Can You Really Do Chemisty Experiments About 4265-16-1

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CERTAIN ARYL-ALIPHATIC AND HETEROARYL-ALIPHATIC PIPERAZINYL PYRAZINES AND THEIR USE IN THE TREATMENT OF SEROTONIN-RELATED DISEASES

Compounds of the general formula (I):wherein the variables are as defined in the specification are useful for the prophylaxis or treatment of serotonin-related, especially 5-HT 2 receptor-related, diseases in human beings or animals, particularly diseases related to the 5-HT2 c receptor, especially diseases such as eating disorders, memory disorders, schizophrenia, mood disorders, anxiety disorders, pain, sexual dysfunctionions, and urinary disorders.

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Benzofuran – Wikipedia,
Benzofuran | C8H654O – PubChem

The important role of 4265-16-1

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Pyrazolopyrimidines as therapeutic agents

The present invention provides compounds of Formula I, 1including pharmaceutically acceptable salts and/or prodrugs thereof, where G, Ra, R2, and R3 are defined as described herein.

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Benzofuran – Wikipedia,
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Brief introduction of Benzo[b]furan-2-carboxaldehyde

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Phospholane-catalyzed wittig reaction

We identified 2-phenylisophosphindoline 2-oxide as a suitable and potentially tunable catalyst for the catalytic Wittig reaction of aldehydes with activated organohalides. This catalyst was obtained by a straightforward two-step synthesis. Trimethoxysilane proved to be an efficient reducing agent for the in situ generation and regeneration of the catalyst from the corresponding phosphane oxide. Sodium carbonate was identified as a suitable base for the transformation. It is noteworthy that the particle size of the sodium carbonate had a tremendous effect on the outcome of the reaction. Under the optimized reaction conditions, 23 aldehydes were converted into the corresponding alkenes in high isolated yields of up to 88%. Moreover, an asymmetric catalytic Wittig reaction was performed for the desymmetrization of a prochiral diketone.

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Benzofuran – Wikipedia,
Benzofuran | C8H1103O – PubChem

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A Catalytic Approach for Enantioselective Synthesis of Homoallylic Alcohols Bearing a Z-Alkenyl Chloride or Trifluoromethyl Group. A Concise and Protecting Group-Free Synthesis of Mycothiazole

A protecting group-free strategy is presented for diastereo- and enantioselective routes that can be used to prepare a wide variety of Z-homoallylic alcohols with significantly higher efficiency than is otherwise feasible. The approach entails the merger of several catalytic processes and is expected to facilitate the preparation of bioactive organic molecules. More specifically, Z-chloro-substituted allylic pinacolatoboronate is first obtained through stereoretentive cross-metathesis between Z-crotyl-B(pin) (pin = pinacolato) and Z-dichloroethene, both of which are commercially available. The organoboron compound may be used in the central transformation of the entire approach, an alpha- and enantioselective addition to an aldehyde, catalyzed by a proton-activated, chiral aminophenol-boryl catalyst. Catalytic cross-coupling can then furnish the desired Z-homoallylic alcohol in high enantiomeric purity. The olefin metathesis step can be carried out with substrates and a Mo-based complex that can be purchased. The aminophenol compound that is needed for the second catalytic step can be prepared in multigram quantities from inexpensive starting materials. A significant assortment of homoallylic alcohols bearing a Z-F3C-substituted alkene can also be prepared with similar high efficiency and regio-, diastereo-, and enantioselectivity. What is more, trisubstituted Z-alkenyl chloride moiety can be accessed with similar efficiency albeit with somewhat lower alpha-selectivity and enantioselectivity. The general utility of the approach is underscored by a succinct, protecting group-free, and enantioselective total synthesis of mycothiazole, a naturally occurring anticancer agent through a sequence that contains a longest linear sequence of nine steps (12 steps total), seven of which are catalytic, generating mycothiazole in 14.5% overall yield.

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Benzofuran – Wikipedia,
Benzofuran | C8H959O – PubChem

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Diastereoselective homoallylation and bis-homoallylation of N-tertbutanesulfinyl imines with organomagnesium compounds

The addition of but-3-enylmagnesium bromide and pent-4-enylmagnesium bromide to N-tert-butanesulfinyl aldimines in toluene as solvent proceeds with high diastereoselectivity to yield the corresponding products of homoallylation and bis-homoallylation, respectively. The reactions are diastereoselective, and the configuration of the sulfur atom of the sulfinyl group determined the stereochemical outcome. The reaction products are aminoalkene derivatives of potential synthetic interest as precursors of nitrogen containing heterocycles.

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Benzofuran – Wikipedia,
Benzofuran | C8H1047O – PubChem

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THE SERIES OF SUBSTITUTED BUTANOLIDES AND BUTENOLIDES. IV. 4-ARYLIDENE(HETEROARYLIDENE)-2-BUTENOLIDES

A larger number of 4-arylidene- and 4-heteroarylidene-2-butenolides were obtained by the reaction of 2-butenolide with aromatic and heteroaromatic aldehydes in the presence of piperidine.

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Benzofuran – Wikipedia,
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Copper-Catalyzed Regioselective Monodefluoroborylation of Polyfluoroalkenes en Route to Diverse Fluoroalkenes

Monodefluoroborylation of polyfluoroalkenes has been achieved in a regioselective manner under mild conditions via copper catalysis. The method has shown an extremely broad scope of substrates, including (difluorovinyl)arenes, tetrafluoroethylene (TFE), (trifluorovinyl)arenes, and trifluoromethylated monofluoroalkenes. The choice of boron source was important for the efficient transformation of (difluorovinyl)arenes; (Bpin)2 was suitable for substrates with an electron-deficient aryl group and (Bnep)2 for those with an electron-rich aryl group. Derivatization of the (fluoroalkenyl)boronic acid esters to the corresponding potassium trifluoroborate salts has rendered the products easily isolable, which greatly improved the synthetic practicality of the monodefluoroborylation reaction. Stoichiometric experiments indicate that the fate of the regioselectivity depends on the mode of beta-fluorine elimination, which depends on the substrate. Further transformation of the boryl group has allowed facile preparation of fluoroalkene derivatives as exemplified by the synthesis of a fluoroalkene mimic of atorvastatin, which potently inhibited the enzyme activity of HMG-CoA reductase.

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Benzofuran – Wikipedia,
Benzofuran | C8H1025O – PubChem

Discovery of Benzo[b]furan-2-carboxaldehyde

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Traceless stereoinduction in the one-pot assembly of all three rings of hexahydrodibenzopyrans

A one-pot method has been developed for the synthesis of all three rings of the hexahydrodibenzopyran ring system. This process involves a tandem sequence consisting of a benzannulation reaction of an alkenyl Fischer carbene complex and an alkyne followed by an elimination reaction that generates an o-quinone methide chromium tricarbonyl complex that is finally followed by an intramolecular heteroatom Diels-Alder cycloaddition. The stereoinduction for the overall process begins with the transfer of stereochemical information from the chiral center at the propargylic ether in the alkyne to the planar center of chirality in the in situ generated arene chromium tricarbonyl complexed intermediate and finally, after base-induced elimination to generate an o-quinone methide chromium tricarbonyl complexed intermediate, a transfer of chirality from the planar center of chirality in the o-quinone methide complex to the two new centers of chirality at positions 6a and 10a in the hexahydrodibenzopyran products upon intramolecular Diels-Alder reaction. The reactions of diastereomeric chiral propargyl ethers that contain an additional center of chirality can lead to high diastereoselectivity in the matched case and to low selectivity in the mismatched case. Copyright

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Benzofuran – Wikipedia,
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New explortion of Benzo[b]furan-2-carboxaldehyde

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Synthesis and antibacterial activity of novel chalcone derivatives of apocynin

A series of novel chalcones 1a- 1l (12 compounds) has been synthesized by using commercially available apocynin and aromatic aldehydes. The newly synthesized chalcone derivatives were screened for their antibacterial activities against gram positive and gram negative bacteria at the concentrations 10 of mug/mL with reference to the standard antibacterial drug Gentamycin. The screening results revealed that among the tested analogs, compounds having the hetero rings such as benzo[b]furan, furan and pyridine (1j,1k and 1l) in the structure exhibited excellent antibacterial activity while the compounds bearing fluorine, 2-CF3, 4-CF3 and 4-OCF3 (1f, 1g, 1h and 1i) also exhibited good to excellent activity. 2013 Bentham Science Publishers.

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Benzofuran – Wikipedia,
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Synthesis and biological evaluation of piperazinyl-2-(benzo)thiophen/- furan-2-yl-acetonitriles as strecker reaction products

Single step construction of heterocyclic alpha-aminonitriles has been carried out using Indium Powder as catalyst in water medium via Strecker reaction methodology. The multicomponent reaction products were examined for their inhibitory potential against two Gram-positive bacteria (S. aureus and B. cereus), three Gram-negative bacteria (E. coli, P. aeruginosa and K. pneumoniae) and two fungal species (A. niger and C. albicans). The biological screening identified that the some compounds were found to possess promising antimicrobial (6.25-50 mug/mL of MIC) potential. A structure-activity relationship (SAR) study was explored to facilitate further development of this new class of compounds. The structural assignments of the new products were done on the basis of IR, 1H NMR, 13C NMR spectroscopy and elemental analysis.

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Benzofuran – Wikipedia,
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