Tag: M.W=200-250

den Hertog, H. J. published the artcileHetarynes. VI. Amination of bromoethoxypyridines, SDS of cas: 17117-13-4, the main research area is .

cf. CA 58, 11325a; 60, 1724d. Some bromoethoxypyridines were aminated with KNH2 in liquid NH3. The 3-bromo- and 4-bromoethoxypyridines reacted via hetaryne intermediates. The reaction of 2-bromo-6-ethoxypyridine proceeded via a rearrangement. 2-Bromo-4-ethoxypyridine, b2 104-6°, m. 35-6°, was prepared by treating 2-bromo-4-hydroxypyridine with diazoethane in Et2O for 16 hrs. at room temperature 4-Bromo-2-ethoxypyridine, m. 5.5-7°, was prepared from 4-amino-2-ethoxypyridine. Amination was carried out by adding 2.5 millimoles of the bromoethoxypyridine in Et2O to a solution prepared from 10 millimoles K and 30-40 ml. liquid NH3 in the presence of Fe(NO3)3 at -33° over a period of 10 min. (with stirring). The reaction-was stopped with 12 millimoles NH4Cl and the mixture evaporated, extracted with Et2O, and analyzed by gas chromatography. The following results were obtained [bromoethoxypyridine used and the aminoethoxypyridine(s) (molar ratio) produced given]: 4-bromo-2-ethoxy, 3-amino-2-ethoxy[-(1-2%)], 4-amino-2-ethoxy[-(98-99%)]; 4-bromo-3-ethoxy, 5-amino-3-ethoxy; 3-bromo-2-ethoxy, 3-amino-2-ethoxy (3), 4-amino-2-ethoxy (97); 3-bromo-4-ethoxy, 2-amino-4-ethoxy (55-60), 2-amino-5-bromo-4-ethoxy (15-20), 4-ethoxy (25); 3-bromo-5-ethoxy, 3-amino-5-ethoxy; 3-bromo-6-ethoxy, 3-amino-6-ethoxy (35), 4-amino-6-ethoxy (65); 2-bromo-3-ethoxy, 2-amino-3-ethoxy (99), 3-ethoxy (1); 2-bromo-4-ethoxy, 2-amino-4-ethoxy; 2-bromo-5-ethoxy, 2-amino-5-ethoxy (90-95), 5-ethoxy (5-10); 2-bromo-6-ethoxy, 2-amino-6-ethoxy (80-85), 4-amino-6-ethoxy (10-15).

Recueil des Travaux Chimiques des Pays-Bas published new progress about Amination. 17117-13-4 belongs to class pyridine-derivatives, name is 2-Bromo-4-ethoxypyridine, and the molecular formula is C7H8BrNO, SDS of cas: 17117-13-4.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Croitoru, M. D. published the artcileDirect HPLC-UV determination of cyclemate, saccharine and aspartame from soft drinks, Recommanded Product: Ethyl 4-hydroxy-6-oxo-6,7-dihydrothieno[2,3-b]pyridine-5-carboxylate, the main research area is cyclamate saccharine aspartame soft drink HPLC UV detection.

Artificial sweeteners were introduced in therapy as sugar substitutes for diabetic patients. Nowadays these substances are widely used for sugar substitution in low calorie drinks and sweets. Most commonly used products to date are saccharine, cyclamate, aspartame, and acesulfam; maximum accepted daily intakes are stated for each one. A simple reverse phase (RP18) HPLC-UV method with direct detection (196 nm) was developed by us in order to measure the concentrations of the three sweeteners. No sample preparation is required, other than dilution Limits of detection are 12 mg l-1, 0.5 mg l-1 and lower than 0.25 mg l-1 for cyclamate, aspartame and saccharine, resp. Concentrations ranged between 113.14-280.07 mg l-1 in the case of cyclamate, 17.96-50.94 mg l-1 for saccharine, and 9.94-296.82 mg l-1 for aspartame.

Acta Alimentaria published new progress about Beverages. 99429-68-2 belongs to class pyridine-derivatives, name is Ethyl 4-hydroxy-6-oxo-6,7-dihydrothieno[2,3-b]pyridine-5-carboxylate, and the molecular formula is C10H9NO4S, Recommanded Product: Ethyl 4-hydroxy-6-oxo-6,7-dihydrothieno[2,3-b]pyridine-5-carboxylate.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Schmidt, Michael A. published the artcileEffect of Terminal Alkylation of Aryl and Heteroaryl Hydrazines in the Fischer Indole Synthesis, Computed Properties of 3469-63-4, the main research area is Fischer indole synthesis; hydrazine ketone alkylation amidation cross coupling.

The effect of alkylation on the terminal position of aryl and heteroaryl hydrazines in the Fischer indole synthesis was examined Compared to their unalkylated counterparts, reactions using alkylated s provided indole products with higher yields and faster rates. The reactions can be conducted at lower temperatures and are compatible with acid-sensitive functionality. The terminally alkylated hydrazines were readily prepared by a new two-step sequence and held as stable hydrazinium salts. The mild formation of the salts along with the favorable Fischer indole reaction conditions highlights the potential of this approach in later-stage synthetic use.

Journal of Organic Chemistry published new progress about Alkylation. 3469-63-4 belongs to class pyridine-derivatives, name is Ethyl 5-methoxy-1H-pyrrolo[2,3-c]pyridine-2-carboxylate, and the molecular formula is C11H12N2O3, Computed Properties of 3469-63-4.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Swanson, Devin M. published the artcileIdentification and biological evaluation of 4-(3-trifluoromethylpyridin-2-yl)piperazine-1-carboxylic acid (5-trifluoromethylpyridin-2-yl)amide, a high affinity TRPV1 (VR1) vanilloid receptor antagonist, Computed Properties of 306934-70-3, the main research area is vanilloid receptor antagonist preparation analgesic.

High throughput screening using the recombinant human TRPV1 receptor was used to identify a series of pyridinylpiperazine ureas as TRPV1 vanilloid receptor ligands. Exploration of the structure-activity relationships by parallel synthesis identified the essential pharmacophoric elements for antagonism that permitted further optimization via targeted synthesis to provide a potent orally bioavailable and selective TRPV1 modulator 41 active in several in vivo models.

Journal of Medicinal Chemistry published new progress about Analgesics. 306934-70-3 belongs to class pyridine-derivatives, name is 1-(5-(Trifluoromethyl)pyridin-2-yl)-1,4-diazepane, and the molecular formula is C11H14F3N3, Computed Properties of 306934-70-3.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Charushin, Valery N. published the artcileRing transformations in reactions of heterocyclic compounds with nucleophiles. Part 26. 1,3- and 1,4-Cyclo adducts as intermediates in the pyrimidine to pyridine ring transformation of 5-nitropyrimidines by α-phenylacetamidines, Formula: C9H11N3O3, the main research area is pyrimidine reaction nucleophile; acetamidine phenyl reaction pyrimidine; pyridine amino nitropyrimidine.

5-Nitropyrimidine reacts with PhCH2CR:NH (R = NH2, NMe2, NEt2) at -40° to form σ adducts at the C-2 position of the ring, but gives 2-aminopyridine derivatives I at temperatures above 0 °. Experiments with 15N-labeled PhCH2C(:NH)NH2 showed that the reaction proceeds via different reaction pathways with replacement of either the N(1)-C(2)-N(3) or N(1)-C(2) fragment of the pyrimidine ring by the C-C-N or the C-C moiety of the amidine. The role of 1,3- and 1,4-cycloadducts as possible intermediates in the ring-transformation reaction is discussed.

Journal of Organic Chemistry published new progress about Nucleophiles. 26820-62-2 belongs to class pyridine-derivatives, name is 4-(5-Nitropyridin-2-yl)morpholine, and the molecular formula is C9H11N3O3, Formula: C9H11N3O3.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Barker, John M. published the artcileThienopyridines. Part 7. Some electrophilic substitution reactions of thieno[2,3-b]- and -[3,2-b]pyridine isosteres of 4-oxygenated and 2,4-dioxygenated quinolines, Product Details of C10H9NO4S, the main research area is electrophilic substitution thienopyridine regiochem; quinolinone isostere electrophilic substitution.

Electrophilic substitution reactions were examined of the title compounds I, II [X = NMe, X1 = CO (III); X = CO, X1 = NH (IV), NMe (V)], VI, and VII. The 4-quinolone analogs I and IV, like the parent compound, were monobrominated and (diethylamino)methylated in the pyridine ring α to the CO group. However, whereas 4-quinolone and IV were nitrated in the pyridine ring by HNO3 alone, I was nitrated mainly in the thiophene ring at C-2 under these conditions. The methylated compounds III and V showed a similar regiochem. to their nonmethylated analogs, although their reactivity was lower. I and II were dinitrated by mixed HNO3-H2SO4 at the position α to the CO group in the pyridine ring and at either C-2 in the [2,3-b] isomers (I and III) or C-3 in the [3,2-b] compounds (IV and V); dibromination of I, III, and IV followed a similar pattern. Mannich reactions of VI and VII occurred in the pyridine rings, whereas bromination occurred in the thiophene and pyridine rings in VI and VII, resp.

Journal of Chemical Research, Synopses published new progress about Bromination. 99429-68-2 belongs to class pyridine-derivatives, name is Ethyl 4-hydroxy-6-oxo-6,7-dihydrothieno[2,3-b]pyridine-5-carboxylate, and the molecular formula is C10H9NO4S, Product Details of C10H9NO4S.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Jin, Bo published the artcileSynthesis, Antibacterial and Anthelmintic Activity of Novel 3-(3-Pyridyl)-oxazolidinone-5-methyl Ester Derivatives, Category: pyridine-derivatives, the main research area is pyridyl oxazolidone methyl ester preparation stereoselective antibacterial anthelmintic human; anthelmintic activity; antibacterial activity; molecular docking; pyridinyl-oxazolidinone derivatives; synthesis.

In this study, a series of 3-(3-pyridyl)-oxazolidone-5-Me ester derivatives I [X = O, C(O)CH2Bn, C(O)NCy, etc.; R1 = C(O)Me, C(O)Cy, S(O)2Me, etc.] was synthesized and characterized by 1H NMR, 13C NMR and LC-MS. The conducted screening antibacterial studies of the new 3-(3-pyridyl)-oxazolidone-5-Me ester derivatives I established that the Me sulfonic acid esters have broad activity spectrum toward Staphylococcus aureus, Streptococcus pneumoniae, Bacillus subtilis and Staphylococcus epidermidis. Among them, compound I [X = O; R1 = C(O)NCy] was the most potent activity, with an MIC of 16μg/mL against B.subtilis and could reduce the instantaneous growth rate of bacteria. Furthermore, mol. docking studies were also simulated for compound I [X = O; R1 = C(O)NCy] to predict the specific binding mode of this compound In addition, anthelmintic activity of these compounds was also evaluated against adult Indian earthworms (Pheretima posthuman). The results showed that compound I [X = O, R1 = C(O)Cy] had the best effect. These results above could provided exptl. reference for the development of novel antibacterial and anthelmintic drugs.

Molecules published new progress about Anthelmintics. 26820-62-2 belongs to class pyridine-derivatives, name is 4-(5-Nitropyridin-2-yl)morpholine, and the molecular formula is C9H11N3O3, Category: pyridine-derivatives.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Mahdhaoui, Faouzi published the artcileSNAr reactions of substituted pyridines with secondary amines in aqueous solution: Kinetic and reactivity indices in density functional theory, Product Details of C9H11N3O3, the main research area is nitropyridine cyclic amine nucleophilic aromatic substitution kinetics mechanism.

A kinetic study is reported for the reactions of 2-methoxy-3-nitropyridine 1a and 2-methoxy-5-nitropyridine 1b with three secondary amines 2a-c (morpholine, piperidine, and pyrrolidine) in aqueous solution at 20°C. The Bronsted-type plots are linear with βnuc = 0.52 and 0.55 for pyridines 1a and 1b, resp., indicating that the reaction proceeds through a SNAr mechanism in which the first step is the rate-determining step. Addnl. theor. calculations using the DFT/B3LYP method confirm that the C-2 carbon being the most electrophilic center for the both pyridines 1a and 1b. The second-order rate constants have been used to evaluate the electrophilicity parameters E of 1a and 1b according to the linear free energy relationship log k (20°C) = sN (N + E). The E parameters thus derived are compared with the electrophilic reactivities of a large variety of anisoles. The validity of these E values has been satisfactorily verified by comparison of calculated and exptl. second-order rate constants for the reactions of pyridines 1a and 1b with anion of Et benzylacetate.

International Journal of Chemical Kinetics published new progress about Atomic charge. 26820-62-2 belongs to class pyridine-derivatives, name is 4-(5-Nitropyridin-2-yl)morpholine, and the molecular formula is C9H11N3O3, Product Details of C9H11N3O3.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Spencer, John published the artcileSynthesis and solid state study of pyridine- and pyrimidine-based fragment libraries, Quality Control of 26820-62-2, the main research area is preparation pyridine pyrimidine library solid state study microwave irradiation.

A library of pyridines and pyrimidines, e.g. I [X = CH, N], has been synthesized in excellent yields employing microwave and flow chem. methodologies. Work-up bottlenecks have been facilitated substantially by the use of supported reagents and many of the final compounds have been studied in the solid state by single crystal X-ray diffraction.

Tetrahedron Letters published new progress about Chemical library. 26820-62-2 belongs to class pyridine-derivatives, name is 4-(5-Nitropyridin-2-yl)morpholine, and the molecular formula is C9H11N3O3, Quality Control of 26820-62-2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Parrino, Barbara published the artcileSynthesis of the new ring system bispyrido[4′,3′:4,5]pyrrolo[1,2-a:1′,2′-d]pyrazine and its deaza analogue, Category: pyridine-derivatives, the main research area is pyrrolopyridinecarboxylic acid preparation; bispyridopyrrolopyrazine dione preparation antineoplastic mol docking; pyridopyrrolopyrazino indole dione antineoplastic mol docking.

A series of bispyridopyrrolopyrazine diones I [R1 = R4 = H, Cl, OMe; R2 = R3 = H, OMe] and their deaza analogs pyridopyrrolopyrazinoindole diones II [R1 = R2 = H, Cl, OMe] was synthesized and evaluated for their antineoplastic activities and mol. docking studies. Among the synthesized compounds I [R1 = R2 = R4 = H; R3 = OMe] and II [R1 = R2 = H; R1 = OMe, R2 = H; R1 = H, R2 = OMe] exhibited modest activity against MCF7 (a breast cancer cell line) and/or UO-31 (a renal cancer cell line).

Molecules published new progress about Antitumor agents. 3469-63-4 belongs to class pyridine-derivatives, name is Ethyl 5-methoxy-1H-pyrrolo[2,3-c]pyridine-2-carboxylate, and the molecular formula is C11H12N2O3, Category: pyridine-derivatives.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem