Day: April 14, 2022

The reaction of an aromatic heterocycle with a proton is called a protonation. One of articles about this theory is 《Preparation of o-dialkylbenzene》. Authors are Ogawa, Masaya; Tanaka, Giichi.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).Reference of 5-(hydroxymethyl)-2,4-dimethylpyridin-3-ol hydrochloride. Through the article, more information about this compound (cas:148-51-6) is conveyed.

1-Butyl-1-cyclohexene (45 g.) was oxidized 2 h. below 45° with 275 g. 80% HCO2H and with 50 g. 30% H2O2, the mixture neutralized and extracted with EtOAc, and the extract distilled to give 26 g. 1-butyl-l,2-cyclohexanediol (I), b2 115-18°. I (10 g.) in 50 cc. EtOH refluxed 30 min. with 0.5 cc. H2SO4, and the mixture distilled gave 4 g. 2-butylcyclohexanone (II), b7 76-8°. II was also prepared (51%) starting with 2-chlorocyclohexanone. II (0.5 mol) and 1 mol RMgX mixed at 0°, refluxed 5-7 h. at 30-5°, and distilled gave the following 1-alkyl-2-butylcyclohexanol (III) (alkyl, b.p./mm., d20, nD20, and % yield given): Bu, 115-17°/3.5, 0.8989, 1.4679, 43.2; octyl, 155-7°/4, 0.8850, 1.4683, 40; dodecyl, 184-5°/1, -, -, 37.4 (m. 46.5-7.5°). III heated 5 h. on oil bath with iodine and the product washed with 1% aqueous Na2S2O3 and distilled gave the following 1-alkyl-2-butyl-l-cyclohexenes (IV) (alkyl, b.p./mm., d20, nD20, and % yield given): Bu, 82-5°/3, 0.8410, 1.4635, 68.5; octyl, 148-51°/6, 0.8407, 1.4654, 85; dodecyl, 161-5°/1, 0.8407, 1.4654, 82.1. The IV were dehydrogenated over Pd-C at 220-80° to give the following 1-alkyl-2-butylbenzene (alkyl, b.p., d20, nD20, and % yield given): Bu, 256-7°, 0.8553, 1.4826, 57; octyl, 305-7°, 0.8570, 1.4827, 69; dodecyl, 358-9°, 0.8579, 1.4820, 46.

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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 《The relation between iodine-131 metabolism, tumor growth, and regression》. Authors are Scott, Kenneth G.; Daniels, Marie B..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).Application of 148-51-6. Through the article, more information about this compound (cas:148-51-6) is conveyed.

Ability of tumors to alter the normal metabolic pathway of I131 and compounds labeled with it (iodide-trapping syndrome) (I) is characterized by higher than normal retention of I131 by skin, muscle, gastrointestinal tract, and plasma, and a lower than normal thyroid uptake and urinary excretion of I131. I was elicited in rats by isografts and homografts of a transmissible fibrosarcoma, but not by homoiografts (which regressed after 5-7 days of growth). The data suggest that local and systemic I parallels progressive tumor growth and is absent in tumor implants destined to regress.

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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 《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).SDS of cas: 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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Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Product Details of 18436-73-2. The fused heterocycle is formed by combining a benzene ring with a single heterocycle, or two or more single heterocycles. Compound: 4-Chloro-8-methylquinoline, is researched, Molecular C10H8ClN, CAS is 18436-73-2, about C(sp3)-H amination of 8-methylquinolines with azodicarboxylates under Rh(III) catalysis: cytotoxic evaluation of quinolin-8-ylmethanamines. Author is Jeong, Taejoo; Mishra, Neeraj Kumar; Dey, Prasanta; Oh, Hyunjung; Han, Sangil; Lee, Suk Hun; Kim, Hyung Sik; Park, Jihye; Kim, In Su.

The rhodium(III)-catalyzed C(sp3)-H amination reaction of 8-methylquinolines and azodicarboxylates is described. A cationic rhodium catalyst in the presence of lithium acetate and lithium carbonate was found to be an optimal catalytic system for the construction of quinolin-8-ylmethanamine derivatives, which were evaluated for in vitro cytotoxicity against human breast adenocarcinoma cells (MCF-7) and human prostate adenocarcinoma cells (LNCaP).

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Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

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.SDS of cas: 18436-73-2.Chen, Junli; Campbell, Adrian P.; Urmi, Kaniz F.; Wakelin, Laurence P. G.; Denny, William A.; Griffith, Renate; Finch, Angela M. published the article 《Human α1-adrenoceptor subtype selectivity of substituted homobivalent 4-aminoquinolines》 about this compound( cas:18436-73-2 ) in Bioorganic & Medicinal Chemistry. Keywords: human adrenoceptor selectivity homobivalent aminoquinoline; 4-Aminoquinolines; 5-HT(1A)-receptor; Affinity; Selectivity; α(1)-adrenoceptor. Let’s learn more about this compound (cas:18436-73-2).

A series of ring-substituted ethyl- and heptyl-linked 4-aminoquinoline dimers were synthesized and evaluated for their affinities at the 3 human α1-adrenoceptor (α1-AR) subtypes and the human serotonin 5-HT1A-receptor (5-HT1A-R). We find that the structure-specificity profiles are different for the two series at the α1-AR subtypes, which suggests that homobivalent 4-aminoquinolines can be developed with α1-AR subtype selectivity. The 8-Me ethyl-linked analog has the highest affinity for the α1A-AR, 7 nM, and the greatest capacity for discriminating between α1A-AR and α1B-AR (6-fold), α1D-AR (68-fold), and the 5-HT1A-R (168-fold). α1B-AR selectivity was observed with the 6-Me derivative of the ethyl- and heptyl-linked 4-aminoquinoline dimers and the 7-methoxy (7-OMe) derivative of the heptyl-linked analog. These substitutions result in 4- to 80-fold selectivity for α1B-AR over α1A-AR, α1D-AR, and 5-HT1A-R. In contrast, 4-aminoquinoline dimers with selectivity for α1D-AR are more elusive, since none studied to date has greater affinity for the α1D-AR over the other two α1-ARs. The selectivity of the 8-Me ethyl-linked 4-aminoquinoline dimer for the α1A-AR, and 6-Me ethyl-linked, and the 6-Me and 7-OMe heptyl-linked 4-aminoquinoline dimers for the α1B-AR, makes them promising leads for drug development of α1A-AR or α1B-AR subtype selective ligands with reduced 5-HT1A-R affinity.

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Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Electric Literature of C10H6Cl2N2O2. 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: 5-(3,4-Dichlorophenyl)-1H-pyrazole-3-carboxylic acid, is researched, Molecular C10H6Cl2N2O2, CAS is 276684-04-9, about Application of a Parallel Synthetic Strategy in the Discovery of Biaryl Acyl Sulfonamides as Efficient and Selective NaV1.7 Inhibitors. Author is DiMauro, Erin F.; Altmann, Stephen; Berry, Loren M.; Bregman, Howard; Chakka, Nagasree; Chu-Moyer, Margaret; Bojic, Elma Feric; Foti, Robert S.; Fremeau, Robert; Gao, Hua; Gunaydin, Hakan; Guzman-Perez, Angel; Hall, Brian E.; Huang, Hongbing; Jarosh, Michael; Kornecook, Thomas; Lee, Josie; Ligutti, Joseph; Liu, Dong; Moyer, Bryan D.; Ortuno, Daniel; Rose, Paul E.; Schenkel, Laurie B.; Taborn, Kristin; Wang, Jean; Wang, Yan; Yu, Violeta; Weiss, Matthew M..

The majority of potent and selective hNaV1.7 inhibitors possess common pharmacophoric features that include a heteroaryl sulfonamide headgroup and a lipophilic aromatic tail group. Recently, reports of similar aromatic tail groups in combination with an acyl sulfonamide headgroup have emerged, with the acyl sulfonamide bestowing levels of selectivity over hNaV1.5 comparable to the heteroaryl sulfonamide. Beginning with com. available carboxylic acids that met selected pharmacophoric requirements in the lipophilic tail, a parallel synthetic approach was applied to rapidly generate the derived acyl sulfonamides. A biaryl acyl sulfonamide hit from this library was elaborated, optimizing for potency and selectivity with attention to physicochem. properties. The resulting novel leads are potent, ligand and lipophilic efficient, and selective over hNaV1.5. Representative lead I demonstrates selectivity over other human NaV isoforms and good pharmacokinetics in rodents. The biaryl acyl sulfonamides reported herein may also offer ADME advantages over known heteroaryl sulfonamide inhibitors.

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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 《The relation between iodine-131 metabolism, tumor growth, and regression》. Authors are Scott, Kenneth G.; Daniels, Marie B..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).Application of 148-51-6. Through the article, more information about this compound (cas:148-51-6) is conveyed.

Ability of tumors to alter the normal metabolic pathway of I131 and compounds labeled with it (iodide-trapping syndrome) (I) is characterized by higher than normal retention of I131 by skin, muscle, gastrointestinal tract, and plasma, and a lower than normal thyroid uptake and urinary excretion of I131. I was elicited in rats by isografts and homografts of a transmissible fibrosarcoma, but not by homoiografts (which regressed after 5-7 days of growth). The data suggest that local and systemic I parallels progressive tumor growth and is absent in tumor implants destined to regress.

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Reference:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Heterocyclic compounds can be divided into two categories: alicyclic heterocycles and aromatic heterocycles. Compounds whose heterocycles in the molecular skeleton cannot reflect aromaticity are called alicyclic heterocyclic compounds. Compound: 65090-78-0, is researched, Molecular C4H7BrO3, about A convenient and exclusive methoxybromination of alkenes, the main research direction is methoxybromination alkene; methoxyiodination alkene; alkene methoxybromination methoxyiodination; bromination methoxy alkene; iodination methoxy cyclohexene.Application of 65090-78-0.

Alkenes R1CR2:CR3R4 (e.g., R1 = Ph, p-tolyl, H; R2 = H, Me; R3 = HCO2Me; R4 = CO2Me, H) were methoxybrominated with Br in MeOH in the presence of AgNO3, Pb(NO3)2 or yellow Pb oxide (which one depended on the nature of the alkene). Cyclohexene was methoxyiodinated similarly in the presence of AgNO3. Electrophilic addition of the elements of MeOBr was general. The trans and stereospecific nature was established by studying dehydrobromination of methoxybromoadducts under E2 elimination conditions.

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Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Stone, William E. published the article 《Effects of alterations in the metabolism of γ-aminobutyrate on convulsant potencies》. Keywords: GABA convulsant mechanism; mercaptopropionate convulsion GABA; pentamethylenetetrazole convulsion GABA; bicuculline convulsion GABA; picrotoxin convulsion GABA.They researched the compound: 5-(hydroxymethyl)-2,4-dimethylpyridin-3-ol hydrochloride( cas:148-51-6 ).Name: 5-(hydroxymethyl)-2,4-dimethylpyridin-3-ol hydrochloride. Aromatic heterocyclic compounds can be divided into two categories: single heterocyclic and fused heterocyclic. In addition, there is a lot of other information about this compound (cas:148-51-6) here.

Drugs that alter γ-aminobutyrate (GABA) [56-12-2] metabolism and presumably affect the availability of GABA in synaptic regions were tested for their relative effects on the potencies of 4 convulsants: 3-mercaptopropionate (3-MP) [107-96-0], pentamethylenetetrazole (PTZ) [54-95-5], bicuculline [485-49-4], and picrotoxin [124-87-8] in mice. Aminooxyacetic acid hemichloride [2921-14-4] given prior to the convulsant tended to decrease the potency of 3-MP more than that of PTZ. It decreased the potency of bicuculline more than that of PTZ but less than that of 3-MP, and did not alter that of picrotoxin. Thiocarbohydrazide (TCH) [2231-57-4], DL-C-allylglycine [7685-44-1], and 4-deoxypyridoxine-HCl (DOP) [148-51-6] tended to potentiate 3-MP more than PTZ. The effects of allylglycine on bicuculline and picrotoxin were intermediate. DOP potentiated bicuculline and picrotoxin only to the extent that it potentiated PTZ. TCH resembled DOP in its effect on bicuculline. Valproic acid [99-66-1] decreased the potency of each convulsant; it was most effective against PTZ, slightly less so against 3-MP, and still less effective against bicuculline and picrotoxin. Its anticonvulsive action probably is not primarily via the GABA system. Phenelzine [51-71-8] slightly decreased the potency of bicuculline, but potentiated 3-MP and picrotoxin and did not affect the potency of PTZ. Diacetyl monoxime [57-71-6] was anticonvulsive against PTZ, bicuculline, and picrotoxin, but not against 3-MP. The results do not support the view that bicuculline and picrotoxin induce seizures by blocking GABA-mediated inhibition.

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Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

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.Landge, Vinod G.; Sahoo, Manoj K.; Midya, Siba P.; Jaiswal, Garima; Balaraman, Ekambaram researched the compound: 4-Chloro-8-methylquinoline( cas:18436-73-2 ).COA of Formula: C10H8ClN.They published the article 《Well-defined palladium(II) complexes for ligand-enabled C(sp3)-alkynylation》 about this compound( cas:18436-73-2 ) in Dalton Transactions. Keywords: palladium catalyst alkynylation methylquinoline; quinoline methyl alkynylation palladium catalyst. We’ll tell you more about this compound (cas:18436-73-2).

The first example of ligand-enabled C(sp3)-alkynylation of 8-methylquinoline is reported. The reaction is catalyzed by well-defined Pd(II) complexes. The present C(sp3)-alkynylation has a broad substrate scope as well as functional group tolerance and proceeds efficiently under mild conditions.

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Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia