Category: 153034-78-7

Li, Yibiao published the artcileAccess to 2-pyridinylamide and imidazopyridine from 2-fluoropyridine and amidine hydrochloride, Computed Properties of 153034-78-7, the main research area is pyridinylamide preparation; fluoropyridine amidation amidine hydrochloride chemoselective; imidazopyridine preparation chemoselective regioselective.

Under catalyst-free conditions, an efficient method to synthesize 2-pyridinylamides has been developed, and the protocol uses inexpensive and readily available 2-fluoropyridines and amidine derivatives as the starting materials. Simultaneously, the copper-catalyzed approach to imidazopyridine derivatives has been established with high chemoselectivity and regiospecificity. The results suggest that the nitrogen-heterocycles containing iodide substituents can also be compatible for the reaction via the cascade Ullmann-type coupling, and the nucleophilic substitution reaction provides the target products in a one-pot manner.

Organic & Biomolecular Chemistry published new progress about Amidation. 153034-78-7 belongs to class iodides-buliding-blocks, name is 2-Fluoro-3-iodo-5-methylpyridine, and the molecular formula is C6H5FIN, Computed Properties of 153034-78-7.

Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com

Mineno, Masahiro published the artcileIntegrated Cross-Coupling Strategy for an α-Carboline-Based Aurora B Kinase Inhibitor, Quality Control of 153034-78-7, the main research area is ethylsulfonylphenyldimethylmethylpiperidinylpyridoindolecarboxamide preparation Aurora B kinase inhibitor; aniline Buchwald Hartwig amination arylation Suzuki coupling Sandmeyer iodination.

An efficient and practical synthetic process for an α-carboline-based Aurora B kinase inhibitor I was achieved using an integrated Pd-catalyzed cross-coupling strategy. The process features a mild and efficient method for construction of the α-carboline core by employing a Pd-catalyzed sequence of Buchwald-Hartwig amination and intramol. direct C-H arylation at the ortho position of an unsubstituted aniline moiety, which is a key functionality for further derivatization with a Suzuki coupling via Sandmeyer iodination. The process has eliminated expensive starting materials and column chromatog. purifications and enabled considerable enhancement of the total yield from 11% to 48%.

Journal of Organic Chemistry published new progress about Arylation. 153034-78-7 belongs to class iodides-buliding-blocks, name is 2-Fluoro-3-iodo-5-methylpyridine, and the molecular formula is C6H5FIN, Quality Control of 153034-78-7.

Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com

Wang, Le published the artcileSynthesis of 1H-pyridin-2-one derivatives as potent and selective farnesyltransferase inhibitors, SDS of cas: 153034-78-7, the main research area is farnesyltransferase protein cysteine inhibitor imidazole pyridinyl benzonitrile pyridinecarbonitrile bioisostere; crystal mol structure methyl oxo trifluoromethylphenyl pyridinecarbonitrile preparation.

The synthesis and biol. evaluation of two novel series of potent and selective FTase inhibitors are described. Thus, 4-[[[4-(3-chlorophenyl)-1-[(3-cyanophenyl)methyl]-6-oxo-1,6-dihydro-3-pyridinyl]methoxy](1-methyl-1H-imidazol-5-yl)methyl]benzonitrile (I) was prepared and found to possess potent whole-cell activity in addition to good oral availability in dogs. The crystal structure of an intermediate dimethyl(oxo)[(trifluoromethyl)phenyl]pyridinecarbonitrile was reported. The selectivity of the compounds prepared for this study toward protein (cysteine) farnesyltransferase over protein (cysteine) geranylgeranyltransferase (GGTase-I) was pointed out.

Bioorganic & Medicinal Chemistry Letters published new progress about Crystal structure. 153034-78-7 belongs to class iodides-buliding-blocks, name is 2-Fluoro-3-iodo-5-methylpyridine, and the molecular formula is C6H5FIN, SDS of cas: 153034-78-7.

Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com

Billaud, Emilie M. F. published the artcileSynthesis, radiolabeling and preliminary in vivo evaluation of multimodal radiotracers for PET imaging and targeted radionuclide therapy of pigmented melanoma, Formula: C6H5FIN, the main research area is radiolabeling radiotracer preparation PET imaging radiotherapy melanoma; Fluorine-18; In vivo screening; Iodine-125; Melanoma; PET imaging.

Melanin pigment represents an attractive target to address specific treatment to melanoma cells, such as cytotoxic radionuclides. However, less than half of the patients have pigmented metastases. Hence, specific marker is required to stratify this patient population before proceeding with melanin-targeted radionuclide therapy. In such a context, we developed fluorinated analogs of a previously studied melanin-targeting ligand, N-(2-diethylaminoethyl)-6-iodoquinoxaline-2-carboxamide (ICF01012). These latter can be labeled either with 18F or 131I/125I for positron emission tomog. imaging (melanin-pos. patient selection) and targeted radionuclide therapy purposes. Here we describe the syntheses, radiosyntheses and preclin. evaluations on melanoma-bearing mice model of several iodo- and fluoro(hetero)aromatic derivatives of the ICF01012 scaffold. After preliminary planar gamma scintigraphic and positron emission tomog. imaging evaluations, [125I]- and [18F]-N-[2-(diethylamino)ethyl]-4-fluoro-3-iodobenzamides ([125I]4, [18F]4) were chem. and biol. stable with quite similar tumor uptakes at 1 h p.i. (9.7±2.6% ID/g and 6.8±1.9% ID/g, resp.).

European Journal of Medicinal Chemistry published new progress about Antitumor agents. 153034-78-7 belongs to class iodides-buliding-blocks, name is 2-Fluoro-3-iodo-5-methylpyridine, and the molecular formula is C6H5FIN, Formula: C6H5FIN.

Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com

Christiansen, Elisabeth published the artcileIdentification of a Potent and Selective Free Fatty Acid Receptor 1 (FFA1/GPR40) Agonist with Favorable Physicochemical and in Vitro ADME Properties, Related Products of iodides-buliding-blocks, the main research area is FFA1 GPR40 receptor preparation structure ADME diabetes.

The free fatty acid receptor 1 (FFA1, also known as GPR40) enhances glucose-stimulated insulin secretion from pancreatic β-cells and is recognized as an interesting new target for treatment of type 2 diabetes. Several series of selective FFA1 agonists are already known. Most of these are derived from free fatty acids (FFAs) or glitazones and are relatively lipophilic. Aiming for the development of potent, selective, and less lipophilic FFA1 agonists, the terminal Ph of a known compound series was replaced by nitrogen containing heterocycles. This resulted in the identification of 37, a selective FFA1 agonist with potent activity on recombinant human FFA1 receptors and on the rat insulinoma cell line INS-1E, optimal lipophilicity, and excellent in vitro permeability and metabolic stability.

Journal of Medicinal Chemistry published new progress about Antidiabetic agents. 153034-78-7 belongs to class iodides-buliding-blocks, name is 2-Fluoro-3-iodo-5-methylpyridine, and the molecular formula is C6H5FIN, Related Products of iodides-buliding-blocks.

Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com

Rocca, P. published the artcileFirst metalation of aryl iodides: directed ortho-lithiation of iodopyridines, halogen-dance, and application to synthesis, Category: iodides-buliding-blocks, the main research area is metalation iodopyridine regiochem rearrangement; ortho lithiation iodopyridine regiochem rearrangement; aryl iodide metalation regiochem rearrangement; perlolidine preparation; diazaphenanthrene preparation; carboline preparation.

Metalation of iodopyridines was successfully achieved by LDA at low temperature In many cases, lithiation is ortho directed by the iodo group which subsequently ortho-migrates very fast to give stabilized iodolithiopyridines. This procedure was applied to 2-fluoro- and 2-chloro-3-iodopyridines, 3-fluoro-4-iodopyridine, and 2-chloro-3-fluoro-4-iodopyridine. The resulting lithio intermediates were obtained in high yields before being reacted with electrophiles leading to various polysubstituted pyridines. Some of these iodopyridines were used as key mols. for the preparation of fused polyaromatic alkaloids. Thus, perlolidine (I), δ-carbolines, and 2,10-diazaphenanthrenes were readily prepared in few steps taking advantage of the iodo reactivity for heteroring cross-coupling. Coupling of [2-(pivaloylamino)phenyl]boronic acid with 2-fluoro-4-iodo-3-pyridinecarboxaldehyde gave I.

Journal of Organic Chemistry published new progress about Cross-coupling reaction. 153034-78-7 belongs to class iodides-buliding-blocks, name is 2-Fluoro-3-iodo-5-methylpyridine, and the molecular formula is C6H5FIN, Category: iodides-buliding-blocks.

Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com

Cai, Jialing published the artcileAccess to functionalized thienopyridines via a reagent-capsule-assisted coupling, thiolation and cyclization cascade sequence, Safety of 2-Fluoro-3-iodo-5-methylpyridine, the main research area is thienopyridine furopyridine green preparation; iodopyridine terminal alkyne reagent capsule cascade coupling thiolation cyclization.

Synthesis of functionalized thienopyridines e.g., I [R1 = H, 5-Me, 5-Cl; R2 = Ph, 3-thienyl, cyclopentyl, etc.] via palladium-catalyzed cross-coupling of ortho-fluorinated iodopyridines and terminal alkynes, followed by a reagent-capsule-assisted thiolation and cyclization sequence was reported. The use of paraffin wax capsules prevented catalyst poisoning and undesired side reactions and the separation and purification processes were also reduced. This coupling and cyclization method displayed broad substrate scope, good tolerance of functional groups and gives moderate to good yields under mild conditions. Further, 2-arylfuro[2,3-b]pyridines were also prepared by using this methodol.

Organic & Biomolecular Chemistry published new progress about Alkynes, α- Role: RCT (Reactant), RACT (Reactant or Reagent). 153034-78-7 belongs to class iodides-buliding-blocks, name is 2-Fluoro-3-iodo-5-methylpyridine, and the molecular formula is C6H5FIN, Safety of 2-Fluoro-3-iodo-5-methylpyridine.

Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com

Li, Yibiao published the artcile2-Acetylthienopyridine Synthesis via Thiolation and Copper-Catalyzed Cyclization of o-Propynol Fluoropyridine Using Xanthate as a Thiol Surrogate, SDS of cas: 153034-78-7, the main research area is fluoropyridinylalkynol xanthate thiolation cyclization oxidation copper; thienopyridine preparation; copper thiolation cyclization oxidation catalyst.

2-Acylthienopyridines and related heterocycles are readily prepared in moderate to good yields under mild conditions by a nucleophilic thiolation, copper-catalyzed cyclization, and an oxidation cascade process using potassium xanthate as the thiol source. Moreover, excellent chemoselectivity, broad substrate scope, and good functional group tolerance are prominent features of this transformation.

Journal of Organic Chemistry published new progress about Cyclization. 153034-78-7 belongs to class iodides-buliding-blocks, name is 2-Fluoro-3-iodo-5-methylpyridine, and the molecular formula is C6H5FIN, SDS of cas: 153034-78-7.

Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com

Li, Yibiao published the artcile2-Acetylthienopyridine Synthesis via Thiolation and Copper-Catalyzed Cyclization of o-Propynol Fluoropyridine Using Xanthate as a Thiol Surrogate, SDS of cas: 153034-78-7, the main research area is fluoropyridinylalkynol xanthate thiolation cyclization oxidation copper; thienopyridine preparation; copper thiolation cyclization oxidation catalyst.

2-Acylthienopyridines and related heterocycles are readily prepared in moderate to good yields under mild conditions by a nucleophilic thiolation, copper-catalyzed cyclization, and an oxidation cascade process using potassium xanthate as the thiol source. Moreover, excellent chemoselectivity, broad substrate scope, and good functional group tolerance are prominent features of this transformation.

Journal of Organic Chemistry published new progress about Cyclization. 153034-78-7 belongs to class iodides-buliding-blocks, name is 2-Fluoro-3-iodo-5-methylpyridine, and the molecular formula is C6H5FIN, SDS of cas: 153034-78-7.

Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com