Tag: M.W=200-250

Katoh, Taisuke published the artcileFacile preparation of 3-substituted-2,6-difluoropyridines: application to the synthesis of 2,3,6-trisubstituted pyridines, Application In Synthesis of 685517-67-3, the main research area is substituted pyridine preparation; halopyridine fluorination nucleophilic substitution.

We report a facile method for the difluorination of 3-substituted-2,6-dichloropyridines using cesium fluoride as a fluorination reagent in DMSO. It is proposed that this method for preparing 3-substituted-2,6-difluoropyridines is simpler and easier than those reported in previous literature. To examine the utility of 3-substituted-2,6-difluoropyridines in synthetic chem., we also demonstrate a subsequent conversion to 2,3,6-trisubstituted pyridines by a tandem nucleophilic aromatic substitution.

Tetrahedron Letters published new progress about Fluorination. 685517-67-3 belongs to class iodides-buliding-blocks, name is 2,6-Difluoro-3-iodopyridine, and the molecular formula is C5H2F2IN, Application In Synthesis of 685517-67-3.

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

Cheng, Dachen published the artcileSynthetic Entries to Substituted Bicyclic Pyridones, Product Details of C5H2F2IN, the main research area is bicyclic pyridone synthesis; Mitsunobu cyclodehydration bicyclic pyridone synthesis; Suzuki coupling bicyclic pyridone synthesis; imidazopyridinone pyridopyrimidinone pyridodiazepinone synthesis.

The synthesis of 6,6- and 5,6-bicyclic pyridone scaffolds (e.g. 2,3-dihydro-1-benzylimidazo[1,2-a]pyridin-5-one, 1,2,3,4-tetrahydro-6H-pyrido[1,2-a]pyrimidin-6-one and 1-benzyl-2,3,4,5-tetrahydropyrido[1,2-a][1,3]diazepin-7-one) was completed using (i) an intramol. Mitsunobu reaction and/or (ii) hydrolysis of a bicyclic pyridinium salt intermediate. Regioselective functionalization of the pyridone ring was achieved via either direct lithiation or use of the halogen dance reaction. Suzuki coupling then allows introduction of aryl units at C(7)/C(9) or C(8) onto the bicyclic pyridone scaffold at either an early or late stage in the synthetic sequence. Suzuki couplings involving iodopyridinium intermediates are particularly effective.

Organic Letters published new progress about Cyclocondensation reaction, intramolecular (Mitsunobu). 685517-67-3 belongs to class iodides-buliding-blocks, name is 2,6-Difluoro-3-iodopyridine, and the molecular formula is C5H2F2IN, Product Details of C5H2F2IN.

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

Chen, Qiwei published the artcileSteering On-Surface Reactions by a Self-Assembly Approach, SDS of cas: 685517-67-3, the main research area is on surface synthesis functional nanostructure preparation; difluoropyridnyl terphenyl self assembly mediated reaction gold surface; scanning tunneling microscopy assessment self assembly reaction gold surface; density functional theory calculation self assembly reaction gold surface; self assembly reaction gold surface scanning tunneling microscopy; dehydrocyclization coupling reaction difluoropyridnyl terphenyl gold surface; dehydrocyclization; density functional theory; on-surface reaction; scanning tunneling microscope; self-assembly.

4,4′-Bis(2,6-difluoropyridin-4-yl)-1,1′:4′,1”-terphenyl (BDFPTP) mols. underwent dehydrocyclization and covalent coupling reactions on Au(111) according to scanning tunneling microscopy measurements and d. functional theory calculations Self-assembly of the reactants in well-defined mol. domains prior to reaction greatly enhances the regio-selectivity of the dehydrocyclization reaction and suppressed defluorinated coupling, demonstrating that self-assembly can efficiently steer on-surface reactions. Such a strategy could be greatly important for surface chem. and widely used to control on-surface reactions.

Angewandte Chemie, International Edition published new progress about Coupling reaction (defluorinated). 685517-67-3 belongs to class iodides-buliding-blocks, name is 2,6-Difluoro-3-iodopyridine, and the molecular formula is C5H2F2IN, SDS of cas: 685517-67-3.

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

Awad, Hacan published the artcileDeprotonation of fluoro aromatics using lithium magnesates, Recommanded Product: 2,6-Difluoro-3-iodopyridine, the main research area is deprotonation fluoro aromatic lithium magnesate.

3-Fluoropyridine was deprotonated on treatment with 1/3 equiv of Bu3MgLi in THF at -10 °C. The lithium arylmagnesate formed was either trapped with electrophiles or involved in a palladium-catalyzed cross-coupling reaction with 2-bromopyridine. The use of a less nucleophilic lithium-magnesium-dialkylamide, (TMP)3MgLi (TMP = 2,2,6,6-tetramethylpiperidino) allowed the reaction of 3-fluoroquinoline, giving the 2,2′-dimeric derivative 2-Fluoropyridine and 2,6-difluoropyridine were deprotonated using 1/3 equiv of the highly coordinated magnesate Bu4MgLi2 in THF at -10 °C in the presence of a substoichiometric amount of 2,2,6,6-tetramethylpiperidine. 1,3-Difluorobenzene reacted similarly when treated with Bu3MgLi; the reactivity of the base proved to be enhanced by the presence of TMEDA.

Tetrahedron Letters published new progress about Aryl fluorides Role: RCT (Reactant), RACT (Reactant or Reagent). 685517-67-3 belongs to class iodides-buliding-blocks, name is 2,6-Difluoro-3-iodopyridine, and the molecular formula is C5H2F2IN, Recommanded Product: 2,6-Difluoro-3-iodopyridine.

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

Xiao, Li-Jun published the artcilePdII-Catalyzed Enantioselective C(sp3)-H Arylation of Cyclobutyl Ketones Using a Chiral Transient Directing Group, COA of Formula: C5H2F2IN, the main research area is arylcyclobutyl ketone regioselective diastereoselective enantioselective preparation; palladium catalyst stereoselective arylation cyclobutyl ketone transient directing group; C−H activation; arylation; palladium; pyridone ligands; transient directing groups.

In the presence of Pd(OAc)2, 3-nitro-5-trifluoromethyl-2-pyridone, and D-valine as a transient directing group reagent, cyclobutyl ketones such as I (R = H) underwent regioselective, diastereoselective, and enantioselective arylation with aryl iodides R1I (R1 = 4-MeO2CC6H4, 4-O2NC6H4, 4-MeCOC6H4, 4-NCC6H4, 4-F3CC6H4, 3-O2NC6H4, 3-PhCOC6H4, 3,4,5-F3C6H2, 3,5-Br2C6H3, 3-Br-5-ClC6H3, 4-Me-3-O2NC6H3, 2-Br-5-FC6H3, 6-F-3-pyridinyl, 2-F3C-4-pyridinyl, 6-Cl-5-F3C-3-pyridinyl, 6-Br-3-pyridinyl, 2,6-F2-4-pyridinyl, 2,6-F2-3-pyridinyl, 2,6-Cl2-4-pyridinyl, 5-acetyl-2-thienyl) to yield arylcyclobutyl ketones such as I (R = 4-MeO2CC6H4, 4-O2NC6H4, 4-MeCOC6H4, 4-NCC6H4, 4-F3CC6H4, 3-O2NC6H4, 3-PhCOC6H4, 3,4,5-F3C6H2, 3,5-Br2C6H3, 3-Br-5-ClC6H3, 4-Me-3-O2NC6H3, 2-Br-5-FC6H3, 6-F-3-pyridinyl, 2-F3C-4-pyridinyl, 6-Cl-5-F3C-3-pyridinyl, 6-Br-3-pyridinyl, 2,6-F2-4-pyridinyl, 2,6-F2-3-pyridinyl, 2,6-Cl2-4-pyridinyl, 5-acetyl-2-thienyl). In the presence of either L-valine as a transient directing group reagent or when silver trifluoroacetate, acetate, carbonate, or oxide were used as bases, enantiomeric arylcyclobutyl ketones were formed. A sequential diarylation was performed to yield diastereomeric diarylcyclobutyl ketones enantioselectively.

Angewandte Chemie, International Edition published new progress about Aryl iodides Role: RCT (Reactant), RACT (Reactant or Reagent). 685517-67-3 belongs to class iodides-buliding-blocks, name is 2,6-Difluoro-3-iodopyridine, and the molecular formula is C5H2F2IN, COA of Formula: C5H2F2IN.

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