Tag: 300-400

Discovery of Potent Irreversible Pan-Fibroblast Growth Factor Receptor (FGFR) Inhibitors was written by Wang, Yuming;Li, Lijun;Fan, Jun;Dai, Yang;Jiang, Alan;Geng, Meiyu;Ai, Jing;Duan, Wenhu. And the article was included in Journal of Medicinal Chemistry in 2018.Safety of 2,4-Dichloro-5-iodo-7H-pyrrolo[2,3-d]pyrimidine This article mentions the following:

Fibroblast growth factor receptors (FGFR1-4) are promising therapeutic targets in many cancers. With the resurgence of interest in irreversible inhibitors, efforts have been directed to the discovery of irreversible FGFR inhibitors. Currently, several selective irreversible inhibitors are being evaluated in clin. trials that could covalently target a conserved cysteine in the P-loop of FGFR. In this article, the authors used a structure-guided approach that is rationalized by a computer-aided simulation to discover the novel and irreversible pan-FGFR inhibitor, 9g ((S)-1-(3-(4-amino-5-(7-methoxy-5-methylbenzo[b]thien-2-yl)-7H-pyrrolo[2,3-d]pyrimidin-7-yl)pyrrolidin-1-yl)prop-2-en-1-one), which provided superior FGFR in vitro activities and decent selectivity over VEGFR2 (vascular endothelia growth factor receptor 2). In in vivo studies, 9g displayed clear antitumor activities in NCI-H1581 and SNU-16 xenograft mice models. Addnl., the diluting method confirmed the irreversible binding of 9g to FGFR. In the experiment, the researchers used many compounds, for example, 2,4-Dichloro-5-iodo-7H-pyrrolo[2,3-d]pyrimidine (cas: 1012785-51-1Safety of 2,4-Dichloro-5-iodo-7H-pyrrolo[2,3-d]pyrimidine).

2,4-Dichloro-5-iodo-7H-pyrrolo[2,3-d]pyrimidine (cas: 1012785-51-1) belongs to iodide derivatives. Organic iodides are organic compounds containing a carbon-iodine (C-I) bond. The carbon-iodine bond is weaker than other carbon-halogen bonds due to the poor electronegative nature of the iodine atom. Alkyl iodides react at a faster rate than alkyl fluorides due to the weak C-I bond.Safety of 2,4-Dichloro-5-iodo-7H-pyrrolo[2,3-d]pyrimidine

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

7-halogenated 7-deazapurine 2′-deoxyribonucleosides related to 2′-deoxyadenosine, 2′-deoxyxanthosine, and 2′-deoxyisoguanosine: syntheses and properties was written by Seela, Frank;Xu, Kuiying. And the article was included in Helvetica Chimica Acta in 2008.Related Products of 1012785-51-1 This article mentions the following:

A series of 7-fluorinated 7-deazapurine 2′-deoxyribonucleosides related to 2′-deoxyadenosine, 2′-deoxyxanthosine, and 2′-deoxyisoguanosine as well as intermediates, e.g. I, were synthesized. The 7-fluoro substituent was introduced in 2,6-dichloro-7-deaza-9H-purine with Selectfluor. Apart from 2,6-dichloro-7-fluoro-7-deaza-9H-purine, the 7-chloro compound was formed and used for the glycosylation reaction; the separation of the 7-fluoro from the 7-chloro compound was performed on the level of the unprotected nucleosides. Other halogen substituents were introduced with N-halogenosuccinimides. The 2′-deoxyisoguanosine derivative I was prepared from 2-chloro-7-fluoro-7-deaza-2′-deoxyadenosine via a photochem. induced nucleophilic displacement reaction. The pK_a values of the halogenated nucleosides were determined ¹³C-NMR chem.-shift dependencies of C(7), C(5), and C(8) were related to the electronegativity of the 7-halogen substituents. In aqueous solution, 7-halogenated 2′-deoxyribonucleosides show an approx. 70% S population. In the experiment, the researchers used many compounds, for example, 2,4-Dichloro-5-iodo-7H-pyrrolo[2,3-d]pyrimidine (cas: 1012785-51-1Related Products of 1012785-51-1).

2,4-Dichloro-5-iodo-7H-pyrrolo[2,3-d]pyrimidine (cas: 1012785-51-1) belongs to iodide derivatives. Organic iodides can be alkyl, alkenyl, or alkynyl, and all of them are very reactive toward with many kinds of nucleophiles. The C–I bond is the weakest of the carbon–halogen bonds. These bond strengths correlate with the electronegativity of the halogen, decreasing in the order F > Cl > Br > I. This periodic order also follows the atomic radius of halogens and the length of the carbon-halogen bond.Related Products of 1012785-51-1

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

Efficient iodination of aromatic compounds using potassium ferrate supported on montmorillonite was written by Keipour, Hoda;Khalilzadeh, Mohammad A.;Mohtat, Bita;Hosseini, Abolfazl;Zareyee, Daryoush. And the article was included in Chinese Chemical Letters in 2011.Application In Synthesis of 4,5-Diiodo-1H-imidazole This article mentions the following:

Potassium ferrate impregnated on montmorillonite is a mild, cheap, and non-toxic reagent for the iodination of phenols, including naphthol, aromatic amines, and heterocyclic substrates in fair to excellent yields by a simple isolation procedure. In the experiment, the researchers used many compounds, for example, 4,5-Diiodo-1H-imidazole (cas: 15813-09-9Application In Synthesis of 4,5-Diiodo-1H-imidazole).

4,5-Diiodo-1H-imidazole (cas: 15813-09-9) belongs to iodide derivatives. Organic iodides are organic compounds containing a carbon-iodine (C-I) bond. The carbon-iodine bond is weaker than other carbon-halogen bonds due to the poor electronegative nature of the iodine atom. Alkyl iodides react at a faster rate than alkyl fluorides due to the weak C-I bond.Application In Synthesis of 4,5-Diiodo-1H-imidazole

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

Synthesis and in vivo brain distribution of carbon-11-labeled δ-opioid receptor agonists was written by Pichika, Rama;Jewett, Douglas M.;Sherman, Philip S.;Traynor, John R.;Husbands, Stephen M.;Woods, James H.;Kilbourn, Michael R.. And the article was included in Nuclear Medicine and Biology in 2010.Application of 77350-52-8 This article mentions the following:

Three new radiolabeled compounds, [¹¹C]SNC80 ((+)-4-[(αR)-α-{(2S,5R)-4-allyl-2,5-dimethyl-1-piperazinyl}]-3-[¹¹C]methoxybenzyl-N,N-diethylbenzamide), N,N-diethyl-4-(3-methoxyphenyl-1-[¹¹C]methylpiperidin-4-ylidenemethyl)benzamide and N,N-diethyl-4-[(1-[¹¹C]methylpiperidin-4-ylidene)phenylmethyl]benzamide, were prepared as potential in vivo radiotracers for the δ-opioid receptor. Each compound was synthesized by alkylation of the appropriate desmethyl compounds using [¹¹C]methyl triflate. In vivo biodistribution studies in mice showed very low initial brain uptake of all three compounds and no regional specific binding for [¹¹C]SNC80. A monkey positron emission tomog. study of [¹¹C]SNC80 confirmed low brain permeability and uniform regional distribution of this class of opioid agonists in a higher species. Opioid receptor ligands of this structural class are thus unlikely to succeed as in vivo radiotracers, likely due to efficient exclusion from the brain by the P-glycoprotein efflux transporter. In the experiment, the researchers used many compounds, for example, N,N-Diethyl-4-iodobenzamide (cas: 77350-52-8Application of 77350-52-8).

N,N-Diethyl-4-iodobenzamide (cas: 77350-52-8) belongs to iodide derivatives. In general, organic iodides are light-sensitive and turn yellow during storage, owing to the formation of iodine. Organoiodine lubricants can be used with titanium, stainless steels, and other metals which tend to seize up with conventional lubricants: organoiodine lubricants can be used in turbines and spacecraft, and as a cutting oil in machining.Application of 77350-52-8

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

Efficient Copper-Catalyzed Trifluoromethylation of Aromatic and Heteroaromatic Iodides: The Beneficial Anchoring Effect of Borates was written by Gonda, Zsombor;Kovacs, Szabolcs;Weber, Csaba;Gati, Tamas;Meszaros, Attila;Kotschy, Andras;Novak, Zoltan. And the article was included in Organic Letters in 2014.Synthetic Route of C11H14INO This article mentions the following:

Efficient copper-catalyzed trifluoromethylation of aromatic iodides was achieved with TMSCF₃ in the presence of tri-Me borate. The Lewis acid was used to anchor the in situ generated trifluoromethyl anion and suppress its rapid decomposition Broad applicability of the new trifluoromethylating reaction was demonstrated in the functionalization of different aromatic and heteroaromatic iodides. In the experiment, the researchers used many compounds, for example, N,N-Diethyl-4-iodobenzamide (cas: 77350-52-8Synthetic Route of C11H14INO).

N,N-Diethyl-4-iodobenzamide (cas: 77350-52-8) belongs to iodide derivatives. Iodide-containing intermediates are common in organic synthesis, because of the easy formation and cleavage of the C–I bond. Iodo alkanes participate in a variety of organic synthesis reactions, which include the Simmons–Smith reaction (cyclopropanation using iodomethane), Williamson ether synthesis, Wittig reaction, Grignard reaction, alkyl coupling reactions, and Wurtz reaction.Synthetic Route of C11H14INO

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

Coupling of N-heterocycle-fused enyne aldehydes with γ,δ-unsaturated Fischer carbene complexes was written by Zhang, Jianwei;Zhang, Yanshi;Schnatter, Wayne F. K.;Herndon, James W.. And the article was included in Organometallics in 2006.HPLC of Formula: 15813-09-9 This article mentions the following:

The coupling of γ,δ-unsaturated Fischer carbene complexes, e.g. H₂C:CHCH₂CH₂C(OMe):Cr(CO)₅ with enyne aldehyde derivatives fused to indole, imidazole, and pyrazole ring systems, e.g. I (R¹ = Me₃Si, n-Bu; R² = PhCH₂, PhCHMe, ribofuranosyl; R³ = H, Me₃C, Ph), has been examined The reaction leads to heterocycles fused to the hydronaphthalene ring system, e.g. II, in a single step. The products of the reaction feature heterocycles fused either to benzene rings or to a cyclohexane ring. The product distribution correlates with the electronic richness of the heterocyclic ring. A moderate degree of diastereoselectivity was observed using heterocycles featuring chiral nitrogen substituents. In the experiment, the researchers used many compounds, for example, 4,5-Diiodo-1H-imidazole (cas: 15813-09-9HPLC of Formula: 15813-09-9).

4,5-Diiodo-1H-imidazole (cas: 15813-09-9) belongs to iodide derivatives. Organoiodine compounds occur widely in organic chemistry, but are relatively rare in nature. In the chemical industry, alkyl iodides serve as excellent alkylating agents and, specifically, methyl iodide is used as a methylating agent in the synthesis of various pharmaceutical drugs.HPLC of Formula: 15813-09-9

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

Reinvestigation of the orientation of halogen substitution in imidazoles by nuclear magnetic resonance spectroscopy was written by Naidu, M. Seshapathi R.;Bensusan, Howard B.. And the article was included in Journal of Organic Chemistry in 1968.Product Details of 15813-09-9 This article mentions the following:

Imidazole is treated with iodine at pH 7 and in an alk. medium and 4(5)-methylimidazole is treated with iodine in alk. medium to give 4,5-diiodoimidazole and 4(5)-iodo-5(4)-methylimidazole. Similarly prepared is 4(5)-bromo-5(4)-methylimidazole. N.M.R. data are given. In the experiment, the researchers used many compounds, for example, 4,5-Diiodo-1H-imidazole (cas: 15813-09-9Product Details of 15813-09-9).

4,5-Diiodo-1H-imidazole (cas: 15813-09-9) belongs to iodide derivatives. Typical reactions of alkyl iodides include nucleophilic substitution, elimination, reduction, and the formation of organometallics. In the chemical industry, alkyl iodides serve as excellent alkylating agents and, specifically, methyl iodide is used as a methylating agent in the synthesis of various pharmaceutical drugs.Product Details of 15813-09-9

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

2-Dimensional molecular wiring based on toroidal delocalization of hexaarylbenzene was written by Tanaka, Yuya;Koike, Takashi;Akita, Munetaka. And the article was included in Chemical Communications (Cambridge, United Kingdom) in 2010.COA of Formula: C10H12I2 This article mentions the following:

A series of tetraphenylbenzenes having two peripheral thienyliron substituents, and their non-arylated models, I [M = (dppe)Fe(η⁵-C₅H₅); 1, R¹ = Ph, R² = H; 2, R¹ = Ph, R² = Me; 3, R¹ = R² = H] and II [M = (dppe)Fe(η⁵-C₅H₅); 4, R³ = Ph; 5, R³ = Me] has been prepared; the electron communication of the metal centers through toroidal delocalization among the peripheral aromatic groups is evidenced by electrochem. and near-IR data. Crystal structures of 1, 2 and 5 are reported. In the experiment, the researchers used many compounds, for example, 1,4-Diiodo-2,3,5,6-tetramethylbenzene (cas: 3268-21-1COA of Formula: C10H12I2).

1,4-Diiodo-2,3,5,6-tetramethylbenzene (cas: 3268-21-1) belongs to iodide derivatives. Iodide-containing intermediates are common in organic synthesis, because of the easy formation and cleavage of the C–I bond. Organoiodine lubricants can be used with titanium, stainless steels, and other metals which tend to seize up with conventional lubricants: organoiodine lubricants can be used in turbines and spacecraft, and as a cutting oil in machining.COA of Formula: C10H12I2

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

Convenient access to bis-indole alkaloids. Application to the synthesis of topsentins was written by Mal, Sajal K.;Bohe, Luis;Achab, Said. And the article was included in Tetrahedron in 2008.Safety of 4,5-Diiodo-1H-imidazole This article mentions the following:

Topsentins and related bis-indole alkaloids, e.g. I, may be efficiently synthesized through an addition/oxidation sequence leading to 2-(3-indolylcarbonyl)-imidazole derivatives followed by a Pd-catalyzed heteroarylation with the appropriate 3-stannylindoles. In the experiment, the researchers used many compounds, for example, 4,5-Diiodo-1H-imidazole (cas: 15813-09-9Safety of 4,5-Diiodo-1H-imidazole).

4,5-Diiodo-1H-imidazole (cas: 15813-09-9) belongs to iodide derivatives. Organic iodides are widely used in organic synthesis. Halogenation of aromatic hydrocarbons is a very important reaction via an electrophilic aromatic substitution. Iodo alkanes participate in a variety of organic synthesis reactions, which include the Simmons–Smith reaction (cyclopropanation using iodomethane), Williamson ether synthesis, Wittig reaction, Grignard reaction, alkyl coupling reactions, and Wurtz reaction.Safety of 4,5-Diiodo-1H-imidazole

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

Design and synthesis of phenethyl benzo[1,4]oxazine-3-ones as potent inhibitors of PI3Kinaseγ was written by Lanni, Thomas B.;Greene, Keri L.;Kolz, Christine N.;Para, Kimberly S.;Visnick, Melean;Mobley, James L.;Dudley, David T.;Baginski, Theodore J.;Liimatta, Marya B.. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2007.Application of 85356-68-9 This article mentions the following:

The Type 1 PI3-Kinases comprise a family of enzymes, which primarily phosphorylate PIP2 to give the second messenger PIP3, a key player in many intracellular signaling processes. Of the four type 1 PI3Ks, the γ-isoform, which is expressed almost exclusively in leukocytosis of particular interest with respect to its role in inflammatory diseases such as rheumatoid arthritis (RA) and chronic obstructive pulmonary disease (COPD). Investigation of a series of 4,6-disubstituted-4H-benzo[1,4]oxazin-3-ones, e.g., I, has led to the identification of single-digit nanomolar inhibitors of PI3Kγ, several of which had good cell based activity and were shown to be active in vivo in an aspectic peritonitis model of inflammatory cell migration. In the experiment, the researchers used many compounds, for example, 1-Bromo-4-(2-iodoethyl)benzene (cas: 85356-68-9Application of 85356-68-9).

1-Bromo-4-(2-iodoethyl)benzene (cas: 85356-68-9) belongs to iodide derivatives. Generally organic iodides can be divided into two classes of alkyl iodides and aryl iodides. Typical reactions of alkyl iodides include nucleophilic substitution, elimination, reduction, and the formation of organometallics. The C–I bond is the weakest of the carbon–halogen bonds. These bond strengths correlate with the electronegativity of the halogen, decreasing in the order F > Cl > Br > I. This periodic order also follows the atomic radius of halogens and the length of the carbon-halogen bond.Application of 85356-68-9

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