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One-pot synthesis of pyrimido[1,6-a ]indol-1(2 H)-one derivatives by a nucleophilic addition/Cu-catalyzed N-arylation/Pd-catalyzed C-H activation sequential process

A novel and convenient one-pot synthesis of pyrimido[1,6-a]indol-1(2H)-one derivatives through a nucleophilic addition/Cu-catalyzed N-arylation/Pd- catalyzed C-H activation sequential process is described. The reaction of easily prepared ortho-gem-dibromovinyl isocyanates with N-alkyl-anilines gave the desired indole derivatives in moderate to good yields.

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Isoxazole – Wikipedia,
Isoxazole | C3H3NO – PubChem

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Related Products of 7063-99-2, Because a catalyst decreases the height of the energy barrier, its presence increases the reaction rates of both the forward and the reverse reactions by the same amount.7063-99-2, Name is Ethyl 5-phenylisoxazole-3-carboxylate, molecular formula is C12H11NO3. In a article,once mentioned of 7063-99-2

SUBSTITUTED OXADIAZOLE DERIVATIVES AS S1P AGONISTS IN THE TREATMENT OF AUTOIMMUNE AND INFLAMMATORY DISEASES

Disclosed are compounds of Formula (I) [INSERT CHEMICAL STRUCTURE HERE] (I) or pharmaceutically acceptable salts thereof, wherein Q is [INSERT CHEMICAL STRUCTURE HERE] or [INSERT CHEMICAL STRUCTURE HERE]; R1 is alkyl or aryl, said aryl optionally substituted with one to five substituents independently selected from C1 to C6 alkyl, C1 to C4 haloalkyl, OR4, and/or halogen; and R2, R3, R4, and n are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.

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Isoxazole – Wikipedia,
Isoxazole | C3H3NO – PubChem

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The first synthesis of N-alkyl-N-arylthiocarbamoylacetates and acetic acids

N-Alkyl-N-arylthiocarbamoylacetates, the key intermediates for the synthesis of novel antinephritic agents, have been prepared for the first time. Some of the esters were in turn hydrolyzed to the corresponding acids. An alternative, indirect synthetic route was also developed to prepare some unusual acids.

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Isoxazole – Wikipedia,
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N-Methylation of amines and nitroarenes with methanol using heterogeneous platinum catalysts

We report herein the selective N-methylation of amines and nitroarenes with methanol under basic conditions using carbon-supported Pt nanoparticles (Pt/C) as a heterogeneous catalyst. This method is widely applicable to four types of N-methylation reactions: (1) N,N-dimethylation of aliphatic amines under N2, (2) N-monomethylation of aliphatic amines under 40 bar H2, (3) N-monomethylation of aromatic amines under N2, and (4) tandem synthesis of N-methyl anilines from nitroarenes and methanol under 2 bar H2. All these reactions under the same catalytic system showed high yields of the corresponding methylamines for a wide range of substrates, high turnover number (TON), and good catalyst reusability. Mechanistic studies suggested that the reaction proceeded via a borrowing hydrogen methodology. Kinetic results combined with density functional theory (DFT) calculations revealed that the high performance of Pt/C was ascribed to the moderate metal?hydrogen bond strength of Pt.

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Isoxazole – Wikipedia,
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Microwave assisted synthesis of phenanthridinones and dihydrophenanthridines by vasicine/KO: T Bu promoted intramolecular C-H arylation

A simple, efficient, rapid and transition metal-free methodology has been developed by utilizing vasicine (a natural product), as a catalyst for the synthesis of phenanthridinones and dihydrophenanthridines. The reaction proceeds through intramolecular C-H arylation with aryl halides in the presence of KOtBu as a base under microwave irradiation in sulfolane as a solvent. The reaction proceeds well with various aryl iodides, bromides and more remarkably with less reactive aryl chlorides for 15 minutes, providing the corresponding products in 45-90% yields.

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Isoxazole – Wikipedia,
Isoxazole | C3H3NO – PubChem

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N-H insertion reactions of rhodium carbenoids. Part 3. The development of a modified Bischler indole synthesis and a new protecting-group strategy for indoles

A modified version of the Bischler indole synthesis has been developed in which the key step is the N-H insertion reaction of rhodium carbene intermediates derived from alpha-diazo-beta-ketoesters with anilines. Thus N-methylanilines 1 react with diazoketoesters 2 in the presence of dirhodium(II) acetate to give (N-arylamino)ketones 3, cyclisation of which using boron trifluoride-ethyl acetate or acidic ion exchange resin gives the indoles 4. In order to extend this method to the synthesis of N-unsubstituted indoles, a new protecting group strategy for indoles was developed. In this, anilines are reacted with alpha,beta-unsaturated-esters or -sulfones to give the conjugate addition products 6 and 9, cyclisation of which gives indoles 8 and 11. The N-(2-ethoxycarbonylethyl)- and -(2-sulfonylethyl)- protecting groups are readily removed from indoles 8 and 11 by treatment with base.

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Isoxazole – Wikipedia,
Isoxazole | C3H3NO – PubChem

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A Facile Synthesis of Trifluoromethylamines by Oxidative Desulfurization-Fluorination of Dithiocarbamates

Trifluoromethylamines are easily synthesized from dithiocarbamates by a reagent system consisting of tetrabutylammonium dihydrogentrifluoride and an N-halo imide under mild conditions. When this reaction was applied to dithiocarbamates ArN(R)CS2Me at higher temperatures, the trifluoromethylation was accompanied by halogen substitution at the p-position of the Ar group. The synthesis of trifluoromethyl-substituted adenosine is also described.

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Isoxazole – Wikipedia,
Isoxazole | C3H3NO – PubChem

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In homogeneous catalysis, the catalyst is in the same phase as the reactant. The number of collisions between reactants and catalyst is at a maximum.In a patent, 33282-15-4, name is 5-(4-Hydroxyphenyl)isoxazole-3-carboxylic acid, introducing its new discovery. HPLC of Formula: C10H7NO4

SYNTHESIS AND BIOLOGICAL ACTIVITY OF SOME BASIC-SUBSTITUTED 4,9-DIHYDRO-3-METHYL-4-OXO-1H(2H)-PYRAZOLO<3,4-b>QUINOLINES

Compounds Ia, Ib were obtained by an alkylation of 4,9-dihydro-6-hydroxy-1,3,9-trimethyl-4-oxo-1H-pyrazolo<3,4-b>quinoline (VIIb) with the respective dialkylaminoalkyl chloride.The same alkylation of 4,9-dihydro-6-hydroxy-2,3,9-trimethyl-4-oxo-2H-pyrazolo<3,4-b>quinoline (VIIIb) yielded compounds IIa and IIb.Similar alkylation of 4,9-dihydro-3,9-dimethyl-4-oxo-1H-pyrazolo<3,4-b>quinoline (IXa) and its 6-methoxy derivative (IXb) afforded IIIa – IIId.Compound IV was prepared from 4-chloro-3-methyl-1H-pyrazolo<3,4-b>quinoline (Xa) via its 1-(3-dimethylaminopropyl) derivative (Xb).Compounds VIa, VIb were prepared from 4,9-dihydro-6-hydroxy-3,9-dimethyl-4-oxo-1H-pyrazolo<3,4-b>quinoline (IXc) and the respective dialkylaminoalkyl chloride.The compounds prepared were tested for antiviral activity in vivo in mice against influenza virus A2-Hongkong and encephalomyocarditis virus.

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Reference:
Isoxazole – Wikipedia,
Isoxazole | C3H3NO – PubChem

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Synthesis and quantitative structure-activity relationship of imidazotetrazine prodrugs with activity independent of O6-methylguanine-DNA- methyltransferase, DNA mismatch repair, and p53

The antitumor prodrug temozolomide is compromised by its dependence for activity on DNA mismatch repair (MMR) and the repair of the chemosensitive DNA lesion, O6-methylguanine (O6-MeG), by O6-methylguanine-DNA-methyltransferase (E.C. 2.1.1.63, MGMT). Tumor response is also dependent on wild-type p53. Novel 3-(2-anilinoethyl)-substituted imidazotetrazines are reported that have activity independent of MGMT, MMR, and p53. This is achieved through a switch of mechanism so that bioactivity derives from imidazotetrazine-generated arylaziridinium ions that principally modify guanine-N7 sites on DNA. Mono- and bifunctional analogues are reported, and a quantitative structure-activity relationship (QSAR) study identified the p-tolyl-substituted bifunctional congener as optimized for potency, MGMT-independence, and MMR-independence. NCI60 data show the tumor cell response is distinct from other imidazotetrazines and DNA-guanine-N7 active agents such as nitrogen mustards and cisplatin. The new imidazotetrazine compounds are promising agents for further development, and their improved in vitro activity validates the principles on which they were designed.

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Isoxazole – Wikipedia,
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Catalytic synthesis of secondary amine-containing polymers: Variable hydrogen bonding for tunable rheological properties

A synthetic protocol using atom-economic, catalytic hydroaminoalkylation and ring-opening metathesis polymerization (ROMP) has been developed for the versatile synthesis of a new class of aryl-substituted secondary amine-containing polymers. This catalytic route minimizes waste generation and avoids protection/deprotection protocols, postpolymerization modification, and byproduct formation. Different amines can be readily incorporated to access variable hydrogen-bonding characteristics. Thermal and melt rheological characterization has shown the profound effect of hydrogen bonding on the bulk properties of these amine-containing norbornene polymers.

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Reference:
Isoxazole – Wikipedia,
Isoxazole | C3H3NO – PubChem