catalyzed couplings involving several heteroaromatic halides (bromides and chlorides) as well as boronic acids can be done under exceedingly mild conditions (between rt and 40 C) in pure water using commercially available Pd catalysts and PTS, a nanomicelle-forming amphiphile.

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Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

 

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Visible Light-Mediated Direct Decarboxylative C-H Functionalization of Heteroarenes

The direct visible light-mediated C-H alkylation of heteroarenes using aliphatic carboxylic acids is reported. This mild method proceeds at low catalyst loadings (0.5 mol %) and has a high functional group tolerance and a broad substrate scope. Notably, functionalization of (iso)quinoline, pyridine, phthalazine, benzothiazole, and other heterocyclic derivatives with both cyclic and acyclic primary, secondary, and tertiary carboxylic acids as well as amino and fatty acids proceeded under the standard conditions at room temperature. This protocol enables the rapid conversion of abundant feedstock materials into medically relevant “drug-like” moieties.

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Luminescent Pt(ii) complexes bearing dual isoquinolinyl pyrazolates: Fundamentals and applications

A series of four Pt(ii) metal complexes with trans-arranged isoquinolinyl azolates have been prepared, [Pt(Lx)2], x = 1-4, (1-4). The associated chelates possess various substituents; namely: one t-butyl (But) at the 6-position (L1), two But groups at the 5,7-positions (L2), one dip (2,6-di-isopropylphenyl) group at the 6-position (L3), and a single dip group at the 4-position of the 1-isoquinolinyl fragment (L4), respectively. Crystal structures of 1 and 4 were determined to shed light on the relationship of photophysics and packing arrangements. Their photophysical properties were measured and compared, for which the solid-state emission spectra of 2 and 4 are nearly identical to the solution spectra of all the Pt(ii) complexes, showing the formation of isolated molecular entities. In contrast, the Pt(ii) complexes 1 and 3 are found to be sensitive to their morphological states and external stimulus. This is confirmed by the gradual red-shifting of the emission with increasing concentration in the PMMA matrix, and the eventual formation of the broadened, metal-metal-to-ligand charge transfer (MMLCT) emission, by (i) wetting with acetone and drying in air, or (ii) grinding with a mortar and pestle, respectively. Organic light-emitting diodes (OLEDs) were also fabricated using multiple layered architecture and lowered doping concentration (e.g. 8 wt%), the latter is for avoiding dopant aggregation in the emitting layer. The associated OLED performances (i.e. etamax = 11.5%, 8.5%, and 11.2% for 1, 2 and 3) confirmed their suitability and potential as dopants for phosphorescent OLEDs.

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Palladium catalyzed direct 3-arylation of benzofurans using low catalyst loadings

The palladium-catalyzed direct 3-arylation of benzofurans provides a cost-effective and environmentally attractive route for the preparation of 3-arylbenzofuran derivatives. The reactions were carried out using a wide variety of electronically and sterically diverse aryl or heteroaryl bromides with low catalyst loadings. In the presence of only 0.1-0.5 mol% catalyst, products in moderate to good yields were obtained. The aryl bromide reactants were able to tolerate a wide range of functionalities, such as acetyl, propionyl, formyl, ester, nitrile, trifluoromethyl, or fluoro groups. Higher yields were obtained using electron-deficient aryl bromides as reactants compared to using electron-rich aryl bromides. Functionalized benzofuran derivatives, bearing formyl or hydroxymethyl on C2, were also successfully employed.

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Efficient coupling of heteroaryl halides with arylboronic acids in the presence of a palladium-tetraphosphine catalyst

Cis, cis, cis-1,2,3,4-tetrakis(diphenylphosphinomethyl) cyclopentane: ¡¤1/2[PdCl(C3H5)]2 system catalyses the Suzuki cross-coupling of heteroaryl halides with a range of arylboronic acids with very high ratio substrate/catalyst in good yields. Substrates such as pyridines, quinolines, thiophenes, an indole, pyrimidines or a furane have been used successfully.

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