Month: March 2022

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 Discovery of the First α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid (AMPA) Receptor Antagonist Dependent upon Transmembrane AMPA Receptor Regulatory Protein (TARP) γ-8, published in 2016-05-26, which mentions a compound: 84547-64-8, Name is 3-(Chloromethyl)-1-methyl-1H-pyrazole, Molecular C5H7ClN2, Synthetic Route of C5H7ClN2.

Transmembrane AMPA receptor regulatory proteins (TARPs) are a family of scaffolding proteins that regulate AMPA receptor trafficking and function. TARP γ-8 is one member of this family and is highly expressed within the hippocampus relative to the cerebellum. A selective TARP γ-8-dependent AMPA receptor antagonist (TDAA) is an innovative approach to modulate AMPA receptors in specific brain regions to potentially increase the therapeutic index relative to known non-TARP-dependent AMPA antagonists. We describe here, for the first time, the discovery of a noncompetitive AMPA receptor antagonist that is dependent on the presence of TARP γ-8. Three major iteration cycles were employed to improve upon potency, CYP1A2-dependent challenges, and in vivo clearance. An optimized mol., compound (-)-25 (LY3130481), was fully protective against pentylenetetrazole-induced convulsions in rats without the motor impairment associated with non-TARP-dependent AMPA receptor antagonists. Compound (-)-25 could be utilized to provide proof of concept for antiepileptic efficacy with reduced motor side effects in patients.

From this literature《Discovery of the First α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid (AMPA) Receptor Antagonist Dependent upon Transmembrane AMPA Receptor Regulatory Protein (TARP) γ-8》,we know some information about this compound(84547-64-8)Synthetic Route of C5H7ClN2, but this is not all information, there are many literatures related to this compound(84547-64-8).

Reference:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

COA of Formula: C5H7ClN2. Aromatic compounds can be divided into two categories: single heterocycles and fused heterocycles. Compound: 3-(Chloromethyl)-1-methyl-1H-pyrazole, is researched, Molecular C5H7ClN2, CAS is 84547-64-8, about Discovery of the First α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid (AMPA) Receptor Antagonist Dependent upon Transmembrane AMPA Receptor Regulatory Protein (TARP) γ-8. Author is Gardinier, Kevin M.; Gernert, Douglas L.; Porter, Warren J.; Reel, Jon K.; Ornstein, Paul L.; Spinazze, Patrick; Stevens, F. Craig; Hahn, Patric; Hollinshead, Sean P.; Mayhugh, Daniel; Schkeryantz, Jeff; Khilevich, Albert; De Frutos, Oscar; Gleason, Scott D.; Kato, Akihiko S.; Luffer-Atlas, Debra; Desai, Prashant V.; Swanson, Steven; Burris, Kevin D.; Ding, Chunjin; Heinz, Beverly A.; Need, Anne B.; Barth, Vanessa N.; Stephenson, Gregory A.; Diseroad, Benjamin A.; Woods, Tim A.; Yu, Hong; Bredt, David; Witkin, Jeffrey M..

Transmembrane AMPA receptor regulatory proteins (TARPs) are a family of scaffolding proteins that regulate AMPA receptor trafficking and function. TARP γ-8 is one member of this family and is highly expressed within the hippocampus relative to the cerebellum. A selective TARP γ-8-dependent AMPA receptor antagonist (TDAA) is an innovative approach to modulate AMPA receptors in specific brain regions to potentially increase the therapeutic index relative to known non-TARP-dependent AMPA antagonists. We describe here, for the first time, the discovery of a noncompetitive AMPA receptor antagonist that is dependent on the presence of TARP γ-8. Three major iteration cycles were employed to improve upon potency, CYP1A2-dependent challenges, and in vivo clearance. An optimized mol., compound (-)-25 (LY3130481), was fully protective against pentylenetetrazole-induced convulsions in rats without the motor impairment associated with non-TARP-dependent AMPA receptor antagonists. Compound (-)-25 could be utilized to provide proof of concept for antiepileptic efficacy with reduced motor side effects in patients.

From this literature《Discovery of the First α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid (AMPA) Receptor Antagonist Dependent upon Transmembrane AMPA Receptor Regulatory Protein (TARP) γ-8》,we know some information about this compound(84547-64-8)COA of Formula: C5H7ClN2, but this is not all information, there are many literatures related to this compound(84547-64-8).

Reference:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Product Details of 84547-64-8. 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: 3-(Chloromethyl)-1-methyl-1H-pyrazole, is researched, Molecular C5H7ClN2, CAS is 84547-64-8, about Synthesis of pyrazole derivatives from 1,1-dimethylhydrazine and chlorovinyl ketones. Author is Levkovskaya, G. G.; Bozhenkov, G. V.; Malyushenko, R. N.; Mirskova, A. N..

The reaction of accessible 2-chlorovinyl Me ketones with 1,1-dimethylhydrazine gave pyrazole derivatives in high yields. 1,1,1-Trimethylhydrazinium chloride was isolated as second product of this reaction in high yield.

From this literature《Synthesis of pyrazole derivatives from 1,1-dimethylhydrazine and chlorovinyl ketones》,we know some information about this compound(84547-64-8)Product Details of 84547-64-8, but this is not all information, there are many literatures related to this compound(84547-64-8).

Reference:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

The preparation of ester heterocycles mostly uses heteroatoms as nucleophilic sites, which are achieved by intramolecular substitution or addition reactions. Compound: 5-Bromo-4-methyl-thiazol-2-ylamine hydrobromide( cas:79247-77-1 ) is researched.Formula: C4H6Br2N2S.Jaeger, Jakob; Schraff, Sandra; Pammer, Frank published the article 《Synthesis, Properties, and Solar Cell Performance of Poly(4-(p-alkoxystyryl)thiazole)s》 about this compound( cas:79247-77-1 ) in Macromolecular Chemistry and Physics. Keywords: solar cell polyalkoxystyrylthiazole. Let’s learn more about this compound (cas:79247-77-1).

Polythiazoles (PvTzs) featuring conjugated styryl sidechains equipped with different solubilizing p-alkoxy-groups (-OR, R = n-octyl, n-dodecyl, 2-ethylhexyl, 2-hexyldecyl) is prepared by Negishi-coupling polycondensation. Soluble material with number-average mol. weights of up to Mn = 8.5 kDa (polydispersity (PDI) = 1.3, d.p. (DPn) ≈ 20) is obtained, with a head-to-tail content of the PvTzs of ≈77%, as estimated from comparison with reference polymers. The polymers exhibit optical absorption properties similar to their polythiophene analogs, while their electrochem. characterization shows a significant stabilization of their frontier orbital levels. Fluorescence measurements indicate that upon excitation of the electron rich alkoxystyryl side-chains charge transfer onto the more electron deficient polythiazole backbone occurs. This finding is corroborated by d. functional theory (DFT) calculations on oligomeric model systems, which also consistently reproduce the optical properties observed for the polymers. The potential of these materials for applications in organic electronics can be demonstrated by their use as donor materials in organic photovoltaic cells, which exhibit higher open circuit voltages (VOC, up to 0.86 V) than P3HT- or analogous polythiophene-based cells (VOC = 0.5-0.6 V).

There is still a lot of research devoted to this compound(SMILES：NC1=NC(C)=C(Br)S1.[H]Br)Formula: C4H6Br2N2S, and with the development of science, more effects of this compound(79247-77-1) can be discovered.

Reference:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Perevalov, V. P.; Karim, A. Kh.; Andreeva, M. A.; Rumyantseva, E. G.; Stepanov, B. I. published the article 《1,3- And 1,5-dimethylpyrazole-based syntheses. VI. Stilbene and 1,4-distyrylbenzene analogs containing 3-, 4-, and 5-pyrazolyl radicals》. Keywords: pyrazolyl styrene IR fluorescence; aniline pyrazolylvinyl; nitrobenzene pyrazolylvinyl.They researched the compound: 3-(Chloromethyl)-1-methyl-1H-pyrazole( cas:84547-64-8 ).Quality Control of 3-(Chloromethyl)-1-methyl-1H-pyrazole. 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:84547-64-8) here.

Condensation of 4-O2NC6H4CH2CO2H with pyrazolecarboxaldehydes, followed by reduction with SnCl2, gave I (R, R1 = H, H; Me, H; H, Me). Appropriate Wittig reactions gave II (R = 1-methyl-3-pyrazolyl, 4,5-dichloro-1-methyl-3-pyrazolyl, 1-methyl-5-pyrazolyl, 4-chloro-1-methyl-5-pyrazolyl), which showed intensive blue fluorescence in PhMe solution

There is still a lot of research devoted to this compound(SMILES：CN1N=C(CCl)C=C1)Quality Control of 3-(Chloromethyl)-1-methyl-1H-pyrazole, and with the development of science, more effects of this compound(84547-64-8) can be discovered.

Reference:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

The chemical properties of alicyclic heterocycles are similar to those of the corresponding chain compounds. Compound: 3-(Chloromethyl)-1-methyl-1H-pyrazole, is researched, Molecular C5H7ClN2, CAS is 84547-64-8, about Synthesis of new proton-pump inhibitors (2) and tests for it’s biological activity, the main research direction is antiulcer agent omeprazole analog preparation.COA of Formula: C5H7ClN2.

For development new anti-ulcer agents, we synthesized proton-pump (H+/K+-ATPase) inhibitors which inhibit gastric acid secretion at the last step in the parietal cell. These are omeprazole analogs, in which pyridine group is replaced by pyrazole moiety, to increase pharmacol. activity and to decrease side effects, and we also synthesized substituted benzimidazole rings. The structure of the compounds was identified with 1H-NMR, M.S. and I.R. The compounds with 5-substituted benzimidazoles showed good activity in the following order MeO > Cl > H, and also, 1-benzyl group of pyrazole substituted compounds has enhanced activity.

There is still a lot of research devoted to this compound(SMILES：CN1N=C(CCl)C=C1)COA of Formula: C5H7ClN2, and with the development of science, more effects of this compound(84547-64-8) can be discovered.

Reference:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Perevalov, V. P.; Karim, A. Kh.; Andreeva, M. A.; Rumyantseva, E. G.; Stepanov, B. I. published the article 《1,3- And 1,5-dimethylpyrazole-based syntheses. VI. Stilbene and 1,4-distyrylbenzene analogs containing 3-, 4-, and 5-pyrazolyl radicals》. Keywords: pyrazolyl styrene IR fluorescence; aniline pyrazolylvinyl; nitrobenzene pyrazolylvinyl.They researched the compound: 3-(Chloromethyl)-1-methyl-1H-pyrazole( cas:84547-64-8 ).SDS of cas: 84547-64-8. 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:84547-64-8) here.

Condensation of 4-O2NC6H4CH2CO2H with pyrazolecarboxaldehydes, followed by reduction with SnCl2, gave I (R, R1 = H, H; Me, H; H, Me). Appropriate Wittig reactions gave II (R = 1-methyl-3-pyrazolyl, 4,5-dichloro-1-methyl-3-pyrazolyl, 1-methyl-5-pyrazolyl, 4-chloro-1-methyl-5-pyrazolyl), which showed intensive blue fluorescence in PhMe solution

There is still a lot of research devoted to this compound(SMILES：CN1N=C(CCl)C=C1)SDS of cas: 84547-64-8, and with the development of science, more effects of this compound(84547-64-8) can be discovered.

Reference:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

HPLC of Formula: 79247-77-1. The fused heterocycle is formed by combining a benzene ring with a single heterocycle, or two or more single heterocycles. Compound: 5-Bromo-4-methyl-thiazol-2-ylamine hydrobromide, is researched, Molecular C4H6Br2N2S, CAS is 79247-77-1, about An infrared study of rotational isomerism in thiazole-2-carboxylates. Author is Kaye, Perry T.; Meakins, G. Denis; Willbe, Charles; Williams, Peter R..

Twenty-five alkyl thiazole-2-carboxylates with a range of 4- and 5-substituents were prepared through the Hantzsch synthesis. E.g., cyclocondensation reaction of (H2N)2CS with MeCOCH2Br followed by bromination, oxidation, and alkylation gave the thiazole esters I (R = Me, Et). Solutions of these esters show well resolved doublets in the carbonyl IR spectra, due to rotational isomers. The higher wave number components were assigned to the more polar carbonyl O,S-anti-s-trans rotamers and those at lower wave number to the O,S-syn-s-trans forms. Small, but systematic, differences between the Me esters were noted.

There is still a lot of research devoted to this compound(SMILES：NC1=NC(C)=C(Br)S1.[H]Br)HPLC of Formula: 79247-77-1, and with the development of science, more effects of this compound(79247-77-1) can be discovered.

Reference:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Application In Synthesis of 3-(Chloromethyl)-1-methyl-1H-pyrazole. 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: 3-(Chloromethyl)-1-methyl-1H-pyrazole, is researched, Molecular C5H7ClN2, CAS is 84547-64-8, about Synthesis of new proton-pump inhibitors (2) and tests for it’s biological activity. Author is Kim, Hyo-Jeong; Kwon, Tae-Ik; Park, Il-Hyun.

For development new anti-ulcer agents, we synthesized proton-pump (H+/K+-ATPase) inhibitors which inhibit gastric acid secretion at the last step in the parietal cell. These are omeprazole analogs, in which pyridine group is replaced by pyrazole moiety, to increase pharmacol. activity and to decrease side effects, and we also synthesized substituted benzimidazole rings. The structure of the compounds was identified with 1H-NMR, M.S. and I.R. The compounds with 5-substituted benzimidazoles showed good activity in the following order MeO > Cl > H, and also, 1-benzyl group of pyrazole substituted compounds has enhanced activity.

There is still a lot of research devoted to this compound(SMILES：CN1N=C(CCl)C=C1)Application In Synthesis of 3-(Chloromethyl)-1-methyl-1H-pyrazole, and with the development of science, more effects of this compound(84547-64-8) can be discovered.

Reference:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Reference of 5-Bromo-4-methyl-thiazol-2-ylamine hydrobromide. Aromatic compounds can be divided into two categories: single heterocycles and fused heterocycles. Compound: 5-Bromo-4-methyl-thiazol-2-ylamine hydrobromide, is researched, Molecular C4H6Br2N2S, CAS is 79247-77-1, about An infrared study of rotational isomerism in thiazole-2-carboxylates. Author is Kaye, Perry T.; Meakins, G. Denis; Willbe, Charles; Williams, Peter R..

Twenty-five alkyl thiazole-2-carboxylates with a range of 4- and 5-substituents were prepared through the Hantzsch synthesis. E.g., cyclocondensation reaction of (H2N)2CS with MeCOCH2Br followed by bromination, oxidation, and alkylation gave the thiazole esters I (R = Me, Et). Solutions of these esters show well resolved doublets in the carbonyl IR spectra, due to rotational isomers. The higher wave number components were assigned to the more polar carbonyl O,S-anti-s-trans rotamers and those at lower wave number to the O,S-syn-s-trans forms. Small, but systematic, differences between the Me esters were noted.

There is still a lot of research devoted to this compound(SMILES：NC1=NC(C)=C(Br)S1.[H]Br)Reference of 5-Bromo-4-methyl-thiazol-2-ylamine hydrobromide, and with the development of science, more effects of this compound(79247-77-1) can be discovered.

Reference:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics