Category: 141032-72-6

Miki, Yasuyoshi et al. published their research in Heterocycles in 1996 | CAS: 141032-72-6

Pyrazolo[1,5-a]pyridin-4-ol (cas: 141032-72-6) belongs to pyrazole derivatives. Pyrazole and its derivatives are considered a pharmacologically important active scaffold that possesses almost all types of pharmacological activities. The presence of both electronegative nitrogen atoms in the pyrazole ring reduces the electron density of the C3- and C5-positions leaving electron density of C4-position unaltered. Thus the C4-position is vulnerable to electrophilic attack. The C3 electrophilic-position may undergo deprotonation in the presence of a strong base leading to ring opening.Application of 141032-72-6

Synthesis of 1-isopropylamino-3-(pyrazolo[1,5-a]pyridyloxy)-2-propanols was written by Miki, Yasuyoshi;Tasaka, Junko;Uemura, Kyoko;Miyazeki, Kunihiro;Yamada, Jun. And the article was included in Heterocycles in 1996.Application of 141032-72-6 The following contents are mentioned in the article:

Treatment of the 4-hydroxypyrazolo[1,5-a]pyridine with glycidyl tosylate in the presence of base, followed by reaction with isopropylamine gave 1-isopropylamino-3-(pyrazolo[1,5-a]pyrid-4-yloxy)-2-propanol. In a similar manner, 1-isopropylamino-3-(pyrazolo[1,5-a]pyrid-6- and 1-isopropylamino-3-(pyrazolo[1,5-a]pyrid-3-yloxy)-2-propanol were also prepared This study involved multiple reactions and reactants, such as Pyrazolo[1,5-a]pyridin-4-ol (cas: 141032-72-6Application of 141032-72-6).

Pyrazolo[1,5-a]pyridin-4-ol (cas: 141032-72-6) belongs to pyrazole derivatives. Pyrazole and its derivatives are considered a pharmacologically important active scaffold that possesses almost all types of pharmacological activities. The presence of both electronegative nitrogen atoms in the pyrazole ring reduces the electron density of the C3- and C5-positions leaving electron density of C4-position unaltered. Thus the C4-position is vulnerable to electrophilic attack. The C3 electrophilic-position may undergo deprotonation in the presence of a strong base leading to ring opening.Application of 141032-72-6

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

Moeller, Dorothee et al. published their research in Journal of Medicinal Chemistry in 2014 | CAS: 141032-72-6

Pyrazolo[1,5-a]pyridin-4-ol (cas: 141032-72-6) belongs to pyrazole derivatives. Pyrazole and its derivatives are considered a pharmacologically important active scaffold that possesses almost all types of pharmacological activities. Pyrazoles can be selectively lithiated at different carbons and subsequently react with electrophiles depending on the substitution patterns.Synthetic Route of C7H6N2O

Functionally Selective Dopamine D2, D3 Receptor Partial Agonists was written by Moeller, Dorothee;Kling, Ralf C.;Skultety, Marika;Leuner, Kristina;Huebner, Harald;Gmeiner, Peter. And the article was included in Journal of Medicinal Chemistry in 2014.Synthetic Route of C7H6N2O The following contents are mentioned in the article:

Dopamine D2 receptor-promoted activation of Gαo over Gαi may increase synaptic plasticity and thereby might improve neg. symptoms of schizophrenia. Heterocyclic dopamine surrogates comprising a pyrazolo[1,5-a]pyridine moiety were synthesized and investigated for their binding properties when low- to subnanomolar Ki values were determined for D2L, D2S, and D3 receptors. Measurement of [35S]GTPγS incorporation at D2S coexpressed with G-protein subunits indicated significant bias for promotion of Gαo1 over Gαi2 coupling for several test compounds Functionally selective D2S activation was most striking for the carbaldoxime I (Gαo1, pEC50 = 8.87, Emax = 65%; Gαi2, pEC50 = 6.63, Emax = 27%). In contrast, the investigated 1,4-disubstituted aromatic piperazines (1,4-DAPs) behaved as antagonists for β-arrestin-2 recruitment, implying significant ligand bias for G-protein activation over β-arrestin-2 recruitment at D2S receptors. Ligand efficacy and selectivity between D2S and D3 activation were strongly influenced by regiochem. and the nature of functional groups attached to the pyrazolo[1,5-a]pyridine moiety. This study involved multiple reactions and reactants, such as Pyrazolo[1,5-a]pyridin-4-ol (cas: 141032-72-6Synthetic Route of C7H6N2O).

Pyrazolo[1,5-a]pyridin-4-ol (cas: 141032-72-6) belongs to pyrazole derivatives. Pyrazole and its derivatives are considered a pharmacologically important active scaffold that possesses almost all types of pharmacological activities. Pyrazoles can be selectively lithiated at different carbons and subsequently react with electrophiles depending on the substitution patterns.Synthetic Route of C7H6N2O

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

Ochiai, Koji et al. published their research in Bioorganic & Medicinal Chemistry Letters in 2012 | CAS: 141032-72-6

Pyrazolo[1,5-a]pyridin-4-ol (cas: 141032-72-6) belongs to pyrazole derivatives. The strategies for the synthesis of pyrazoles generally can be applied for the construction of indazoles. Protonation of pyrazole in strong acid leads to pyrazolium cations, which undergo electrophilic substitution preferentially at C3 rather than C4. The pyrazole anion is not reactive toward nucleophiles but is mostly reactive to electrophiles.Related Products of 141032-72-6

Phosphodiesterase inhibitors. Part 4: Design, synthesis and structure-activity relationships of dual PDE3/4-inhibitory fused bicyclic heteroaromatic-4,4-dimethylpyrazolones was written by Ochiai, Koji;Takita, Satoshi;Kojima, Akihiko;Eiraku, Tomohiko;Ando, Naoki;Iwase, Kazuhiko;Kishi, Tetsuya;Ohinata, Akira;Yageta, Yuichi;Yasue, Tokutaro;Adams, David R.;Kohno, Yasushi. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2012.Related Products of 141032-72-6 The following contents are mentioned in the article:

(-)-6-(7-Methoxy-2-trifluoromethylpyrazolo[1,5-a]pyridin-4-yl)-5-methyl-4,5-dihydro-3-(2H)-pyridazinone (KCA-1490) is a dual PDE3/4 inhibitor that exhibits potent combined bronchodilatory and anti-inflammatory activity. Here we show that a 4,4-dimethylpyrazolone subunit serves as an effective surrogate for the 5-methyl-4,5-dihydropyridazin-3(2H)-one ring of KCA-1490 while lacking a stereogenic center. The 2- and 7-substituents in the pyrazolo[1,5-a]pyridine subunit markedly influence the PDE-inhibitory profile and can be adjusted to afford either potent PDE4-selective inhibitors or dual PDE3/4 inhibitors. A survey of bicyclic heteroaromatic replacements for the pyrazolo[1,5-a]pyridine allowed further refinement of the inhibitory profile and identified 3-(8-methoxy-2-(trifluoromethyl)imidazo[1,2-a]pyridin-5-yl)-4,4-dimethyl-1H-pyrazol-5(4H)-one as an orally active, achiral KCA-1490 analog with well-balanced dual PDE3/4-inhibitory activity. This study involved multiple reactions and reactants, such as Pyrazolo[1,5-a]pyridin-4-ol (cas: 141032-72-6Related Products of 141032-72-6).

Pyrazolo[1,5-a]pyridin-4-ol (cas: 141032-72-6) belongs to pyrazole derivatives. The strategies for the synthesis of pyrazoles generally can be applied for the construction of indazoles. Protonation of pyrazole in strong acid leads to pyrazolium cations, which undergo electrophilic substitution preferentially at C3 rather than C4. The pyrazole anion is not reactive toward nucleophiles but is mostly reactive to electrophiles.Related Products of 141032-72-6

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics