Category: 1827-27-6

Most of the compounds have physiologically active properties, and their biological properties are often attributed to the heteroatoms contained in their molecules, and most of these heteroatoms also appear in cyclic structures. A Journal, Article, Research Support, N.I.H., Extramural, Research Support, Non-U.S. Gov’t, Bioorganic & Medicinal Chemistry Letters called Synthesis and evaluation of radiolabeled AGI-5198 analogues as candidate radiotracers for imaging mutant IDH1 expression in tumors, Author is Chitneni, Satish K.; Reitman, Zachary J.; Spicehandler, Rebecca; Gooden, David M.; Yan, Hai; Zalutsky, Michael R., which mentions a compound: 1827-27-6, SMILESS is NC1=CN=C(C=C1)F, Molecular C5H5FN2, Application of 1827-27-6.

Mutations in the metabolic enzyme isocitrate dehydrogenase 1 (IDH1) are commonly found in gliomas. AGI-5198, a potent and selective inhibitor of the mutant IDH1 enzyme, was radiolabeled with radioiodine and fluorine-18. These radiotracers were evaluated as potential probes for imaging mutant IDH1 expression in tumors with positron emission tomog. (PET). Radioiodination of AGI-5198 was achieved using a tin precursor in 79±6% yield (n=9), and 18F-labeling was accomplished by the Ugi reaction in a decay-corrected radiochem. yield of 2.6±1.6% (n=5). The inhibitory potency of the analogous nonradioactive compounds against mutant IDH1 (IDH1-R132H) was determined in enzymic assays. Cell uptake studies using radiolabeled AGI-5198 analogs revealed somewhat higher uptake in IDH1-mutated cells than that in wild-type IDH1 cells. The radiolabeled compounds displayed favorable tissue distribution characteristics in vivo, and good initial uptake in IDH1-mutated tumor xenografts; however, tumor uptake decreased with time. Radioiodinated AGI-5198 exhibited higher tumor-to-background ratios compared with 18F-labeled AGI-5198; unfortunately, similar results were observed in wild-type IDH1 tumor xenografts as well, indicating lack of selectivity for mutant IDH1 for this tracer. These results suggest that AGI-5198 analogs are not a promising platform for radiotracer development. Nonetheless, insights gained from this study may help in design and optimization of novel chem. scaffolds for developing radiotracers for imaging the mutant IDH1 enzyme.

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The reaction of an aromatic heterocycle with a proton is called a protonation. One of articles about this theory is 《Aromatic fluorine compounds. X. The 2,3- and 2,6-difluoropyridines》. Authors are Finger, G. C.; Starr, Laurence D.; Roe, Arthur; Link, William J..The article about the compound:5-Amino-2-fluoropyridinecas:1827-27-6,SMILESS:NC1=CN=C(C=C1)F).Recommanded Product: 5-Amino-2-fluoropyridine. Through the article, more information about this compound (cas:1827-27-6) is conveyed.

cf. CA 54, 6713i. The preparation of difluoropyridines by the Schiemann reaction was investigated. 2-Amino-6-fluoropyridine, necessary for the synthesis of 2,6-difluoropyridine by the Schiemann reaction, was conveniently prepared by the Curtius degradation of 6-fluoropicolinic hydrazide and by the Hofmann reaction on 6-fluoropicolinamide. Since an α-fluorine on a pyridine nucleus is preferentially replaced by hydrazine when it is either adjacent to or opposite a carbomethoxy group, the hydrazides necessary for the synthesis of 3-amino-2- and 6-fluoropyridine could not be prepared These amines were prepared from the appropriate 2-fluoropyridinecarboxamide by the Hofmann reaction. The preparation of difluoropyridines was successful with two of the aminofluoropyridines and led to the following new compounds: 2,3-difluoro- and 2,6-difluoropyridine.

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Product Details of 1827-27-6. Aromatic compounds can be divided into two categories: single heterocycles and fused heterocycles. Compound: 5-Amino-2-fluoropyridine, is researched, Molecular C5H5FN2, CAS is 1827-27-6, about 5-Azido-2-aminopyridine, a New Nitrene/Nitrenium Ion Photoaffinity Labeling Agent That Exhibits Reversible Intersystem Crossing between Singlet and Triplet Nitrenes. Author is Panov, Maxim S.; Voskresenska, Valentyna D.; Ryazantsev, Mikhail N.; Tarnovsky, Alexander N.; Wilson, R. Marshall.

The photochem. of a new photoaffinity labeling (PAL) agent, 5-azido-2-(N,N-diethylamino)-pyridine, was studied in aprotic and protic solvents using femtosecond-to-microsecond transient absorption and product anal., in conjunction with ab initio multiconfigurational and multireference quantum chem. calculations The excited singlet S1 state is spectroscopically dark, whereas photoexcitation to higher-lying singlet excited S2 and S3 states drives the photochem. reaction toward a barrierless ultrafast relaxation path via two conical intersections to S1, where N2 elimination leads to the formation of the closed-shell singlet nitrene. The singlet nitrene undergoes intersystem crossing (ISC) to the triplet nitrene in aprotic and protic solvents as well as protonation to form the nitrenium ion. The ISC rate constants in aprotic solvents increase with solvent polarity, displaying a “”direct”” gap effect, whereas an “”inverse”” gap effect is observed in protic solvents. Transient absorption actinometry experiments suggest that a solvent-dependent fraction from 20% to 50% of nitrenium ions is generated on a time scale of a few tens of picoseconds. The closed-shell singlet and triplet nitrene are separated by a small energy gap in protic solvents. As a result, the unreactive triplet state nitrene undergoes delayed, thermally activated reverse ISC to reform the reactive closed-shell singlet nitrene, which subsequently protonates, forming the remaining fraction of nitrenium ions. The product studies demonstrate that the resulting nitrenium ion stabilized by the electron-donating 4-amino group yields the final cross-linked product with high, almost quant. efficiency. The enhanced PAL function of this new azide with respect to the widely applied 4-amino-3-nitrophenyl azide is discussed.

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In general, if the atoms that make up the ring contain heteroatoms, such rings become heterocycles, and organic compounds containing heterocycles are called heterocyclic compounds. An article called Pyridyl-urea catalysts for the solvent-free ring-opening polymerization of lactones and trimethylene carbonate, published in 2019-12-31, which mentions a compound: 1827-27-6, Name is 5-Amino-2-fluoropyridine, Molecular C5H5FN2, Electric Literature of C5H5FN2.

The ring-opening polymerization (ROP) of lactones is an effective method for the preparation of biocompatible and biodegradable aliphatic polyesters, for which the development of efficient organocatalysts with high activity and good controllability is highly desirable. A series of novel pyridyl-urea catalysts was synthesized and applied in the solvent-free ROP of lactones and trimethylene carbonate. Combined with 7-methyl-1,5,7-triazabicyclo[4.4.0]dec-5-ene (MTBD), the pyridyl-urea/MTBD systems showed a fast and living/controlled behavior in the ROP, generating polymers with narrow mol. weight distributions. The influences of catalyst structure, type of base, pyridyl-urea/base ratio, feed ratio of monomer/initiator and reaction temperature on the catalytic properties were investigated. A possible mechanism was proposed on the basis of NMR titration and dilution experiments

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Electric Literature of C5H5FN2. The fused heterocycle is formed by combining a benzene ring with a single heterocycle, or two or more single heterocycles. Compound: 5-Amino-2-fluoropyridine, is researched, Molecular C5H5FN2, CAS is 1827-27-6, about Synthesis, biological evaluation and 3D-QSAR studies of 1,2,4-triazole-5-substituted carboxylic acid bioisosteres as uric acid transporter 1 (URAT1) inhibitors for the treatment of hyperuricemia associated with gout. Author is Wu, Jing-wei; Yin, Ling; Liu, Yu-qiang; Zhang, Huan; Xie, Ya-fei; Wang, Run-ling; Zhao, Gui-long.

Bromonaphthylmethyltriazolyl thioether lesinurad analogs and bioisosteres such as I were prepared as inhibitors of uric acid transporter 1 (URAT1) for potential use in treating hyperuricemia and gout. I inhibited URAT1 with an IC50 value of 32 nM, 225-fold lower than lesinurad. The pharmacophore for the lesinurad analogs was determined using a 3D-QSAR pharmacophore model; the hypothesis was validated by three methods (cost anal., Fisher’s randomization and leave-one-out).

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Reference of 5-Amino-2-fluoropyridine. So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic. Compound: 5-Amino-2-fluoropyridine, is researched, Molecular C5H5FN2, CAS is 1827-27-6, about Sulfonamide Synthesis via Calcium Triflimide Activation of Sulfonyl Fluorides.

A method using calcium triflimide [Ca(NTf2)2] as a Lewis acid to activate sulfonyl fluorides toward nucleophilic addition with amines is described. The reaction converts a wide array of sterically and electronically diverse sulfonyl fluorides and amines into the corresponding sulfonamides in good yield.

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The reaction of an aromatic heterocycle with a proton is called a protonation. One of articles about this theory is 《Synthesis, biological evaluation and 3D-QSAR studies of 1,2,4-triazole-5-substituted carboxylic acid bioisosteres as uric acid transporter 1 (URAT1) inhibitors for the treatment of hyperuricemia associated with gout》. Authors are Wu, Jing-wei; Yin, Ling; Liu, Yu-qiang; Zhang, Huan; Xie, Ya-fei; Wang, Run-ling; Zhao, Gui-long.The article about the compound:5-Amino-2-fluoropyridinecas:1827-27-6,SMILESS:NC1=CN=C(C=C1)F).Reference of 5-Amino-2-fluoropyridine. Through the article, more information about this compound (cas:1827-27-6) is conveyed.

Bromonaphthylmethyltriazolyl thioether lesinurad analogs and bioisosteres such as I were prepared as inhibitors of uric acid transporter 1 (URAT1) for potential use in treating hyperuricemia and gout. I inhibited URAT1 with an IC50 value of 32 nM, 225-fold lower than lesinurad. The pharmacophore for the lesinurad analogs was determined using a 3D-QSAR pharmacophore model; the hypothesis was validated by three methods (cost anal., Fisher’s randomization and leave-one-out).

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Recommanded Product: 1827-27-6. The mechanism of aromatic electrophilic substitution of aromatic heterocycles is consistent with that of benzene. Compound: 5-Amino-2-fluoropyridine, is researched, Molecular C5H5FN2, CAS is 1827-27-6, about Divergent Aminocarbonylations of Alkynes Enabled by Photoredox/Nickel Dual Catalysis. Author is Zhao, Xian; Feng, Xiaoliang; Chen, Fan; Zhu, Shengqing; Qing, Feng-Ling; Chu, Lingling.

A metallaphotoredox-catalyzed strategy for the selective and divergent aminocarbonylation of alkynes with amines and 1 atm of CO was reported. This synergistic protocol not only enables the Markovnikov-selective hydroaminocarbonylation of alkynes to afford α,β-unsaturated amides, but also facilitated a sequential four-component hydroaminocarbonylation/radical alkylation in the presence of tertiary and secondary alkyl boronate esters, which allowed for straightforward conversion of alkynes into corresponding amides. Preliminary mechanistic studied disclose that a photoinduced oxidative insertion of aniline and CO into nickel followed by a migratory insertion of (carbamoyl)nickel species was involved.

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In general, if the atoms that make up the ring contain heteroatoms, such rings become heterocycles, and organic compounds containing heterocycles are called heterocyclic compounds. An article called Asymmetric synthesis of heterocyclic chloroamines and aziridines by enantioselective protonation of catalytically generated enamines, published in 2021, which mentions a compound: 1827-27-6, Name is 5-Amino-2-fluoropyridine, Molecular C5H5FN2, Safety of 5-Amino-2-fluoropyridine.

We report a method for the synthesis of chiral vicinal chloroamines via asym. protonation of catalytically generated prochiral chloroenamines using chiral Bronsted acids. The process is highly enantioselective, with the origin of asymmetry and catalyst substituent effects elucidated by DFT calculations We show the utility of the method as an approach to the synthesis of a broad range of heterocycle-substituted aziridines by treatment of the chloroamines with base in a one-pot process, as well as the utility of the process to allow access to vicinal diamines.

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The preparation of ester heterocycles mostly uses heteroatoms as nucleophilic sites, which are achieved by intramolecular substitution or addition reactions. Compound: 5-Amino-2-fluoropyridine( cas:1827-27-6 ) is researched.Recommanded Product: 1827-27-6.Wu, Jing-wei; Yin, Ling; Liu, Yu-qiang; Zhang, Huan; Xie, Ya-fei; Wang, Run-ling; Zhao, Gui-long published the article 《Synthesis, biological evaluation and 3D-QSAR studies of 1,2,4-triazole-5-substituted carboxylic acid bioisosteres as uric acid transporter 1 (URAT1) inhibitors for the treatment of hyperuricemia associated with gout》 about this compound( cas:1827-27-6 ) in Bioorganic & Medicinal Chemistry Letters. Keywords: bromonaphthylmethyltriazolyl thioether preparation URAT1 inhibitor; structure bromonaphthylmethyltriazolyl thioether inhibition uric acid transporter; pharmacophore determination bromonaphthylmethyltriazolyl thioether URAT1 inhibition QSAR; 3D-QSAR; Bioisosteres; Biological evaluation; Gout; Synthesis. Let’s learn more about this compound (cas:1827-27-6).

Bromonaphthylmethyltriazolyl thioether lesinurad analogs and bioisosteres such as I were prepared as inhibitors of uric acid transporter 1 (URAT1) for potential use in treating hyperuricemia and gout. I inhibited URAT1 with an IC50 value of 32 nM, 225-fold lower than lesinurad. The pharmacophore for the lesinurad analogs was determined using a 3D-QSAR pharmacophore model; the hypothesis was validated by three methods (cost anal., Fisher’s randomization and leave-one-out).

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Pyrazine – Wikipedia,
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