Tag: M.W=200-250

Rong, Jian published the artcileNovel Reversible-Binding PET Ligands for Imaging Monoacylglycerol Lipase Based on the Piperazinyl Azetidine Scaffold, Recommanded Product: 2-Fluoro-4-iodo-6-methylpyridine, the main research area is piperazinyl azetidine PET ligand preparation imaging monoacylglycerol lipase.

Monoacylglycerol lipase (MAGL) is a 33 kDa serine protease primarily responsible for hydrolyzing 2-arachidonoylglycerol into the proinflammatory eicosanoid precursor arachidonic acid in the central nervous system. Inhibition of MAGL constitutes an attractive therapeutic concept for treating psychiatric disorders and neurodegenerative diseases. Herein, we present the design and synthesis of multiple reversible MAGL inhibitor candidates based on a piperazinyl azetidine scaffold. Compounds 10 and 15 were identified as the best-performing reversible MAGL inhibitors by pharmacol. evaluations, thus channeling their radiolabeling with fluorine-18 in high radiochem. yields and favorable molar activity. Furthermore, evaluation of [18F]10 and [18F]15 ([18F]MAGL-2102) by autoradiog. and positron emission tomog. (PET) imaging in rodents and nonhuman primates demonstrated favorable brain uptakes, heterogeneous radioactivity distribution, good specific binding, and adequate brain kinetics, and [18F]15 demonstrated a better performance. In conclusion, [18F]15 was found to be a suitable PET radioligand for the visualization of MAGL, harboring potential for the successful translation into humans.

Journal of Medicinal Chemistry published new progress about Homo sapiens. 884494-45-5 belongs to class iodides-buliding-blocks, name is 2-Fluoro-4-iodo-6-methylpyridine, and the molecular formula is C6H5FIN, Recommanded Product: 2-Fluoro-4-iodo-6-methylpyridine.

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

Huang, Jingjia published the artcileSynthesis of N-Alkylpyridin-4-ones and Thiazolo[3,2-a]pyridin-5-ones through Pummerer-Type Reactions, Category: iodides-buliding-blocks, the main research area is alkylpyridinone thiazolopyridinone preparation Pummerer.

N-Alkylated 4-pyridones were obtained through a one-pot procedure involving either normal or interrupted Pummerer reactions between triflic anhydride-activated sulfoxides and 4-fluoropyridine derivatives, followed by hydrolysis. However, triflic anhydride-activated benzyl 6-fluoro-2-pyridyl sulfoxide could react with alkenes or alkynes to afford thiazolo[3,2-a]pyridin-5-ones, via the pyridinium salt intermediates.

Journal of Organic Chemistry published new progress about Hydrolysis. 685517-67-3 belongs to class iodides-buliding-blocks, name is 2,6-Difluoro-3-iodopyridine, and the molecular formula is C5H2F2IN, Category: iodides-buliding-blocks.

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

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

Hedidi, Madani published the artcileDeprotometalation of substituted pyridines and regioselectivity-computed CH acidity relationships, Recommanded Product: 2,6-Difluoro-3-iodopyridine, the main research area is pyridine deprotometalation regioselectivity CH acidity relationship DFT B3LYP G3MP2B3.

A series of methoxy- and fluoro-pyridines have been deprotometalated in THF at room temperature by using a mixed lithium-zinc combination obtained from ZnCl2·TMEDA (TMEDA=N,N,N’,N’-tetramethylethylenediamine) and LiTMP (TMP=2,2,6,6-tetramethylpiperidino) in a 1:3 ratio, and the metalated species intercepted by iodine. Efficient functionalization at the 3 position was observed from 4-methoxy, 2-methoxy, 2,6-dimethoxy, 2-fluoro and 2,6-difluoropyridine, and at the 4 position from 3-methoxy and 2,3-dimethoxypyridine. Interestingly, clean dideprotonation was noted from 3-fluoropyridine (at C2 and C4) and 2,6-difluoropyridine (at C3 and C5). The obtained regioselectivities have been discussed in light of the CH acidities of the substrates, determined both in the gas phase (DFT B3LYP and G3MP2B3 levels) and in THF solution In the case of methoxypyridines, the pKa values have also been calculated for complexes with LiCl and LiTMP.

Tetrahedron published new progress about Acidity. 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

Schlosser, Manfred published the artcileThe structural proliferation of 2,6-difluoropyridine through organometallic intermediates, Quality Control of 685517-67-3, the main research area is difluoropyridine reaction; pyridine difluoro reaction.

Contrary to a literature claim, 2,6-difluoropyridine-3-carboxaldehyde can be readily prepared by consecutive treatment of 2,6-difluoropyridine with lithium diisopropylamide and N,N-dimethylformamide. Regioselective displacements of fluorine from the aldehyde by nucleophiles were carried out. To demonstrate the versatility of the organometallic approach, some two dozens of further 2,6-difluoropyridine derivatives were prepared applying a combination of modern organometallic methods such as site selective hydrogen/metal and halogen/metal permutations and deprotonation-triggered heavy halogen migrations.

European Journal of Organic Chemistry published new progress about difluoropyridine reaction; pyridine difluoro reaction. 685517-67-3 belongs to class iodides-buliding-blocks, name is 2,6-Difluoro-3-iodopyridine, and the molecular formula is C5H2F2IN, Quality Control of 685517-67-3.

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

Ren, Li published the artcileDiscovery of Highly Potent, Selective, and Efficacious Small Molecule Inhibitors of ERK1/2, Safety of 2-Fluoro-4-iodo-6-methylpyridine, the main research area is pyridone ERK inhibitor pharmacokinetics.

Using structure-based design, a novel series of pyridone ERK1/2 inhibitors was developed. Optimization led to the identification of I, a potent, selective, and orally bioavailable agent that inhibited tumor growth in mouse xenograft models. On the basis of its in vivo efficacy and preliminary safety profiles, I was selected for further preclin. evaluation.

Journal of Medicinal Chemistry published new progress about Antitumor agents. 884494-45-5 belongs to class iodides-buliding-blocks, name is 2-Fluoro-4-iodo-6-methylpyridine, and the molecular formula is C6H5FIN, Safety of 2-Fluoro-4-iodo-6-methylpyridine.

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

Montgomery, Justin I. published the artcilePyridone methylsulfone hydroxamate LpxC inhibitors for the treatment of serious gram-negative infections, Formula: C6H5FIN, the main research area is pyridone methylsulfone hydroxamate LpxC inhibitor treatment gram neg infection.

The synthesis and biol. activity of a new series of LpxC inhibitors represented by pyridone methylsulfone hydroxamate 2a (I) is presented. Members of this series have improved solubility and free fraction when compared to compounds in the previously described biphenyl methylsulfone hydroxamate series, and they maintain superior Gram-neg. antibacterial activity to comparator agents.

Journal of Medicinal Chemistry published new progress about Acinetobacter. 884494-45-5 belongs to class iodides-buliding-blocks, name is 2-Fluoro-4-iodo-6-methylpyridine, and the molecular formula is C6H5FIN, Formula: C6H5FIN.

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

Jin, Xin published the artcilePinning-down molecules in self-assemblies with multiple weak hydrogen bonds of C-H···F and C-H···N, Application In Synthesis of 685517-67-3, the main research area is mol self assembly hydrogen bond.

Two-dimensional self-assemblies of four partially fluorinated mols., 1,4-bis(2,6-difluoropyridin-4-yl)benzene, 4,4′-bis(2,6-difluoropyridin-4-yl)-1,1′-biphenyl, 4,4′-bis(2,6-difluoropyridin-4-yl)-1,1′:4′,1”-terphenyl and 4,4′-bis(2,6-difluoropyridin-3-yl)-1,1′-biphenyl, involving weak intermol. C-H···F and C-H···N hydrogen bonds were systematically investigated on Au(111) with low-temperature scanning tunneling microscopy. The inter-mol. connecting modes and binding sites were closely related to the backbones of the building blocks, i.e., the mol. length determines its binding sites with neighboring mols. in the assemblies while the attaching positions of the N and F atoms dictate its approaching and docking angles. The exptl. results demonstrate that multiple weak hydrogen bonds such as C-H···F and C-H···N can be efficiently applied to tune the mol. orientations and the self-assembly structures accordingly.

Chinese Chemical Letters published new progress about Hydrogen bond. 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