Month: November 2022

Parmar, Narsidas J. published the artcileCatalyst-and solvent-free one-pot synthesis of some novel polyheterocycles from aryldiazenyl salicylaldehyde derivatives, Application of 1-(2-Chlorophenyl)-3-methyl-5-pyrazolone, the publication is RSC Advances (2012), 2(7), 3069-3075, database is CAplus.

A catalyst- and solvent-free domino/Knoevenagel-hetero-Diels-Alder (DKHDA) reaction of allyl/prenyl ether-tethered aryldiazenylsalicylaldehydes with corresponding pyrazolones and heterocyclic 1,3-diketones is described. Subsequent reduction of aryldiazenylpolyheterocycles, thus obtained in high yields (70-86%), afforded amino frameworks with anticipated biol. activity. While in a conventional procedure, no reaction was observed without activation of an allyl-based substrate, an excellent yield was achieved at higher temperature For a prenyl based substrate, however it underwent smoothly to form a desired cyclized product. The stereochem. of the compound was confirmed by various NMR experiments and a single crystal X-ray diffraction anal.

RSC Advances published new progress about 14580-22-4. 14580-22-4 belongs to pyrazoles-derivatives, auxiliary class Organic Pigment, name is 1-(2-Chlorophenyl)-3-methyl-5-pyrazolone, and the molecular formula is C10H9ClN2O, Application of 1-(2-Chlorophenyl)-3-methyl-5-pyrazolone.

Referemce:
https://en.wikipedia.org/wiki/Pyrazole,
Pyrazoles – an overview | ScienceDirect Topics

Parmar, Narsidas J. published the artcileAn efficient domino reaction in ionic liquid: Synthesis and biological evaluation of some pyrano- and thiopyrano-fused heterocycles, COA of Formula: C10H9ClN2O, the publication is Bioorganic & Medicinal Chemistry Letters (2013), 23(6), 1656-1661, database is CAplus and MEDLINE.

An improved domino/Knoevenagel-hetero-Diels-Alder reaction of two new aldehyde substrates; 7-olefinoxy-coumarin-8-carbaldehyde and 2-alkensulfanyl-quinoline-3-carbaldehyde, with pyrazolones was studied in the ionic liquid triethylammonium acetate (TEAA), affording a series of pyrazolopyran annulated-pyrano-fused coumarins, and thiopyrano-fused quinolones. Besides acting as the catalyst, since no addnl. catalyst used, the ionic liquid TEAA also provided an easy recovery. In the polyheterocycles prepared, the cis-fusion of the two pyranyl rings has been inferred from 2D NMR COSY and NOESY experiments All are good antitubercular agents, as they are found active against Mycobacterium tuberculosis H37Rv, and antibacterial agents, as they are found active against three Gram-pos. (Streptococcus pneumoniae, Clostridium tetani, Bacillus subtilis) and three Gram-neg. (Salmonella typhi, Vibrio cholerae, Escherichia coli) bacteria.

Bioorganic & Medicinal Chemistry Letters published new progress about 14580-22-4. 14580-22-4 belongs to pyrazoles-derivatives, auxiliary class Organic Pigment, name is 1-(2-Chlorophenyl)-3-methyl-5-pyrazolone, and the molecular formula is C10H9ClN2O, COA of Formula: C10H9ClN2O.

Referemce:
https://en.wikipedia.org/wiki/Pyrazole,
Pyrazoles – an overview | ScienceDirect Topics

Malik, G. M. published the artcileSynthesis, characterization and dyeing properties of mono azo pyrazolone dyes based on 2-amino 5-methyl thiazole, Formula: C10H9ClN2O, the publication is International Journal of Chemistry (Mumbai, India) (2015), 4(3), 284-294, database is CAplus.

Different substituted monoazo pyrazolone dyes from N⁴-(5-methyl-1,3-thiazol-2-yl)-1,3-thiazole-2,4-diamine have been synthesized. The condensation of 5-Me 2-amino thiazole with chloroacetylchloride yielded 2-chloro-N-(5- methyl-1,3-thiazol-2-yl)acetamide which was reacted with thiourea at reflux temperature using methanol and cyclized to yield N⁴-(5-methyl-1,3-thiazol-2-yl)-1,3-thiazole-2,4-diamine. This was diazotized and coupled with various substituted pyrazolones to give a new series of pyrazolone dyes, which were characterized using elemental anal., UV, IR and 1H NMR spectra. Dyeing performance and fastness properties were evaluated by applying them on nylon and polyester fabrics.

International Journal of Chemistry (Mumbai, India) published new progress about 14580-22-4. 14580-22-4 belongs to pyrazoles-derivatives, auxiliary class Organic Pigment, name is 1-(2-Chlorophenyl)-3-methyl-5-pyrazolone, and the molecular formula is C10H9ClN2O, Formula: C10H9ClN2O.

Referemce:
https://en.wikipedia.org/wiki/Pyrazole,
Pyrazoles – an overview | ScienceDirect Topics

O’Sullivan, Leonie published the artcileRegioselective Synthesis of C3-Hydroxyarylated Pyrazoles, Safety of 1-Methylpyrazole, the publication is Journal of Organic Chemistry (2022), 87(1), 846-854, database is CAplus and MEDLINE.

The first regioselective route to C3-hydroxyarylated pyrazoles obtained through reaction of pyrazole N-oxides with arynes using mild conditions is reported. Importantly, this method does not require the C4 and C5 positions of the pyrazole to be functionalized to observe regioselectivity. Using this method, authors completed the synthesis of a recently reported JAK 1/2 inhibitor. Authors’ synthesis produces the desired product in 4 steps from com. available starting materials.

Journal of Organic Chemistry published new progress about 930-36-9. 930-36-9 belongs to pyrazoles-derivatives, auxiliary class Pyrazole, name is 1-Methylpyrazole, and the molecular formula is C4H6N2, Safety of 1-Methylpyrazole.

Referemce:
https://en.wikipedia.org/wiki/Pyrazole,
Pyrazoles – an overview | ScienceDirect Topics

Venier, Olivier published the artcilePyrrolidine-pyrazole ureas as potent and selective inhibitors of 11β-hydroxysteroid-dehydrogenase type 1, Application of 1H-Pyrazole-4-boronic acid, the publication is Bioorganic & Medicinal Chemistry Letters (2011), 21(8), 2244-2251, database is CAplus and MEDLINE.

A High Throughput Screening campaign allowed the identification of a novel class of ureas as 11β-HSD1 inhibitors. Rational chem. optimization provided potent and selective inhibitors of both human and murine 11β-HSD1 with an appropriate ADME profile and ex vivo activity in target tissues.

Bioorganic & Medicinal Chemistry Letters published new progress about 763120-58-7. 763120-58-7 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Boronic acid and ester,Boronic Acids,Boronic acid and ester, name is 1H-Pyrazole-4-boronic acid, and the molecular formula is C4H3Cl2N3, Application of 1H-Pyrazole-4-boronic acid.

Referemce:
https://en.wikipedia.org/wiki/Pyrazole,
Pyrazoles – an overview | ScienceDirect Topics

Venier, Olivier published the artcilePyrrolidine-pyrazole ureas as potent and selective inhibitors of 11β-hydroxysteroid-dehydrogenase type 1, Recommanded Product: (1H-Pyrazol-5-yl)boronic acid, the publication is Bioorganic & Medicinal Chemistry Letters (2011), 21(8), 2244-2251, database is CAplus and MEDLINE.

A High Throughput Screening campaign allowed the identification of a novel class of ureas as 11β-HSD1 inhibitors. Rational chem. optimization provided potent and selective inhibitors of both human and murine 11β-HSD1 with an appropriate ADME profile and ex vivo activity in target tissues.

Bioorganic & Medicinal Chemistry Letters published new progress about 724710-02-5. 724710-02-5 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Boronic acid and ester,Pyrazole,Boronic Acids,Boronic acid and ester, name is (1H-Pyrazol-5-yl)boronic acid, and the molecular formula is C11H14BNO3, Recommanded Product: (1H-Pyrazol-5-yl)boronic acid.

Referemce:
https://en.wikipedia.org/wiki/Pyrazole,
Pyrazoles – an overview | ScienceDirect Topics

Dwyer, Michael P. published the artcileDiscovery of pyrazolo[1,5-a]pyrimidine-based CHK1 inhibitors: A template-based approach-Part 1, Recommanded Product: (1H-Pyrazol-5-yl)boronic acid, the publication is Bioorganic & Medicinal Chemistry Letters (2011), 21(1), 467-470, database is CAplus and MEDLINE.

The synthesis and hit-to-lead SAR development of a pyrazolo[1,5-a]pyrimidine hit I is described leading to a series of potent, selective CHK1 inhibitors such as compound II. The further utility of the pyrazolo[1,5-a]pyrimidine template for the development of potent, selective kinase inhibitors is detailed.

Bioorganic & Medicinal Chemistry Letters published new progress about 724710-02-5. 724710-02-5 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Boronic acid and ester,Pyrazole,Boronic Acids,Boronic acid and ester, name is (1H-Pyrazol-5-yl)boronic acid, and the molecular formula is C3H5BN2O2, Recommanded Product: (1H-Pyrazol-5-yl)boronic acid.

Referemce:
https://en.wikipedia.org/wiki/Pyrazole,
Pyrazoles – an overview | ScienceDirect Topics

Dorgan, Roderick J. J. published the artcileN-Alkyl and N-acyl derivatives of 3(5)-aminopyrazole, Safety of 3-Acetamidopyrazole, the publication is Journal of Chemical Research, Synopses (1979), 198, database is CAplus.

3(5)-Aminopyrazole (I) underwent benzylation on the exocyclic N to give II [R = H, R¹ = R² = CH₂Ph; R = R¹ = H, R² = CH₂Ph (III)] whereas acetylation gave II (R = R¹ = Ac, R² = H), which on subsequent benzylation gave II (R = CH₂Ph, R¹ = Ac, R² = H) and IV (R = CH₂Ph, R¹ = H, R² = Ac) (V). In the presence of MeCOCH₂CO₂Et, III gave the pyrazolo[1,5-a]pyrimidine VI (R = CH₂Ph) which was debenzylated to VI (R = H). PhCH₂NHNH₂ reacted with CH₂:CClCN to give IV (R = CH₂Ph, R¹ = R² = H) which on acetylation gave V. I with phthalic anhydride gave II (R = H, NR¹R² = phthalimido) which on benzylation and benzyloxymethylation gave II (R = CH₂Ph, R¹R² as before) and IV (R = CH₂OCH₂Ph, R¹R² as before), resp.

Journal of Chemical Research, Synopses published new progress about 3553-12-6. 3553-12-6 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Amine,Amide, name is 3-Acetamidopyrazole, and the molecular formula is C5H7N3O, Safety of 3-Acetamidopyrazole.

Referemce:
https://en.wikipedia.org/wiki/Pyrazole,
Pyrazoles – an overview | ScienceDirect Topics

Nguyen, Diem N. published the artcileCalcitonin gene-related peptide (CGRP) receptor antagonists: Investigations of a pyridinone template, Related Products of pyrazoles-derivatives, the publication is Bioorganic & Medicinal Chemistry Letters (2008), 18(2), 755-758, database is CAplus and MEDLINE.

In our effort to find potent, orally bioavailable CGRP receptor antagonists for the treatment of migraine, a novel series based on a pyridinone template was investigated. After optimizing the privileged structure and the placement of the attached Ph ring, systematic SAR was carried out on both the N-alkyl and C-5 aryl substituents. Several analogs with good potency and pharmacokinetic profiles were identified.

Bioorganic & Medicinal Chemistry Letters published new progress about 724710-02-5. 724710-02-5 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Boronic acid and ester,Pyrazole,Boronic Acids,Boronic acid and ester, name is (1H-Pyrazol-5-yl)boronic acid, and the molecular formula is C3H5BN2O2, Related Products of pyrazoles-derivatives.

Referemce:
https://en.wikipedia.org/wiki/Pyrazole,
Pyrazoles – an overview | ScienceDirect Topics

Parmar, Narsidas J. published the artcileTriethylammonium acetate-mediated domino-Knoevenagel-hetero-Diels-Alder reaction: synthesis of some angular polyheterocycles, Computed Properties of 14580-22-4, the publication is Monatshefte fuer Chemie (2013), 144(6), 865-878, database is CAplus.

A solvent-cum catalyst, ionic liquid triethylammonium acetate-mediated one-pot procedure for the synthesis of some new angular benzopyrano[3,4-c]pyrano-fused pyrazoles, e.g., I, all of which incorporate a tertiary ring junction carbon, has been developed. The stereochem. of the products has been confirmed by single-crystal X-ray diffraction data.

Monatshefte fuer Chemie published new progress about 14580-22-4. 14580-22-4 belongs to pyrazoles-derivatives, auxiliary class Organic Pigment, name is 1-(2-Chlorophenyl)-3-methyl-5-pyrazolone, and the molecular formula is C10H9ClN2O, Computed Properties of 14580-22-4.

Referemce:
https://en.wikipedia.org/wiki/Pyrazole,
Pyrazoles – an overview | ScienceDirect Topics