Day: December 2, 2022

Zhao, Hui published the artcileN-alkylation of N-H compounds in N, N-dimethylformamide dialkyl acetal, Synthetic Route of 930-36-9, the publication is Youji Huaxue (2019), 39(2), 434-442, database is CAplus.

The N, N-dimethylformamide dialkyl acetal was used as the alkyl source to achieve different nitrogen alkylation reactions of N-H compounds The reaction has the advantages of cheap raw materials, easy operation, mild reaction conditions, broad substrate scope and no metal participation. By studying the effects of solvents, temperature, reaction time, and the amount of N, N-dimethylformamide dialkyl acetal on the reaction, the optimal reaction conditions were obtained. The effect of different N, N-dimethylformamide dialkyl acetals on the alkylation ability of the substrate was investigated.

Youji Huaxue 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 C18H15N3O3, Synthetic Route of 930-36-9.

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

Igarashi, Mami published the artcileCatalytic oxidation of 2,4,6-tribromophenol using iron(III) complexes with imidazole, pyrazole, triazine and pyridine ligands, Recommanded Product: 1-Methylpyrazole, the publication is Journal of Molecular Catalysis A: Chemical (2016), 100-106, database is CAplus.

Five types of non-heme iron complexes, coordinated with imidazole, pyrazole, triazine and pyridine ligands, which had been previously synthesized, were used in the following studies. Among these complexes, the mer-[FeCl₃(terpy)] complex showed the highest catalytic activity for the oxidative degradation of 2,4,6-tribromophenol (TrBP) using KHSO₅ as an oxygen donor. The turnover numbers for the degradation and debromination of TrBP in the mer-[FeCl₃(terpy)]/KHSO₅ catalytic system were estimated to be 1890 ± 1 and 4020 ± 216, resp. The catalytic activity was significantly inhibited at pH 4-7 in the presence of a humic acid, a major component of landfill leachates. However, the percent of TrBP degradation and debromination increased at pH 8. GC/MS analyses showed that a major oxidation product was 2,6-dibromo-p-benzoquinone (DBQ) and its level decreased with increasing reaction time, suggesting that organic acids (identified by LC/TOF-MS) are formed via the ring-cleavage of DBQ. Mineralization to CO₂ was observed to be 15% as a result of the oxidation for a 3 h period, where TOC values before and after the reaction were measured. Absorption spectra of mer-[FeCl₃(terpy)] with m-chloroperoxybenzoic acids as an oxygen donor in acetonitrile showed that a center metal, Fe, formed a peroxide complex with the oxygen donor.

Journal of Molecular Catalysis A: Chemical 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, Recommanded Product: 1-Methylpyrazole.

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

Liu, Deng-Feng published the artcileRing-opening copolymerization of epoxide and dianhydride in the presence of manganese(III) asymmetrical bis-Schiff base catalysts, Related Products of pyrazoles-derivatives, the publication is Canadian Journal of Chemistry (2014), 92(11), 1098-1105, database is CAplus.

Based on a series of asym. bis-Schiff base H₂Lⁿ (n = 1-4) ligands with different electronic and steric effects, a series of [Mn(Lⁿ)Cl] complexes 1-4 are obtained and shown to be effective catalysts in ring-opening copolymerization of epoxides and dianhydrides. Through the structure design, the input of electron-withdrawing bromine substituent para to the phenoxide group of the complexes is considerately beneficial to the improved activities. Moreover, steric and electronic effects of the suitable MeO substituent at the ortho orientation on the phenoxide group may both play a role in the formation of alternating ring-opening copolymers under the identical reaction conditions. In three cocatalysts tested, n-Bu₄NBr is pos. to monomer conversion and chain growth of polymer.

Canadian Journal of Chemistry published new progress about 4551-69-3. 4551-69-3 belongs to pyrazoles-derivatives, auxiliary class Benzenes, name is 4-Benzoyl-5-methyl-2-phenyl-2,4-dihydro-3H-pyrazol-3-one, and the molecular formula is C17H14N2O2, Related Products of pyrazoles-derivatives.

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

Liu, Deng-Feng published the artcileRing-opening copolymerization of epoxides and anhydrides using manganese(III) asymmetrical Schiff base complexes as catalysts, Formula: C17H14N2O2, the publication is RSC Advances (2015), 5(5), 3854-3859, database is CAplus.

Based on a series of asym. Schiff base H₂Lⁿ (n = 1-4) ligands with different electronic and steric effects, a series of [Mn(Lⁿ)Cl] complexes were obtained and shown to be effective catalysts in cyclohexene oxide and maleic anhydride, cyclohexene oxide and phthalic anhydride, styrene oxide and maleic anhydride or styrene oxide and phthalic anhydride ring-opening copolymerizations Through the structure design, the input of the electron-withdrawing Br substituent para to the phenoxide group of the complexes is quite beneficial to the improved activities. Moreover, both steric and electronic effects of a suitable MeO substituent at the ortho position of the phenoxide group have much more influence on the formation of alternating ring-opening copolymers than that of selected reaction conditions.

RSC Advances published new progress about 4551-69-3. 4551-69-3 belongs to pyrazoles-derivatives, auxiliary class Benzenes, name is 4-Benzoyl-5-methyl-2-phenyl-2,4-dihydro-3H-pyrazol-3-one, and the molecular formula is C17H14N2O2, Formula: C17H14N2O2.

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

Song, Zongqiang published the artcileSynthesis of 1,3-Dioxepine-Fused (Tricyclic) Bispyrazoles Involved with Pyrazolone Derivatives and Dichloromethane, Application of 1-(2-Chlorophenyl)-3-methyl-5-pyrazolone, the publication is Journal of Organic Chemistry (2022), 87(6), 4284-4290, database is CAplus and MEDLINE.

A simple and novel method was described for the synthesis of novel 1,3-dioxepine-fused (tricyclic) bispyrazoles I (R = H, Me, t-Bu, Cl, etc.; R¹ = H; RR¹ = -CH=CH-CH=CH-; R² = Me, CF₃, i-Pr, Ph; R³ = H, Me). It involves a Cs₂CO₃ mediated O-alkylation of readily available pyrazolone derivatives II with dichloromethane as methylene source followed by PhI(OAc)₂-mediated intramol. oxidative biheteroaryl coupling under mild conditions. This scalable protocol was applied for the preparation of valuable and novel 1,3-dioxepine-fused (tricyclic) bispyrazoles I which could find potential applications in medicinal or material chem.

Journal of Organic Chemistry 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 C10H19NO3, Application of 1-(2-Chlorophenyl)-3-methyl-5-pyrazolone.

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

Tang, Cheng-Ke published the artcileCombining Organocatalysis and Iodine Catalysis: One-Pot Sequential Catalytic Synthesis of Chiral Spirodihydrobenzofuran Pyrazolones and Spirodihydrobenzofuran Oxindoles, Formula: C10H9ClN2O, the publication is Organic Letters (2018), 20(18), 5840-5844, database is CAplus and MEDLINE.

O-Hydroxystyrenes such as (E)-2-HOC₆H₄CH:CHNO₂ underwent diastereoselective and enantioselective oxidative spirocyclization reactions (via sequential Michael addition, iodination, and cyclization reactions) with pyrazolones and N-Boc oxindoles in the presence of a nonracemic squaramide and a nonracemic alkaloid-derived thiourea to give spirobenzofuranpyrazolones such as I and spirobenzofuranoxindoles such as II, resp.

Organic 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 CBF6K, Formula: C10H9ClN2O.

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

Liu, Jiang published the artcileRing-opening copolymerization of CHO and MA catalyzed by the asymmetrical Cr(III)-bis-Schiff-base complex, Application of 4-Benzoyl-5-methyl-2-phenyl-2,4-dihydro-3H-pyrazol-3-one, the publication is Inorganic Chemistry Communications (2017), 86-88, database is CAplus.

Using an asym. Cr(III)-bis-Schiff-base complex [Cr(L)Cl] (1; H₂L obtained from condensation of 5-bromo-salicylaldehyde and HL⁰ (Z)-4-((2-aminophenylimino)(phenyl)methyl)-3-methyl-1H-pyrazol-5(4H)-one) as the catalyst, bulk solvent-free ring-opening copolymerization of CHO (cyclohexene oxide) and MA (maleic anhydride) in the presence of cocatalyst DMAP (4-(dimethylamino)-pyridine) was effectively realized, in which, on the condition of low 1/DMAP concentration for a controllable polymerization, perfectly alternating polyester while not poly(ester-coether) could be obtained.

Inorganic Chemistry Communications published new progress about 4551-69-3. 4551-69-3 belongs to pyrazoles-derivatives, auxiliary class Benzenes, name is 4-Benzoyl-5-methyl-2-phenyl-2,4-dihydro-3H-pyrazol-3-one, and the molecular formula is C17H14N2O2, Application of 4-Benzoyl-5-methyl-2-phenyl-2,4-dihydro-3H-pyrazol-3-one.

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

Zhao, Xiao-Yun published the artcileSynthesis and characterization of N-heterocyclic carbene-palladium(II) chlorides-1-methylindazole and -1-methylpyrazole complexes and their catalytic activity toward C-N coupling of aryl chlorides, Category: pyrazoles-derivatives, the publication is RSC Advances (2016), 6(29), 24484-24490, database is CAplus.

A series of N-heterocyclic carbene-palladium(II) chlorides-1-methylindazole and -1-methylpyrazole complexes was successfully synthesized and fully characterized by x-ray single crystal diffraction. In addition, initial investigations of their catalytic activity showed that they were efficient catalysts in the C-N coupling of primary and secondary amines with aryl chlorides at low catalyst loadings.

RSC Advances 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 C27H29N5, Category: pyrazoles-derivatives.

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

Yu, Jiang published the artcileDiscovery and biological evaluation of darolutamide derivatives as inhibitors and down-regulators of wild-type AR and the mutants, Product Details of C10H6ClN3, the publication is European Journal of Medicinal Chemistry (2019), 111608, database is CAplus and MEDLINE.

Androgen receptor (AR) has been a target of prostate cancer (PC) for nearly six decades. Recently, down-regulating or degrading AR and the mutants especially the splice variant 7 (AR-V7) lacking ligand binding domain (LBD) emerged as an advantageous therapeutic approach to overcome drug resistance. Here, the structural modification of darolutamide resulted in the discovery of dual-action AR inhibitors and down-regulators. Unlike other traditional AR antagonists targeting the AR-LBD, compounds 4k and 4b not only inhibit the activities of wt-AR and AR-F876L mutant but also down-regulate the protein expression of full-length (AR-full) and AR variant 7 (AR-V7) at mRNA level. In cell proliferation assays, compounds 4k and 4b exhibited better antiproliferative activities than darolutamide and enzalutamide against AR-V7-pos. 22Rv1 cells and VCaP cells. In addition, 4k demonstrated better antitumor activity than clin. used enzalutamide in castration-resistant VCaP xenograft model. Collectively, combining the activities of AR inhibition and down-regulation, compound 4k is proposed as an advantageous lead compound to disrupt AR signaling and overcome resistance.

European Journal of Medicinal Chemistry published new progress about 1297537-37-1. 1297537-37-1 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Chloride,Nitrile,Benzene, name is 2-Chloro-4-(1H-pyrazol-5-yl)benzonitrile, and the molecular formula is C14H20BNO3, Product Details of C10H6ClN3.

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

Rong, Deqin published the artcileStructure-Aided Design, Synthesis, and Biological Evaluation of Potent and Selective Non-Nucleoside Inhibitors Targeting Protein Arginine Methyltransferase 5, Application In Synthesis of 930-36-9, the publication is Journal of Medicinal Chemistry (2022), 65(11), 7854-7875, database is CAplus and MEDLINE.

PRMT5 is a major type II protein arginine methyltransferase and plays important roles in diverse cellular processes. Overexpression of PRMT5 is implicated in various types of cancer. Many efforts have been made to develop potent and selective PRMT5 inhibitors, the most potent of which is usually derived from nucleoside structures. Here, we designed a novel series of non-nucleoside PRMT5 inhibitors through the structure-aided drug design approach. SAR exploration and metabolic stability optimization led to the discovery of compound 41 as a potent PRMT5 inhibitor with good selectivity. Addnl., compound 41 exerted antiproliferative effects against A375 cells by inducing apoptosis and potently inhibited the methyltransferase activity of PRMT5 in cells. Moreover, it showed attractive pharmacokinetic properties and markedly suppressed the tumor growth in an A375 tumor xenograft model. These results clearly indicate that 41 is a highly potent and selective non-nucleoside PRMT5 inhibitor.

Journal of Medicinal 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, Application In Synthesis of 930-36-9.

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