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Microwave-assisted multi-component reaction in water leading to highly regioselective formation of benzo[f]azulen-1-ones

Microwave-assisted three-component reaction has been established for the regioselective synthesis of benzo[f]azulen-1-ones. The reaction was performed in aqueous media under microwave irradiation by using readily available and inexpensive starting materials. A total of 38 examples were examined to show a broad substrate scope and good overall yields (70-89%). The present new synthesis shows attractive green chemistry characteristics, such as the use of water as reaction media, concise one-pot conditions, short reaction periods (7-24 min), easy work-up/purification, and reduced waste production without the use of any strong acids or metal promoters.

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Tetrahydrofuran – Wikipedia,
Tetrahydrofuran | (CH2)3CH2O – PubChem

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Computer aided ligand based screening for identification of promising molecules against enzymes involved in peptidoglycan biosynthetic pathway from Acinetobacter baumannii

A. baumannii has been considered as Priority-I as suggested by the World Health Organization (WHO) and the most critical pathogenic microorganism for causing nosocomial infection in imunno-compromised hospital-acquired patients due to multi-drug resistance (MDR). In the current study, we utilized ?Computer-aided ligand-based virtual screening approach? for identification of promising molecules against Mur family proteins based on the known inhibitor (Naphthyl Tetronic Acids ((5Z)-3-(4-chlorophenyl)-4-hydroxy-5-(1-naphthylmethylene) furan-2(5H)-one)) of MurB from E. coli. The in-house library was prepared using a similarity search of a known inhibitor (Drug Bank ID: DB07296) against several relevant chemical databases. The molecules obtained from virtual screening of Naphthyl Tetronic Acids in-house library were successively subjected to physicochemical and ADMET screening. After this, the molecules which passed all the filters, subsequently subjected into interaction analysis with the drug target proteins (MurB, MurD, MurE and MurG) of A. baumanni and the results explained that four molecules were promising (CHEMBL468144, DB07296, Enamine_T5956969 and 54723243) for further molecular dynamics simulations. The free and ligand bounded proteins that undergone MD simulation are listed as follows: MurB, MurB-CHEMBL468144, MurB-DB07296, MurE, MurE-54723243, MurE-DB07296, MurD, MurD-Enamine_T5956969, MurD-DB07296, MurG, MurG-CHEMBL468144, and MurG-DB07296. Based on global and essential dynamics analysis, the stability order of molecules towards MurB (CHEMBL468144 > DB07296); MurD (Enamine_T5956969 > DB07296); MurE (54723243 > DB07296) and MurG (CHEMBL468144 > DB07296) indicates that the newly identified molecules are more promising one in comparison with the existing inhibitor. Based on all the docking and MD simulation results, the stability order of the free and ligand bounded protein are as follows; MurB and MurB-ligand complexes > MurD and MurD-ligand complexes > MurG and MurG-ligand complexes > MurE and MurE-ligand complexes. Finally, the selected compounds would be recommended for further experimental investigations and used as promising inhibitors of the infection caused by A. baumannii.

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Tetrahydrofuran – Wikipedia,
Tetrahydrofuran | (CH2)3CH2O – PubChem

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Electrochemical reduction of 3-phenyl azo-2,4(3H,5H) -furandione at the DME

The electroreduction of 3-phenyl azo-2,4(3H,5H)-furandione and five of its phenyl-substituted derivatives in aqueous ethanolic buffered solutions (pH ? 2-12) have been investigated at the DME. The acid dissociation constants were determined spectrophotometrically. A mechanism for the electroreduction pathway is proposed. On the basis of the data obtained the azomethine linkage is thought to be in the azo and not the hydrazone form.

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Tetrahydrofuran – Wikipedia,
Tetrahydrofuran | (CH2)3CH2O – PubChem

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Synthesis of (¡À)-camptothecin using a [3+2] nitrone cycloaddition to construct the CDE ring moiety

A novel synthesis to camptothecin is described. A Friedlander condensation of o-aminobenzaldehye with tricylclic ketone affords camptothecin after further elaboration. Tricyclic ketone is prepared via a route employing a [3+2] nitrone cycloaddition and an intramolecular Knoevenagel condensation. A novel synthesis to camptothecin is described. A Friedlander condensation of o-aminobenzaldehye 2 with tricylclic ketone 3 affords camptothecin after further elaboration. Tricyclic ketone 3 is prepared via a route employing a [3+2] nitrone cycloaddition and an intramolecular Knoevenagel condensation.

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Tetrahydrofuran – Wikipedia,
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106. Photochemical Synthesis of Cyclic 2-(2,2,-Dimethylpropylidene)-1,3-Dicarbonyl Compounds

Photolysis (lambda=254 nm) of 4-(t-Bu)-substituted -fused bi- and tricyclic pyrandiones 5 affords title compounds 4 in good yields as well a small amounts of spiroalkanediones 8.The alkyl-substitution pattern at C(4) of the pyran ring in 5 determines the relative amount of alpha- vs. beta-cleavage products obtained from the primarly formed acyl-vinyloxy biradical.

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METABOLICALLY ROBUST ANALOGS OF CYP-EICOSANOIDS FOR THE TREATMENT OF CARDIAC DISEASE

The present invention relates to compounds according to general formula (I) which are metabolically robust analogues of bioactive lipid mediators derived from omega-3 polyunsaturated fatty acids (n-3 PUFAs).The present invention further relates to compositions containing one or more of these compounds and to the use of these compounds or compositions for the treatment or prevention of cardiovascular diseases.

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Tetrahydrofuran – Wikipedia,
Tetrahydrofuran | (CH2)3CH2O – PubChem

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A novel and efficient one-pot synthesis of furo[3?,4?:5,6]pyrido[2,3-c]pyrazole derivatives using organocatalysts

A novel approach to one-pot synthesis of dihydrofuro[3?,4?:5,6]pyrido[2,3-c]pyrazole and indeno[2?,1?:5,6]pyrido[2,3-c]pyrazole derivatives have been investigated using organocatalysts that are recyclable. This new protocol has the advantages of environmental friendliness, higher yield, low cost, as well as convenient operation. The catalytic efficiency of various small organocatalysts such as l-proline, trans-4-hydroxy-l-proline, l-thiaproline, cinchonidine, (+)-cinchonine, and dl-2-phenylglycine has also been studied.

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Tetrahydrofuran – Wikipedia,
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An efficient one-pot three-component synthesis of tetrahydrofuro[3,4-b] quinoline-1,8(3H,4H)-dione derivatives catalyzed by L-proline

L-Proline is found to be an efficient catalyst for the synthesis of tetrahydrofuro[3,4-b]quinoline- 1,8(3H,4H)-dione derivatives. This protocol is novel and has the advantages of mild condition, high yield, and easy operation.

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Tetrahydrofuran – Wikipedia,
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The versatility of DABCO: synthetic applications of its basic, nucleophilic, and catalytic properties Part 1. Catalysis of Morita?Baylis?Hillman and Knoevenagel reactions

[Figure not available: see fulltext.] This review article covers literature data from the last 5 years regarding the various applications of 1,4-diazabicyclo[2.2.2]octane (DABCO) in organic chemistry. The frequent use of DABCO as a base, catalyst, and reagent has been reflected in the large number of publications, therefore our review will be published in 4 parts. The first part of the review is dedicated to the use of DABCO as catalyst for Morita?Baylis?Hillman and Knoevenagel reactions.

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Tetrahydrofuran – Wikipedia,
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Multicomponent reactions studies: Yonemitsu-type trimolecular condensations promoted by Ti(IV) derivatives

We have developed a Ti(IV)/Et3N-promoted trimolecular condensation of aromatic heterocycles (furan, pyrrole, imidazole, indole) with aldehydes and active methylene compounds. In the case of indole and methyl acetoacetate the reaction afforded three-component products or tricyclic cyclopenta[b]indole derivative, depending on the reaction conditions. In both cases, NMR analysis evidenced that titanium enolate is the reactive species involved in the reaction.

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Tetrahydrofuran – Wikipedia,
Tetrahydrofuran | (CH2)3CH2O – PubChem