Tag: 200-300

Design, synthesis and structure-activity relationships of novel biarylamine-based Met kinase inhibitors was written by Williams, David K.;Chen, Xiao-Tao;Tarby, Christine;Kaltenbach, Robert;Cai, Zhen-Wei;Tokarski, John S.;An, Yongmi;Sack, John S.;Wautlet, Barri;Gullo-Brown, Johnni;Henley, Benjamin J.;Jeyaseelan, Robert;Kellar, Kristen;Manne, Veeraswamy;Trainor, George L.;Lombardo, Louis J.;Fargnoli, Joseph;Borzilleri, Robert M.. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2010.Reference of 29241-66-5 This article mentions the following:

Aminopyridinyloxy- or azaindolyloxy phenylamino heteroarylcarboxamides such as I are prepared and tested for their inhibition of Met kinase and for their inhibition of a human gastric cancer cell line. X-ray crystallog. of an aminopyridinyloxyphenylamino pyridinecarboxamide bound to Met kinase reveals that these compounds adopt a bioactive conformation, in the kinase domain, consistent with that seen for a 2-pyridone-based Met kinase inhibitor. I demonstrated potent in vivo antitumor activity in the GTL-16 human tumor xenograft model; its selectivity against various kinases is determined In the experiment, the researchers used many compounds, for example, 5-Bromo-2-fluoronicotinic acid (cas: 29241-66-5Reference of 29241-66-5).

5-Bromo-2-fluoronicotinic acid (cas: 29241-66-5) belongs to organobromine compounds. Many of the organo bromine compounds are relatively nonpolar. Bromine is more electronegative than carbon (2.8 vs 2.5) and hence the carbon in a carbon–bromine bond is electrophilic in nature. The principal reactions for organobromides include dehydrobromination, Grignard reactions, reductive coupling, and nucleophilic substitution.Reference of 29241-66-5

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Bromide – Wikipedia,
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Multicomponent synthesis of furopyridopyrimidines – heterocyclic analogs of podophyllotoxin was written by author. And the article was included in Izvestiya Timiryazevskoi Sel’skokhozyaistvennoi Akademii in 2012.SDS of cas: 108940-96-1 This article mentions the following:

Proposed a convenient method for the synthesis of furopyridopyrimidines I [R¹ = HO, H₂N; R² = 4-HOC₆H₄, 3,4,5-(MeO)₃C₆H₂, 3-Br-4,5-(MeO)₂C₆H₂, etc.] by multicomponent reaction of 2-methylthiopyrimidine-4,6-diamine, tetronic acid and aromatic aldehydes R²CHO. In the experiment, the researchers used many compounds, for example, 3,5-Dibromo-4-methoxybenzaldehyde (cas: 108940-96-1SDS of cas: 108940-96-1).

3,5-Dibromo-4-methoxybenzaldehyde (cas: 108940-96-1) belongs to organobromine compounds. A variety of minor organobromine compounds are found in nature, but none are biosynthesized or required by mammals. Organobromine compounds have fallen under increased scrutiny for their environmental impact. The reactivity of organobromine compounds resembles but is intermediate between the reactivity of organochlorine and organoiodine compounds. For many applications, organobromides represent a compromise of reactivity and cost.SDS of cas: 108940-96-1

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Bromide – Wikipedia,
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Sequential Assembly of Morita-Baylis-Hillman Carbonates and Activated ortho-Vinylbenzaldehydes To Construct Chiral Methanobenzo[7]annulenone Frameworks was written by Jiang, Bo;Xiao, Ben-Xian;Ouyang, Qin;Liang, Hua-Ping;Du, Wei;Chen, Ying-Chun. And the article was included in Organic Letters in 2019.Reference of 85118-24-7 This article mentions the following:

The α-regioselective asym. [3 + 2] annulation reaction of Morita-Baylis-Hillman carbonates from isatins and activated ortho-vinylbenzaldehyses was developed by the catalysis of a chiral tertiary amine. The sequential N-heterocyclic carbene-mediated intramol. Stetter reaction was conducted to finally furnish the bridged 5,8-methanobenzo[7]annulen-9-one architectures incorporating a spirooxindole motif with excellent stereoselectivity. In the experiment, the researchers used many compounds, for example, 2-Bromo-4-(trifluoromethyl)benzaldehyde (cas: 85118-24-7Reference of 85118-24-7).

2-Bromo-4-(trifluoromethyl)benzaldehyde (cas: 85118-24-7) belongs to organobromine compounds. Bromine is more electronegative than carbon (2.9 vs 2.5). Consequently, the carbon in a carbon–bromine bond is electrophilic, i.e. alkyl bromides are alkylating agents. Bromine-containing agents predominate because not only are they more efficient than similar chlorine-containing species, but also the high atomic weight of bromine ensures that it is present in a high mass fraction within most organobromine compounds.Reference of 85118-24-7

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Bromide – Wikipedia,
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Iron-catalyzed C(sp²)-H alkylation of carboxamides with primary electrophiles was written by Monks, Brendan M.;Fruchey, Erin R.;Cook, Silas P.. And the article was included in Angewandte Chemie, International Edition in 2014.Safety of 1-(2-Bromoethyl)-4-methoxybenzene This article mentions the following:

A robust iron-catalyzed ortho alkylation of aryl amides was carried out. The reaction generally proceeds in high yields with exceptional regioselectivity. The reaction is complete in less than 10 min and can be performed in bio-derived 2-methyltetrahydrofuran as solvent on gram scale. The reactivity and selectivity provides a reaction profile unique among the reported C-H functionalization reactions, thereby complementing current strategies. The low cost and toxicity of the reagents should simplify the large-scale implementation of this C-H functionalization. Moreover, mechanistic experiments indicate that substrate coordination is irreversible and occurs prior to C-H cleavage. Further efforts will be directed toward mechanistic understanding and expanding the scope of this interesting transformation. © 2014 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim. In the experiment, the researchers used many compounds, for example, 1-(2-Bromoethyl)-4-methoxybenzene (cas: 14425-64-0Safety of 1-(2-Bromoethyl)-4-methoxybenzene).

1-(2-Bromoethyl)-4-methoxybenzene (cas: 14425-64-0) belongs to organobromine compounds. Many of the organo bromine compounds are relatively nonpolar. Bromine is more electronegative than carbon (2.8 vs 2.5) and hence the carbon in a carbon–bromine bond is electrophilic in nature. Commercially available organobromine pharmaceuticals include the vasodilator nicergoline, the sedative brotizolam, the anticancer agent pipobroman, and the antiseptic merbromin. Safety of 1-(2-Bromoethyl)-4-methoxybenzene

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Bromide – Wikipedia,
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Internal lewis acid assisted benzoic acid catalysis was written by Auvil, Tyler J.;Mattson, Anita E.. And the article was included in Synthesis in 2012.Category: bromides-buliding-blocks This article mentions the following:

Internal Lewis acid assisted benzoic acid derivatives are introduced as new low-mol.-weight single-hydrogen-bond donor catalysts for the activation of nitroalkenes. Selected 2-borylbenzoic acid derivatives gave good yields of products in the addition of indoles to nitroalkenes. Control experiments suggest that both the internal Lewis acid coordination and the carboxylic acid functionalities are critical to the optimal performance of these catalysts. In the experiment, the researchers used many compounds, for example, Methyl 2-bromo-4-fluorobenzoate (cas: 653-92-9Category: bromides-buliding-blocks).

Methyl 2-bromo-4-fluorobenzoate (cas: 653-92-9) belongs to organobromine compounds. Bromo compounds are employed in a variety of metal-catalyzed coupling reactions. They are also ideal candidates for the synthesis of Grignard reagents that have wide-applicability in organic synthesis. alpha-Bromoesters are employed in the Reformatsky reaction for the synthesis of beta-hydroxyesters. When the molecular ion is detected, the bromine and chlorine isotope patterns are very distinct, but caution is to be exercised for certain mixed chlorinated/brominated compounds, which can look similar to homohalogen patterns.Category: bromides-buliding-blocks

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Bromide – Wikipedia,
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Copper(I)-Catalyzed Asymmetric Desymmetrization: Synthesis of Five-Membered-Ring Compounds Containing All-Carbon Quaternary Stereocenters was written by Aikawa, Kohsuke;Okamoto, Tatsuya;Mikami, Koichi. And the article was included in Journal of the American Chemical Society in 2012.Recommanded Product: 162258-89-1 This article mentions the following:

A highly stereoselective catalytic alkylation sequence for the synthesis of highly functionalized and versatile five-membered-ring compounds bearing all-carbon quaternary stereocenters was developed. Enantioselective desymmetrization of achiral cyclopentene-1,3-diones was thus executed by chiral Cu-phosphoramidite catalysts. A variety of complicated cyclopentane derivatives can be synthesized with excellent stereoselectivities using a low catalyst loading in a one-pot operation. In the experiment, the researchers used many compounds, for example, 4-Bromo-4′-tert-butylbiphenyl (cas: 162258-89-1Recommanded Product: 162258-89-1).

4-Bromo-4′-tert-butylbiphenyl (cas: 162258-89-1) belongs to organobromine compounds. A variety of minor organobromine compounds are found in nature, but none are biosynthesized or required by mammals. Organobromine compounds have fallen under increased scrutiny for their environmental impact. Commercially available organobromine pharmaceuticals include the vasodilator nicergoline, the sedative brotizolam, the anticancer agent pipobroman, and the antiseptic merbromin. Recommanded Product: 162258-89-1

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Bromide – Wikipedia,
bromide – Wiktionary

The influence of solvent on the addition of hydrogen bromide to some allylbenzenes in the presence of peroxides was written by Delobelle, Jacques;Fetizon, Marcel;Baranger, Pierre;Schalbar, Jeanine. And the article was included in Compt. rend. in 1957.Product Details of 57293-19-3 This article mentions the following:

p-MeOC₆H₄(CH₂)₃Br (I) has been prepared in 2 ways: (a) from anisaldehyde via Me p-methoxycinnamate and p-MeOC₆H₄(CH₂)₃OH, b_0.2 104-6°, n_D¹⁹ 1.5493; (b) from p-methoxyallylbenzene (II) by the addition of HBr in PhMe in the presence of Bz₂O₂, b_0.06 97°, n_D¹⁹ 1.5502. The Grignard reagent of each treated with PhNCO gave the anilide, m. 100-1° (from cyclohexane). The infrared spectra of I from b had an addnl. band at 1000 cm.^-1, attributable to a small amount of p-MeOC₆H₄CH₂CHBrMe (III), formed as a side-product. An authentic sample of III b_0.6 110-12°, n_D¹⁷ 1.5508. A qualitative study of this reaction showed that in the presence of Bz₂O₂ in PhMe, HBr added to II to give nearly pure I, but that in MeNO₂ a much greater proportion of III resulted. In the experiment, the researchers used many compounds, for example, 1-(3-Bromopropyl)-4-methoxybenzene (cas: 57293-19-3Product Details of 57293-19-3).

1-(3-Bromopropyl)-4-methoxybenzene (cas: 57293-19-3) belongs to organobromine compounds. Bromine is more electronegative than carbon (2.9 vs 2.5). Consequently, the carbon in a carbon–bromine bond is electrophilic, i.e. alkyl bromides are alkylating agents. Commercially available organobromine pharmaceuticals include the vasodilator nicergoline, the sedative brotizolam, the anticancer agent pipobroman, and the antiseptic merbromin. Product Details of 57293-19-3

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Bromide – Wikipedia,
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Novel Class of Colony-Stimulating Factor 1 Receptor Kinase Inhibitors Based on an o-Aminopyridyl Alkynyl Scaffold as Potential Treatment for Inflammatory Disorders was written by Xie, Zhicheng;Wu, Bing;Liu, Yingqiang;Ren, Wenming;Tong, Linjiang;Xiang, Caigui;Wei, Aihuan;Gao, Yuanzhuo;Zeng, Limin;Xie, Hua;Tang, Wei;Hu, Youhong. And the article was included in Journal of Medicinal Chemistry in 2020.Recommanded Product: 6-Amino-5-bromonicotinic acid This article mentions the following:

Colony-stimulating factor 1 receptor (CSF-1R) is involved in inflammatory disorders as well as in many types of cancer. Based on high-throughput screening and docking results, we performed a detailed structure-activity-relationship study, leading to the discovery of a new series of compounds with nanomolar IC₅₀ values against CSF-1R without the inhibition of fibroblast growth factor receptors. One of the most promising hits, compound 29, potently inhibited CSF-1R kinase with an IC₅₀ value of 0.7 nM, while it showed no inhibition to the same family member FMS-like tyrosine kinase 3. Compound 29 displayed excellent anti-inflammatory effects against RAW264.7 macrophages indicated by significant inhibition against the activation of the CSF-1R pathway with low cytotoxicity. In addition, compound 29 exhibited strong in vivo anti-inflammatory efficacy alongside favorable drug characteristics. This novel compound 29 may serve as a new drug candidate with promising applications in inflammatory disorders. In the experiment, the researchers used many compounds, for example, 6-Amino-5-bromonicotinic acid (cas: 180340-69-6Recommanded Product: 6-Amino-5-bromonicotinic acid).

6-Amino-5-bromonicotinic acid (cas: 180340-69-6) belongs to organobromine compounds. Many of the organo bromine compounds are relatively nonpolar. Bromine is more electronegative than carbon (2.8 vs 2.5) and hence the carbon in a carbon–bromine bond is electrophilic in nature. Many of the alkyl bromine derivatives are excellent alkylating agents since bromides are good leaving groups. Tribromides, like tetrabutylammonium tribromide, are used as a solid source of bromine. N-bromosuccimide (NBS) is used for the selective bromination of allylic bonds.Recommanded Product: 6-Amino-5-bromonicotinic acid

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Intramolecular Pd-Catalyzed Reductive Amination of Enolizable sp³-C-H Bonds was written by Ford, Russell L.;Alt, Isabel;Jana, Navendu;Driver, Tom G.. And the article was included in Organic Letters in 2019.Computed Properties of C7H5BrFNO2 This article mentions the following:

A palladium-catalyzed reductive cyclization of nitroarenes has been designed to construct sp³-C-NHAr bonds from sp³-C-H bonds by using an enolizable nucleophile to intercept a nitrosoarene intermediate. Exposure of ortho-substituted nitroarenes to 5 mol % of Pd(OAc)₂ and 10 mol % of phenanthroline under 2 atm of CO constructs partially saturated 5-, 6-, or 7-membered N-heterocycles I (R¹ = H, Cl, Me, etc.; R² = H, F, Me, etc.; R³ = H, Me) using α-pyridyl carboxylates, malonates, 1,3-dimethylbarbituric acid, 1,3-diones, or difurans as the nucleophile. In the experiment, the researchers used many compounds, for example, 1-(Bromomethyl)-4-fluoro-2-nitrobenzene (cas: 76437-44-0Computed Properties of C7H5BrFNO2).

1-(Bromomethyl)-4-fluoro-2-nitrobenzene (cas: 76437-44-0) belongs to organobromine compounds. Bromine is more electronegative than carbon (2.9 vs 2.5). Consequently, the carbon in a carbon–bromine bond is electrophilic, i.e. alkyl bromides are alkylating agents. In the pharmaceutical industry organo bromine derivatives are used as sedatives, vasodilators, antiseptic agents, and anticancer agents.Computed Properties of C7H5BrFNO2

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MeOTf-Catalyzed Intramolecular Acyl-Cyclization of Aryl Isocyanates: Efficient Access to Phenanthridin-6(5H)-one and 3,4-Dihydroisoquinolin-1(2H)-one Derivatives was written by Zou, Song;Zhang, Zeyu;Chen, Chao;Xi, Chanjuan. And the article was included in Asian Journal of Organic Chemistry in 2021.Formula: C9H11BrO This article mentions the following:

MeOTf-catalyzed intramol. acyl-cyclization of aryl isocyanates has been realized to provide (NH)-phenanthridinones and lactams under metal-free conditions. A variety of functional groups are tolerated in their scaffolds with good to excellent yields. The reaction could be carried to gram scale and a range of natural alkaloids, such as crinasiadine, benzophenidine alkaloid (ZYH005), N-methylcrinasiadine, and trisphaeridine could be synthesized directly or in short steps with high yields. In the experiment, the researchers used many compounds, for example, 1-(2-Bromoethyl)-4-methoxybenzene (cas: 14425-64-0Formula: C9H11BrO).

1-(2-Bromoethyl)-4-methoxybenzene (cas: 14425-64-0) belongs to organobromine compounds. Bromine is more electronegative than carbon (2.9 vs 2.5). Consequently, the carbon in a carbon–bromine bond is electrophilic, i.e. alkyl bromides are alkylating agents. One prominent application of synthetic organobromine compounds is the use of polybrominated diphenyl ethers as fire-retardants, and in fact fire-retardant manufacture is currently the major industrial use of the element bromine.Formula: C9H11BrO

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Bromide – Wikipedia,
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