Day: April 2, 2022

The preparation of ester heterocycles mostly uses heteroatoms as nucleophilic sites, which are achieved by intramolecular substitution or addition reactions. Compound: 4-Chloro-8-methylquinoline( cas:18436-73-2 ) is researched.Product Details of 18436-73-2.Calligaris, Mario; Illuminati, Gabriello; Marino, Gianlorenzo published the article 《Nucleophilic heteroaromatic substitution. XXVII. Piperidino dechlorination and methoxy dechlorination of 6- and 8-alkyl-4-chloroquinolines. Steric hindrance to specific solvation》 about this compound( cas:18436-73-2 ) in Journal of the American Chemical Society. Keywords: KINETICS PIPERIDINO DECHLORINATION; METHOXY DECHLORINATION; PIPERIDINO DECHLORINATION KINETICS; DECHLORINATION PIPERIDINO KINETICS; SOLVATION. Let’s learn more about this compound (cas:18436-73-2).

Kinetic data for the reaction of 6- and 8-alkyl-substituted 4-chloroquinolines with piperidine in four different solvents and with NaOMe in MeOH were obtained and compared. The tert-butyl group located at the position peri to the aza group is found to cause rate-depressing effects and significant increases in the energy and entropy of activation when the solvent is hydroxylic (methanol) whereas only minor changes are observed in aprotic or poor proton-donor solvents (toluene, HCONMe2, and piperidine). The results are interpreted in terms of steric inhibition of specific solvation (H bonding). 15 references.

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Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Wei, Yunlong; Zhang, Hong; Wu, Xinxin; Zhu, Chen published an article about the compound: 5-Methylfuran-2(3H)-one( cas:591-12-8,SMILESS:O=C1OC(C)=CC1 ).Category: pyrimidines. Aromatic heterocyclic compounds can be classified according to the number of heteroatoms or the size of the ring. The authors also want to convey more information about this compound (cas:591-12-8) through the article.

Radical-mediated difunctionalization of alkenes provides a promising approach to introduce one alkenyl or alkynyl group to target compounds However, simultaneous installation of two unsaturated C-C bonds via alkene difunctionalization remains elusive, attributable to the high instability and transient lifetimes of alkenyl and alkynyl radicals. Herein, we report the photocatalytic 1,2-alkynylalkenylation and 1,2-enynylalkenylation of alkenes for the first time, triggered by the intermol. addition of a stabilized allenyl radical to an alkene. A portfolio of strategically designed, easily accessible dual-function reagents are applied to a radical docking-migration cascade. The protocol has broad substrate scope and efficiently increases the degree of unsaturation

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Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Name: Piperidin-4-amine dihydrochloride. The reaction of aromatic heterocyclic molecules with protons is called protonation. Aromatic heterocycles are more basic than benzene due to the participation of heteroatoms. Compound: Piperidin-4-amine dihydrochloride, is researched, Molecular C5H14Cl2N2, CAS is 35621-01-3, about Efficient and Scalable Method for the Selective Alkylation and Acylation of Secondary Amines in the Presence of Primary Amines. Author is Laduron, Frederic; Tamborowski, Vanessa; Moens, Luc; Horvath, Andras; De Smaele, Dirk; Leurs, Stef.

Selective substitution of secondary amines in the presence of primary amines is performed by using the reaction solvent, Me isobutylketone (MIBK), as a temporary protecting group for the primary amine. After acylation or alkylation of the secondary amine, the resulting imine intermediate is smoothly hydrolyzed, leading to the free primary amine in high yield and purity. This procedure represents a cheap and scalable alternative to multistep methods requiring several protections and deprotections.

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The reaction of an aromatic heterocycle with a proton is called a protonation. One of articles about this theory is 《Derivatives of pyridine and quinoline. LII. Synthesis of 2,4-dimethyl-3-hydroxy-5-(hydroxymethyl)pyridine (4-desoxyadermine)》. Authors are van Wagtendonk, H. M.; Wibaut, J. P..The article about the compound:5-(hydroxymethyl)-2,4-dimethylpyridin-3-ol hydrochloridecas:148-51-6,SMILESS:OC1=C(C)C(CO)=CN=C1C.[H]Cl).Recommanded Product: 148-51-6. Through the article, more information about this compound (cas:148-51-6) is conveyed.

cf. C. A. 35, 5112.3. NCCH2CONH2 and CH2Ac2 with piperidine in EtOH at 80° give 87% of 4,6-dimethyl-3-cyano-2-pyridone (I), m. 293° (corrected); with HNO3 (d. 1.52) in Ac2O at 5°, I gives a crude yield of 40-6% of the 5-NO2 derivative which with PCl5 in PhCl gives 24-8% of 2,4-dimethyl-3-nitro-5-cyano-6-chloropyridine (II), yellow, m. 114-15°. Catalytic reduction of II with Pd-C in 96% EtOH gives 81.4% of 2,4-dimethyl-3-amino-5-cyano-6-chloropyridine, m. 149-9.2° (corrected); further reduction with Pd-C catalyst in AcOH-AcONa at room temperature gives 2,4-dimethyl-3-amino-5-(aminomethyl)pyridine, characterized as the dipicrate, m. 244° (decomposition), and the di-HCl salt (III), with 1 mol. H2O, does not m. 300°. Reaction of III in 2 N H2SO4 with NaNO2 at 80° gives 2,4-dimethyl-3-hydroxy-5-(hydroxymethyl)pyridine (4-desoxyadermine), isolated as the HCl salt, m. 257°.

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Recommanded Product: 1260667-65-9. The fused heterocycle is formed by combining a benzene ring with a single heterocycle, or two or more single heterocycles. Compound: 5-Chloro-4-iodopyridin-2-amine, is researched, Molecular C5H4ClIN2, CAS is 1260667-65-9, about Discovery of AZD4573, a Potent and Selective Inhibitor of CDK9 That Enables Short Duration of Target Engagement for the Treatment of Hematological Malignancies. Author is Barlaam, Bernard; Casella, Robert; Cidado, Justin; Cook, Calum; De Savi, Chris; Dishington, Allan; Donald, Craig S.; Drew, Lisa; Ferguson, Andrew D.; Ferguson, Douglas; Glossop, Steve; Grebe, Tyler; Gu, Chungang; Hande, Sudhir; Hawkins, Janet; Hird, Alexander W.; Holmes, Jane; Horstick, James; Jiang, Yun; Lamb, Michelle L.; McGuire, Thomas M.; Moore, Jane E.; O’Connell, Nichole; Pike, Andy; Pike, Kurt G.; Proia, Theresa; Roberts, Bryan; San Martin, Maryann; Sarkar, Ujjal; Shao, Wenlin; Stead, Darren; Sumner, Neil; Thakur, Kumar; Vasbinder, Melissa M.; Varnes, Jeffrey G.; Wang, Jianyan; Wang, Lei; Wu, Dedong; Wu, Liangwei; Yang, Bin; Yao, Tieguang.

A CDK9 inhibitor having short target engagement would enable a reduction of Mcl-1 activity, resulting in apoptosis in cancer cells dependent on Mcl-1 for survival. We report the optimization of a series of amidopyridines (from compound 2), focusing on properties suitable for achieving short target engagement after i.v. administration. By increasing potency and human metabolic clearance, we identified compound 24, a potent and selective CDK9 inhibitor with suitable predicted human pharmacokinetic properties to deliver transient inhibition of CDK9. Furthermore, the solubility of 24 was considered adequate to allow i.v. formulation at the anticipated ED. Short-term treatment with compound 24 led to a rapid dose- and time-dependent decrease of pSer2-RNAP2 and Mcl-1, resulting in cell apoptosis in multiple hematol. cancer cell lines. Intermittent dosing of compound 24 demonstrated efficacy in xenograft models derived from multiple hematol. tumors. Compound 24 is currently in clin. trials for the treatment of hematol. malignancies.

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Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

The reaction of an aromatic heterocycle with a proton is called a protonation. One of articles about this theory is 《4,5-Dihalo and 3-amino analogs of pyridoxine. New route to 4-deoxypyridoxine》. Authors are McCasland, G. E.; Gottwald, L. Kenneth; Furst, Arthur.The article about the compound:5-(hydroxymethyl)-2,4-dimethylpyridin-3-ol hydrochloridecas:148-51-6,SMILESS:OC1=C(C)C(CO)=CN=C1C.[H]Cl).Related Products of 148-51-6. Through the article, more information about this compound (cas:148-51-6) is conveyed.

Dihalo analogs of pyridoxine, expected to show good alkylating activity, were prepared as potential antitumor agents. SOCl2 (15.0 ml.) was added to 2.06 g. powd. dry pyridoxine hydrochloride (I), the mixture refluxed 1 hr., cooled to 0-25° for several days, filtered, and the crystals washed with C6H6, then with 10 ml. Me2CO, m. 140-90°. Recrystallization from absolute EtOH-C6H6 gave 1.6 g. needles. Dissolution in 25 ml. boiling absolute EtOH and treatment with 25 ml. hot C6H6 gave on cooling 0.9 g. 2-methyl-3-hydroxy-4,5-bis(chloromethyl)pyridine hydrochloride (II), m. 175-90° (decomposition), recrystallized from 10 ml. EtOH to yield 0.7 g. product, m.p. unchanged. I (6.2 g.) treated with 43.5 ml. SOCl2 but kept at 25° only 12 hrs. gave after washing with Me2CO 7.1 g. II, m. 185-95° (decomposition). The use of PCl5 in CCl4, or concentrated HCl, failed to yield pure II. I (21.4 g.) and 200 ml. 8.8M HBr was refluxed 15 min., cooled, filtered, and the solid washed with H2O and Me, CO to give 24.2 g. crystalline 2methyl-3-hydroxy-4,5-bis(bromomethyl)pyridine hydrobromide (III), m. 224-8° (decomposition). III (1.88 g.) was stirred with 0.463 g. NaHCO3 in 20 ml. H2O; the mixture turned pink, then red, and after 100 min. stirring was filtered. The solid was washed with H2O and dried to give 0.6 g. brown-red powder, m. above 325°. The pH of the filtrate was 2, indicating displacement of one or both Br atoms from BrCH2. The solid was insoluble at the boiling point in EtOH, H2O, or 6M HCl. I (2.06 g.) boiled with 67.2 g. 7.6M HI gave 1.3 g.2-methyl-3-hydroxy-4,5-bis(iodomethyl)pyridine hydriodide (IV), m. 120-60° (decomposition). III with NaI in Me2CO failed to give IV. 2-Methyl-3-amino-4,5-bis(hydroxymethyl)pyridine monohydrochloride (V), m. 195-7°, with 8.8M HBr gave 34% 2 methyl-3-amino4,5-bis(bromomethyl)pyridine hydrobromide, m. 220° (decomposition). When 1.0 g. V was boiled with 6.5 ml. 7.6M HI, iodine was liberated and one of the HOCH2 groups was reduced to Me to give 0.59 g. black crystalline mass, which was crystallized from absolute EtOH to yield light yellow 2,4-dimethyl-3-amino-5-(hydroxymethyl)pyridine hydriodide (VI), m. 190-6°, VI (50 mg.) was heated 5 min. with 43 mg. AgCl in 1.0 ml. H2O, the mixturefiltered to remove AgI, the filtrate acidified with 0.2 ml. 12M HCl, the acid solution treated with 23 mg. NaNO2 in 1.0 ml. H2O, and the mixture heated until N effervescence ceased (10-15 min.). The solution was vacuum-distilled to dryness, 0.5 ml. 12M HCl added to the residue, the distillation to dryness repeated, the residue extracted with 2.0 ml. absolute EtOH, cooled, and filtered. The filtrate was treated with Et2O and the separated crystals collected and dried to yield 10 mg. 4-deoxypyridoxine hydrochloride, m. 255° (decomposition). V (1.0 g.), 0.8 g. fused NaOAc, and 20 ml. Ac2O was boiled 20 min., the solvent removed by vacuum distillation, the residue extracted with 15 ml. CHCl3, the CHCl3 extract treated with C, and evaporated to give a brown oil, which was stirred with 2.0 ml. Et2O to yield 0.4 g. solid 2-methyl-3-acetamido-4,5-bis(acetoxymethyl)pyridine (VII), m. 103-1° (C6H6). VII (0.42 g.) in 12 ml. 0.5M NaOH was kept 2 hrs. at 20°, the clear solution adjusted to pH 6-7 by addition of HOAc, the solvent evaporated in vacuo, the residue extracted (Soxhlet) 24 hrs. with Me2CO, and the extract cooled to give 0.1 g. crystalline 2-methyl-3-acetamido-4,5-bis(hydroxymethyl)pyridine, m. 185-6°.

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Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Quality Control of 5-Chloro-4-iodopyridin-2-amine. Aromatic heterocyclic compounds can also be classified according to the number of heteroatoms contained in the heterocycle: single heteroatom, two heteroatoms, three heteroatoms and four heteroatoms. Compound: 5-Chloro-4-iodopyridin-2-amine, is researched, Molecular C5H4ClIN2, CAS is 1260667-65-9, about From Milligram to Kilogram Manufacture of AZD4573: Making It Possible by Application of Enzyme-, Iridium-, and Palladium-Catalyzed Key Transformations. Author is Karlsson, Staffan; Benson, Helen; Cook, Calum; Currie, Gordon; Dubiez, Jerome; Emtenaes, Hans; Hawkins, Janet; Meadows, Rebecca; Smith, Peter D.; Varnes, Jeffrey.

With the first generation medicinal chem. synthesis as a starting point, herein process development of AZD4573, an oncol. drug candidate was described. In addition to improved yields and removal of chromatog. steps, other factors such as availability of starting materials as well as safety of the chem. involved were addressed. With several steps involving volatile, reactive, and non-UV active materials, reaction optimization was facilitated by implementing off-line 1H NMR anal. of crude mixtures Key transformations targeted for process development included a Wolff-Kishner reduction, an iridium-catalyzed borylation, and enzymic resolution of a racemic amino-ester.

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Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

The reaction of an aromatic heterocycle with a proton is called a protonation. One of articles about this theory is 《Barriers to Cervical Cancer Screening in Geneva (DEPIST Study).》. Authors are Catarino, Rosa R; Vassilakos, Pierre P; Royannez-Drevard, Isabelle I; Guillot, Cécile C; Alzuphar, Stéphanie S; Fehlmann, Aurore A; Meyer-Hamme, Ulrike U; Petignat, Patrick P.The article about the compound:5-(hydroxymethyl)-2,4-dimethylpyridin-3-ol hydrochloridecas:148-51-6,SMILESS:OC1=C(C)C(CO)=CN=C1C.[H]Cl).Recommanded Product: 148-51-6. Through the article, more information about this compound (cas:148-51-6) is conveyed.

OBJECTIVES: Cervical screening is only efficient if a large part of eligible women participate. Our aim was to identify sociodemographic barriers to cervical screening and consider self-reported reasons to postpone screening. METHODS: Between September 2011 and June 2015, a questionnaire addressing reasons for nonparticipation in cervical screening was completed by 556 women who had not undergone a Pap test in the preceding 3 years. Pearson χ test was used to analyze differences between subgroups. Logistic regression was used to explore the association between sociodemographic characteristics and reasons for nonparticipation. RESULTS: The main reasons for nonparticipation in cervical cancer screening were practical barriers, such as lack of time and the cost of screening. These barriers were more likely to be reported by working women, women who were not sexually active, and those without health insurance. Younger women, non-European women living in Switzerland, and childless women were more likely to have never participated in a screening program before (adjusted odds ratio [aOR], 3.15; 95% CI, 1.41-6.98; aOR, 2.76; 95% CI, 1.48-5.16; aOR, 1.74; 95% CI, 1.03-2.99, respectively). CONCLUSIONS: Practical considerations seem to play a more important role in screening participation than emotional reasons and other beliefs. Particular attention should be paid to immigrant communities, where women seem more likely to skip cervical screening.

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Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

SDS of cas: 591-12-8. Aromatic heterocyclic compounds can also be classified according to the number of heteroatoms contained in the heterocycle: single heteroatom, two heteroatoms, three heteroatoms and four heteroatoms. Compound: 5-Methylfuran-2(3H)-one, is researched, Molecular C5H6O2, CAS is 591-12-8, about Catalytic C-C coupling of furanic platform chemicals to high carbon fuel precursors over supported ionic liquids. Author is Gebresillase, Mahlet N.; Seo, Jeong Gil.

Imidazolium-based ionic liquid (IL) catalysts with different anions (Cl-, HSO4-, and CF3SO3-) were covalently anchored to the surface of fibrous silica (FS) by using alkyl chains as a linker. The prepared catalysts were applied for the C-C coupling reactions of 2-methylfuran (2-MF) with levulinic acid (LA), angelica lactone (AL), and Et levulinate (EL) to synthesize high carbon fuel precursors. The hydrophilic nature of FS supported IL catalyst having bisulfate anion was suitable for the self C-C coupling reaction of 2-MF and the reaction of 2-MF with LA. FS supported IL catalyst having triflate anion (FS-ILCF3SO3) exhibited high conversion and selectivity for the target fuel precursors from the C-C coupling reaction of 2-MF with AL and EL. The increased solubility, tunable acidity, and hydrophilicity/hydrophobicity of FS-ILHSO4 and FS-ILCF3SO3 promise a sustainable catalyst system. Supported ILs make the transformation processes greener and more efficient for large-scale production of biomass-derived fuel precursors.

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Lee, Hyunji; Kim, Dong-Guk; Banskota, Suhrid; Lee, You Kyoung; Nam, Tae-gyu; Kim, Jung-Ae; Jeong, Byeong-Seon published an article about the compound: 5-(hydroxymethyl)-2,4-dimethylpyridin-3-ol hydrochloride( cas:148-51-6,SMILESS:OC1=C(C)C(CO)=CN=C1C.[H]Cl ).Electric Literature of C8H12ClNO2. Aromatic heterocyclic compounds can be classified according to the number of heteroatoms or the size of the ring. The authors also want to convey more information about this compound (cas:148-51-6) through the article.

We recently developed an efficient and practical synthesis for a novel series of pyridoxine-derived 6-amido-2,4,5-trimethylpyridin-3-ols and found that this novel scaffold has outstanding activity to inhibit angiogenesis measured by the quant. chick embryo chorioallantoic membrane (CAM) assay. As an effort to extend the scope of the amidopyridinol scaffold, we here report the synthesis and antiangiogenic activities of a series of bicyclic versions of the amidopyridinol including five- and six-membered cyclic amide-, cyclic urea-, and cyclic carbamate-fused pyridinols. The six membered bicyclic derivatives were prepared by the reported procedures, and the five-membered ring-fused ones were synthesized by new synthetic methods developed in this study. CAM assays showed that both six- and five-membered lactam-fused pyridinols have activities comparable to sunitinib malate, the pos. control, in inhibition of vascular endothelial growth factor-induced angiogenesis. On the other hand, the urea and the carbamate derivatives showed modest to moderate antiangiogenic activities. In summary, some bicyclic aminopyridinols can provide a good platform for structural exploitation in future medicinal chem. work.

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