Category: 86129-63-7

Moretto, A. F.; Kirincich, S. J.; Xu, W. X.; Smith, M. J.; Wan, Z.-K.; Wilson, D. P.; Follows, B. C.; Binnun, E.; Joseph-McCarthy, D.; Foreman, K.; Erbe, D. V.; Zhang, Y. L.; Tam, S. K.; Tam, S. Y.; Lee, J. published the artcile< Bicyclic and tricyclic thiophenes as protein tyrosine phosphatase 1B inhibitors>, Application of C9H9Cl2NO2, the main research area is bicyclic tricyclic thiophene protein tyrosine phosphatase inhibitor.

A novel pyridothiophene inhibitor of PTP1B was discovered by rational screening of phosphotyrosine mimics at high micromolar concentrations The potency of this lead compound has been improved significantly by medicinal chem. guided by x-ray crystallog. and mol. modeling. Excellent consistency has been observed between structure-activity relationships and structural information from PTP1B-inhibitor complexes.

Bioorganic & Medicinal Chemistry published new progress about High-throughput screening. 86129-63-7 belongs to class pyridine-derivatives, and the molecular formula is C9H9Cl2NO2, Application of C9H9Cl2NO2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Kooyman, E. C.; Wibaut, J. P. published the artcile< Pyridine and quinoline derivatives. LX. The orientation of the CO2C2H5 group in the condensation product of malonic ester and β-aminocrotonic acid ester>, Product Details of C9H9Cl2NO2, the main research area is .

In the 2-methyl-4,6-dihydroxypyridinecarboxylate described by Knoevenagel and Fries (Ber. 31, 767(1898)), the position of the carboxylate group was unknown. The location of this group at 5 rather than at 3 was established by the following reactions: The original condensation product, heated with POCl3 at 120° in a sealed tube for 4 hrs., yielded a mixture of the acid chloride (I) and the Et ester (II) of 2-methyl-4,6-dichloro-5-pyridinecarboxylic acid, which could be separated by fractional distillation at 1 mm. The first fraction b. 97-104°, and after a 2nd distillation was obtained as a clear, colorless oil which solidified at 14.8°. The analyses agreed fairly well with C7H4ONCl3. On heating with H2O, HCl was split off, and the free acid was obtained. The compound was therefore believed to be I. The 2nd fraction b. 113-16°. It was obtained in 30% yield as white needles, m. 56° (50% EtOH), which were readily soluble in Et2O and EtOH, and sparingly soluble in H2O. It was identified as II. The free acid obtained from the ester by saponification m. 151.5° (dilute HCl) and was slightly soluble in H2O, very slightly soluble in HCl, but readily soluble in Et2O and EtOH. By catalytic reduction of II in absolute EtOH with Pd chloride and KOAc, the Cl was removed, and Et 2-methyl-5-pyridinecarboxylate (III) was obtained in 72% yield as a colorless oil b2 97° (Graf, C.A. 26, 1932). By saponification of III with KOH, preparation of the Cu salt, and decomposition with H2S, the free acid (IV) was obtained. It was purified by sublimation at 180°/35 mm. and m. 209-10°. It was identified by mixed m.p. with a sample prepared from 2-methyl-5-ethylpyridine. The amide (V), m. 196°, was prepared from III by shaking with NH3 according to the method of Graf. The picrate of the ester m. 170-1° (light yellow needles from alc. picric acid). The amide and the picrate showed no m.p. depression when mixed with the corresponding amide and picrate prepared from the ester obtained from 2-methyl-5-ethylpyridine.

Recueil des Travaux Chimiques des Pays-Bas et de la Belgique published new progress about 86129-63-7. 86129-63-7 belongs to class pyridine-derivatives, and the molecular formula is C9H9Cl2NO2, Product Details of C9H9Cl2NO2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Croisy-Delcey, Martine; Bisagni, Emile published the artcile< Aza analogs of lucanthone: synthesis and antitumor and bactericidal properties>, Product Details of C9H9Cl2NO2, the main research area is aza analog lucanthone; antitumor lucanthone aza analog; bactericide lucanthone aza analog.

Aza analogs of lucanthone (e.g., I; X = S, NH) were synthesized for evaluation as antitumor drugs. None of the compounds had significant cytotoxic effects on either Friend-tumor or L1210 leukemia cells. However, I (X = NH) had noticeable antibiotic properties.

Journal of Medicinal Chemistry published new progress about Antitumor agents. 86129-63-7 belongs to class pyridine-derivatives, and the molecular formula is C9H9Cl2NO2, Product Details of C9H9Cl2NO2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Dyck, Brian; Grigoriadis, Dimitri E.; Gross, Raymond S.; Guo, Zhiqiang; Marinkovic, Dragan; McCarthy, James R.; Moorjani, Manisha; Regan, Collin F.; Saunders, John; Schwaebe, Michael K.; Szabo, Tomas; Williams, John P.; Zhang, Xiaohu; Bozigian, Haig; Chen, Ta Kung published the artcile< Potent, Orally Active Corticotropin-Releasing Factor Receptor-1 Antagonists Containing a Tricyclic Pyrrolopyridine or Pyrazolopyridine Core>, Application of C9H9Cl2NO2, the main research area is oral CRF1 receptor antagonist tricyclic pyrrolopyridine pyrazolopyridine core preparation.

Two new classes of tricyclic-based corticotropin-releasing factor (CRF1) receptor-1 antagonists were designed by constraining known 1H-pyrrolo[2,3-b]pyridine and 1H-pyrazolo[3,4-b]pyridine ligands. Pyrrole- and pyrazole-based mols. 19g and 22a, resp., were discovered that potently bind the recombinant CRF1 receptor (Ki = 3.5, 2.9 nM) and inhibit adrenocorticotropic hormone (ACTH) release from rat pituitary cell culture (IC50 = 14, 6.8 nM). These compounds show good oral bioavailability (F = 24%, 7.0%) and serum half-lives in rats (t1/2 = 6.3, 12 h) and penetrate the rat brain ([brain]/[plasma] = 0.27, 0.52) but tend toward large volumes of distribution (VD = 38, 44 L kg-1) and rapid clearances (CL = 70, 43 mL min-1 kg-1). When given orally, both the pyrazole and the pyrrole leads dose-dependently inhibit stress-induced ACTH release in vivo. ACTH reductions of 84-86% were observed for 30 mg kg-1 doses.

Journal of Medicinal Chemistry published new progress about Blood-brain barrier (penetration). 86129-63-7 belongs to class pyridine-derivatives, and the molecular formula is C9H9Cl2NO2, Application of C9H9Cl2NO2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Di Fabio, Romano; Arban, Roberto; Bernasconi, Giovanni; Braggio, Simone; Blaney, Frank E.; Capelli, Anna M.; Castiglioni, Emiliano; Donati, Daniele; Fazzolari, Elettra; Ratti, Emiliangelo; Feriani, Aldo; Contini, Stefania; Gentile, Gabriella; Ghirlanda, Damiano; Sabbatini, Fabio M.; Andreotti, Daniele; Spada, Simone; Marchioro, Carla; Worby, Angela; St-Denis, Yves published the artcile< Dihydropyrrole[2,3-d]pyridine Derivatives as Novel Corticotropin-Releasing Factor-1 Antagonists: Mapping of the Receptor Binding Pocket by in Silico Docking Studies>, COA of Formula: C9H9Cl2NO2, the main research area is pyrrolo pyridine preparation CRF1 antagonist antidepressant SAR.

In an effort to discover novel CRF-1 receptor antagonists exhibiting improved physicochem. properties, a dihydropirrole[2,3]pyridine scaffold was designed and explored in terms of the SAR of the substitution at the pendent Ph ring and the nature of the heterocyclic moieties present in the upper region of the mol. Selective and potent compounds have been discovered endowed with reduced ClogP with respect to compounds known in the literature. Of particular relevance was the finding that the in vitro affinity of the series was maintained by reducing the overall lipophilicity. The results achieved by this exploration enabled the formulation of a novel hypothesis on the nature of the receptor binding pocket of this class of CRF-1 receptor antagonists, making use of in silico docking studies of the putative nonpeptidic antagonist binding site set up in house by homol. modeling techniques.

Journal of Medicinal Chemistry published new progress about Antidepressants. 86129-63-7 belongs to class pyridine-derivatives, and the molecular formula is C9H9Cl2NO2, COA of Formula: C9H9Cl2NO2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Keller, P. A. published the artcile< Product class 2: pyridinones and related systems>, Category: pyridine-derivatives, the main research area is review pyridinone preparation; pyridinethione preparation review; pyridineselenone preparation review; pyridinetellurone preparation review.

A review of methods to prepare pyridinones and related systems is presented. Synthetic methods include cyclization, aromatization, ring transformation, and substituent modification. The parent pyridinones are generally stable and are easily handled under standard laboratory conditions. The corresponding pyridinethiones are generally more reactive but have the advantage of generally requiring only standard laboratory equipment for their handling. The pyridineselenones are more reactive and the pyridinetellurones have not been comprehensively studied and characterized due to their reactivity and associated difficulty in production

Science of Synthesis published new progress about Aromatization. 86129-63-7 belongs to class pyridine-derivatives, and the molecular formula is C9H9Cl2NO2, Category: pyridine-derivatives.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Caron, Stephane; Do, Nga M.; Sieser, Janice E.; Whritenour, David C.; Hill, Paul D. published the artcile< Preparation of a Corticotropin-Releasing Factor Antagonist by Nucleophilic Aromatic Substitution and Copper-Mediated Ether Formation>, Formula: C9H9Cl2NO2, the main research area is butylamino aryloxy nicotinate preparation process development drug candidate; corticotropin releasing factor antagonist preparation process development drug candidate; nucleophilic aromatic substitution ether formation copper drug candidate preparation.

Several synthetic approaches to a corticotropin-releasing factor (CRF) antagonist containing a tetrasubstituted pyridine (I) were evaluated. In particular, nucleophilic aromatic substitutions on 2,4-dichloropyridine derivatives were attempted using 2,6-dimethyl-4-chlorophenol, (S)-2-aminobutanol, and several sulfur nucleophiles. It was found that a copper-mediated coupling of a phenoxymesylate was preferred for preparation of the diarylether followed by nucleophilic aromatic substitution to introduce the amine side chain, affording the desired drug candidate (I) in two steps from the com. available Me 2,4-dichloro-6-methylnicotinate.

Organic Process Research & Development published new progress about Etherification. 86129-63-7 belongs to class pyridine-derivatives, and the molecular formula is C9H9Cl2NO2, Formula: C9H9Cl2NO2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Mittelbach, Martin published the artcile< An easy and convenient synthesis of 6-methyl-4(1H)-pyridone-3-carboxylic acid>, Reference of 86129-63-7, the main research area is nicotinic acid dihydro oxo methyl.

The title acid (I) was prepared from a nicotinic acid derivative Et 2,4-dichloro-6-methylnicotinate was treated with Na and R1OH (R1 = Me, Et), the alkoxy analog products II were subjected to reductive dechlorination, and the products were hydrolyzed by HCl to give I.

Synthesis published new progress about 86129-63-7. 86129-63-7 belongs to class pyridine-derivatives, and the molecular formula is C9H9Cl2NO2, Reference of 86129-63-7.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Messick, Troy E.; Tolvinski, Lois; Zartler, Edward R.; Moberg, Anna; Frostell, Asa; Smith, Garry R.; Reitz, Allen B.; Lieberman, Paul M. published the artcile< Biophysical screens identify fragments that bind to the viral DNA-binding proteins EBNA1 and LANA>, Synthetic Route of 86129-63-7, the main research area is DNA EBNA1 LANA protein ligand interaction binding fragment NMR; biophys screen surface plasmon resonance saturation transfer difference; Epstein–Barr nuclear antigen 1; Epstein–Barr virus; Kaposi’s sarcoma associated herpesvirus (KSHV); fragment-based lead discovery; latency-associated nuclear antigen; protein–DNA interaction; saturation transfer difference-nuclear magnetic resonance; surface plasmon resonance.

The human gamma-herpesviruses Epstein-Barr virus (EBV) (HHV-4) and Kaposi’s sarcoma-associated herpesvirus (KSHV) (HHV-8) are responsible for a number of diseases, including various types of cancer. Epstein-Barr nuclear antigen 1 (EBNA1) from EBV and latency-associated nuclear antigen (LANA) from KSHV are viral-encoded DNA-binding proteins that are essential for the replication and maintenance of their resp. viral genomes during latent, oncogenic infection. As such, EBNA1 and LANA are attractive targets for the development of small-mol. inhibitors. To this end, we performed a biophys. screen of EBNA1 and LANA using a fragment library by saturation transfer difference (STD)-NMR spectroscopy and surface plasmon resonance (SPR). We identified and validated a number of unique fragment hits that bind to EBNA1 or LANA. We also determined the high-resolution crystal structure of one fragment bound to EBNA1. Results from this screening cascade provide new chem. starting points for the further development of potent inhibitors for this class of viral proteins.

Molecules published new progress about Affinity. 86129-63-7 belongs to class pyridine-derivatives, and the molecular formula is C9H9Cl2NO2, Synthetic Route of 86129-63-7.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Electric Literature of 86129-63-7, Adding some certain compound to certain chemical reactions, such as: 86129-63-7, name is Ethyl 2,4-dichloro-6-methyl-3-pyridinecarboxylate,molecular formula is C9H9Cl2NO2, can increase the reaction rate and produce products with better performance than those obtained under traditional synthetic methods. Here is a downstream synthesis route of the compound 86129-63-7.

To a solution of intermediate 33 (9.73 g, 1.5 eq) in anh. DMF (150 mL), at r. t. , under N2, was added NaH 60%/OIL (1.7 g, 1 eq) and the reaction mixture was stirred at r. t. for 20 min. A solution of ethyl 2, 4-dichloro-6-methyl-3-pyridinecarboxylate (10 g, 42.9 MMOL) was then added dropwise and the reaction mixture was stirred at 80oC for 4 hr. It was then cooled down to r. t. and quenched with ice water. The addition of EtOAc caused a precipitate to form. The white solid was collected by filtration, washed with water and dried in vacuo (5.2 g). The filtrate was transferred into a separatory funnel and the aqueous layer was extracted with EtOAc (2X100 mL). The combined organic layers were washed with sat. aq. NACI, dried over anh. NA2SO4, the solids were filtered and the solvent evaporated. The crude product was treated with EtOAc and left at r. t. overnight. The precipitate was filtrated, dried in vacuo and combined with the previous batch to give the title compound as a white solid (7.2 g, 48%). NMR (‘H, DMSO-D6) : 5 8.53 (d, 1H), 7.77 (s, 1H), 7.18 (bs, 1H), 6.89 (d, 1H), 4.32 (q, 2H), 3.75 (t, 2H), 3.42 (t, 2H), 3.31 (s, 3H), 1.26 (t, 3H). MS (M/Z) : 350 [MH] +.

In the field of chemistry, the synthetic routes of compounds are constantly being developed and updated. I will also mention this compound in other articles. 86129-63-7, Ethyl 2,4-dichloro-6-methyl-3-pyridinecarboxylate, other downstream synthetic routes, hurry up and to see.

Reference:
Patent; SB PHARMCO PUERTO RICO INC; NEUROCRINE BIOSCIENCES INC; WO2004/94419; (2004); A1;,
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem