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An expeditious neat procedure was developed for the synthesis of a series of new methyl phenyl heterocyclic phosphinates (3a-l) through Michaelis-Arbuzov reaction by the reaction of various heterocyclic halides (Cl or Br) (1a-l) with dimethyl phenylphosphonite (2) under N2 atmosphere using a heterogeneous catalyst, LaCl3.7H2O. The advantages of the developed procedure are good yields (80-89%) of the products, less reaction time (2-3 h), avoiding toxic catalysts and harmful solvents and easy work-up procedure. Further, antimicrobial activity of the synthesized compounds was evaluated at different concentrations 50, 100 and 150 mug/mL. Biological data revealed that compounds 3i, 3j and 3h, 3j exhibited potential antibacterial and antifungal activities, respectively, while the rest of the compounds showed moderate antimicrobial activity. [Figure not available: see fulltext.]

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Reference:
Isoquinoline – Wikipedia,
Isoquinoline | C9H3129N – PubChem

 

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To the synthetic method, 3 – aryl flavone or coumarin compound, is synthesized,efficiently, by one-step method, by means of a single electron transfer reaction between a flavones or coumarin compounds excited by light and aryl halides to initiate free radicals 3 – through a single electron transfer reaction to generate.aryl flavone derivatives, through a single electron transfer reaction between the light-excited flavones or coumarin compounds and the aryl halides by using, of the photo-reaction activity 3 – of the photo-excited flavones or coumarin compounds in a single electron transfer reaction to initiate radical, through one-step synthesis of the photo-active, compounds . The invention relates to a, method for, synthesizing, arylflavonoids or coumarin compounds through photo-excitation. (by machine translation)

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Reference:
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Disclosed herein is a visible light mediated cyclization of methyl (alpha-naphthyl) acrylates and heteroaromatic analogues yielding substituted acenaphthenes and azaacenaphthenes. This highly functional-group-tolerant transformation was put to the test in an enantioselective formal synthesis of delavatine A. Mechanistic details were elucidated by DFT-calculations revealing an unusual intramolecular H-transfer mediated by a primary amine. The generality of this transformation enables a novel synthetic strategy of five membered ring annulation at an advanced stage, allowing reliance upon naphthalene chemistry up to the point of acenaphthene construction.

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The present invention relates to a compound of Formula I or a pharmaceutically acceptable salt thereof, its preparation method, a pharmaceutical composition comprising the compound, and its use in manufacture of a medicament for treatment of a disease or disorder, wherein R1, R2, R5, R6, X, Y, Q, W, n1 and n2 are defined as those stated in the description.

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New pyridazin-3(2H)-one derivatives having the chemical structure of formula (I) are disclosed; as well as process for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of the phosphodiesterase IV (PDE4)

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Regio- and chemoselective transfer hydrogenation of isoquinolinium salts catalyzed by [Cp*RhCl2]2 using HCOOH-Et3N (5:2) as a hydrogen source was realized. A variety of N-methyl- and N-benzyl-1,2,3,4-tetrahydroisoquinoline alkaloids were obtained in high yields by the present catalyst system. Georg Thieme Verlag Stuttgart.

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Rhenium-catalyzed epoxidation of olefinic substrates is accelerated by the use of acclerants having a nitrogenous aromatic heterocyclic structure. Use of the accelerants also enables the use of aqueous hydrogen peroxide as an oxidant. To achieve optimum acceleration, the accelerant should have a concentration within a range from 2.0 mole percent to 100 mole percent of the acclerant with respect to 1 mole of the olefinic substrate. Use of the accelerant also results in an increased yield with respect to the conversion of the olefinic substrate to epoxide product.

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Isoquinoline – Wikipedia,
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Fused cyclic compounds, methods of using such compounds in the treatment of nuclear hormone receptor-associated conditions such as cancer and immune disorders, and pharmaceutical compositions containing such compounds.

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Thiete dioxide units have been employed as a template for further functionalization through C?H activation strategies. Using simple thiete dioxide building blocks, a new library of axially chiral molecules has been synthesized that owe their stability to electrostatic interactions in the solid state. Similar starting materials were further engaged in the formation of cyclic trimeric structures, opening the pathway to unprecedented macrocyclic ring systems.

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Reference:
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An expedient approach for the intermolecular C-H functionalization of pyrazines and other heteroarenes by the radical chemistry of xanthates is reported. Incorporation of a multitude of functional alkyl groups onto these heteroarenes proceeds in good yield and good to excellent regioselectivity, leading to highly functionalized heteroaromatics.

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Reference:
Isoquinoline – Wikipedia,
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