Month: March 2022

In organic chemistry, atoms other than carbon and hydrogen are generally referred to as heteroatoms. The most common heteroatoms are nitrogen, oxygen and sulfur. Now I present to you 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, mainly applied to LY3130481 preparation AMPA receptor antagonist TARP gamma8 anticonvulsant epilepsy, Product Details of 84547-64-8.

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.

There is still a lot of research devoted to this compound(SMILES：CN1N=C(CCl)C=C1)Product Details of 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

The reaction of an aromatic heterocycle with a proton is called a protonation. One of articles about this theory is 《New synthesis and properties of 3-alkyl-, 3-chloroalkyl-, 3-perfluoroalkyl-, and 3-aryl-1-methyl-5-halopyrazoles from chloro(bromo)vinyl ketones and N,N-dimethylhydrazine》. Authors are Levkovskaya, G. G.; Bozhenkov, G. V.; Larina, L. I.; Mirskova, A. N..The article about the compound:3-(Chloromethyl)-1-methyl-1H-pyrazolecas:84547-64-8,SMILESS:CN1N=C(CCl)C=C1).SDS of cas: 84547-64-8. Through the article, more information about this compound (cas:84547-64-8) is conveyed.

A new regioselective heterocyclization was revealed in the reaction of 2-chloro- and 2,2-dichloro(bromo)vinyl ketones with N,N-dimethylhydrazine to afford 3-substituted 1-methyl-5-halopyrazoles. The reaction is accompanied by elimination of Me halide and formation of up to 90% of N,N,N-trimethylhydrazinium halide as the second product.

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

Application In Synthesis of 3-(Chloromethyl)-1-methyl-1H-pyrazole. 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 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.

If you want to learn more about this compound(3-(Chloromethyl)-1-methyl-1H-pyrazole)Application In Synthesis of 3-(Chloromethyl)-1-methyl-1H-pyrazole, you may wish to communicate with the author of the article,or consult the relevant literature 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: 3-(Chloromethyl)-1-methyl-1H-pyrazole( cas:84547-64-8 ) is researched.Product Details of 84547-64-8.Bozhenkov, G. V.; Savosik, V. A.; Klyba, L. V.; Zhanchipova, E. R.; Mirskova, A. N.; Levkovskaya, G. G. published the article 《1-Alkylpyrazoles and 1-alkyl-5-chloropyrazoles from halovinyl ketones and 1,1-dialkylhydrazines》 about this compound( cas:84547-64-8 ) in Russian Journal of Organic Chemistry. Keywords: ketone chloro vinyl heterocyclization hydrazine dialkyl; pyrazole alkyl chloro preparation. Let’s learn more about this compound (cas:84547-64-8).

Regioselective heterocyclization of chlorovinyl ketones R1COCH:C(R2)Cl (R1 = Me, R2 = H; R1 = n-Pr, R2 = H, Cl; R1 = CH2Cl, R2 = H) with 1,1-dialkyl-hydrazines NH2N(R3)2 (R3 = Me, n-Bu) to pyrazoles I involved intermediate formation of the corresponding dialkylhydrazones II. The mass spectrum fragmentation pattern of chlorine-containing pyrazoles I (R1 = CH2Cl, R2 = H, R3 = Me; R1 = n-Pr, R2 = Cl, R3 = Me) depended on the position of the halogen atom.

If you want to learn more about this compound(3-(Chloromethyl)-1-methyl-1H-pyrazole)Product Details of 84547-64-8, you may wish to communicate with the author of the article,or consult the relevant literature related to this compound(84547-64-8).

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

Formula: C4H6Br2N2S. 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-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.

If you want to learn more about this compound(5-Bromo-4-methyl-thiazol-2-ylamine hydrobromide)Formula: C4H6Br2N2S, you may wish to communicate with the author of the article,or consult the relevant literature related to this compound(79247-77-1).

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

Application of 84547-64-8. 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: 3-(Chloromethyl)-1-methyl-1H-pyrazole, is researched, Molecular C5H7ClN2, CAS is 84547-64-8, about 1-Alkylpyrazoles and 1-alkyl-5-chloropyrazoles from halovinyl ketones and 1,1-dialkylhydrazines. Author is Bozhenkov, G. V.; Savosik, V. A.; Klyba, L. V.; Zhanchipova, E. R.; Mirskova, A. N.; Levkovskaya, G. G..

Regioselective heterocyclization of chlorovinyl ketones R1COCH:C(R2)Cl (R1 = Me, R2 = H; R1 = n-Pr, R2 = H, Cl; R1 = CH2Cl, R2 = H) with 1,1-dialkyl-hydrazines NH2N(R3)2 (R3 = Me, n-Bu) to pyrazoles I involved intermediate formation of the corresponding dialkylhydrazones II. The mass spectrum fragmentation pattern of chlorine-containing pyrazoles I (R1 = CH2Cl, R2 = H, R3 = Me; R1 = n-Pr, R2 = Cl, R3 = Me) depended on the position of the halogen atom.

If you want to learn more about this compound(3-(Chloromethyl)-1-methyl-1H-pyrazole)Application of 84547-64-8, you may wish to communicate with the author of the article,or consult the relevant literature related to this compound(84547-64-8).

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

Epoxy compounds usually have stronger nucleophilic ability, because the alkyl group on the oxygen atom makes the bond angle smaller, which makes the lone pair of electrons react more dissimilarly with the electron-deficient system. 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.Category: amides-buliding-blocks.

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.

If you want to learn more about this compound(3-(Chloromethyl)-1-methyl-1H-pyrazole)Category: amides-buliding-blocks, you may wish to communicate with the author of the article,or consult the relevant literature related to this compound(84547-64-8).

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

Most of the natural products isolated at present are heterocyclic compounds, so heterocyclic compounds occupy an important position in the research of organic chemistry. A compound: 84547-64-8, is researched, SMILESS is CN1N=C(CCl)C=C1, Molecular C5H7ClN2Journal, Article, Journal of Medicinal Chemistry 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, 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., the main research direction is LY3130481 preparation AMPA receptor antagonist TARP gamma8 anticonvulsant epilepsy.Product Details of 84547-64-8.

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.

If you want to learn more about this compound(3-(Chloromethyl)-1-methyl-1H-pyrazole)Product Details of 84547-64-8, you may wish to communicate with the author of the article,or consult the relevant literature related to this compound(84547-64-8).

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

Kaye, Perry T.; Meakins, G. Denis; Willbe, Charles; Williams, Peter R. published the article 《An infrared study of rotational isomerism in thiazole-2-carboxylates》. Keywords: thiazolecarboxylate IR rotational isomerism; Hantzsch thiourea bromoacetone; bromomethylthiazolecarboxylate ethyl methyl; methylthiazolecarboxylate bromo ethyl methyl; carboxylate thiazole IR rotational isomerism.They researched the compound: 5-Bromo-4-methyl-thiazol-2-ylamine hydrobromide( cas:79247-77-1 ).Category: amides-buliding-blocks. 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:79247-77-1) here.

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.

If you want to learn more about this compound(5-Bromo-4-methyl-thiazol-2-ylamine hydrobromide)Category: amides-buliding-blocks, you may wish to communicate with the author of the article,or consult the relevant literature related to this compound(79247-77-1).

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

HPLC of Formula: 84547-64-8. 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. Compound: 3-(Chloromethyl)-1-methyl-1H-pyrazole, is researched, Molecular C5H7ClN2, CAS is 84547-64-8, about New synthesis and properties of 3-alkyl-, 3-chloroalkyl-, 3-perfluoroalkyl-, and 3-aryl-1-methyl-5-halopyrazoles from chloro(bromo)vinyl ketones and N,N-dimethylhydrazine.

A new regioselective heterocyclization was revealed in the reaction of 2-chloro- and 2,2-dichloro(bromo)vinyl ketones with N,N-dimethylhydrazine to afford 3-substituted 1-methyl-5-halopyrazoles. The reaction is accompanied by elimination of Me halide and formation of up to 90% of N,N,N-trimethylhydrazinium halide as the second product.

If you want to learn more about this compound(3-(Chloromethyl)-1-methyl-1H-pyrazole)HPLC of Formula: 84547-64-8, you may wish to communicate with the author of the article,or consult the relevant literature related to this compound(84547-64-8).

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