Day: October 21, 2022

《Magnesium-Catalyzed N2-Regioselective Alkylation of 3-Substituted Pyrazoles》 was published in Synlett in 2020. These research results belong to Xu, Di; Frank, Lena; Nguyen, Tina; Stumpf, Andreas; Russell, David; Angelaud, Remy; Gosselin, Francis. HPLC of Formula: 15366-34-4 The article mentions the following:

A highly regioselective Mg-catalyzed alkylation of 3-substituted pyrazoles, I (R1 = Ph, Br, i-Pr, etc.; R2 = H, Br, CHO) and 2,4-dihydro-[1]benzopyrano[4,3-c]pyrazole has been developed to provide N2-alkylated regioisomers II (R3 = C(O)N(CH3)2, C6H5, [4-(morpholin-4-yl)piperidin-1-yl]carbonyl, etc.) and 2-(1H,4H-chromeno[4,3-c]pyrazol-1-yl)-N,N-dimethylacetamide. Using α-bromoacetates like iso-Pr 2-bromoacetate and acetamides R3CH2Br as alkylating agents, this new method was applied to a variety of 3-substituted and 3,4-disubstituted pyrazoles I to produce the N2-alkylated products II with high regioselectivities ranging from 76:24 to 99:1 and 44-90% yields. In the experimental materials used by the author, we found Methyl 1H-pyrazole-3-carboxylate(cas: 15366-34-4HPLC of Formula: 15366-34-4)

Methyl 1H-pyrazole-3-carboxylate(cas: 15366-34-4) belongs to pyrazoles. The application of pyrazole derivatives in the development of anticancer agents has been thoroughly investigated and verified. Moreover, the medicinal features of a number of natural products incorporating pyrazole moiety such as pyrazofurin, pyrazofurin B, pyrazole-3(5)-carboxylic acid and 4-methylpyrazole-3(5)-carboxylic acid have been reported.HPLC of Formula: 15366-34-4

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

Yang, Tao; Li, Xiaoqian; Deng, Shuang; Qi, Xiaotian; Cong, Hengjiang; Cheng, Hong-Gang; Shi, Liangwei; Zhou, Qianghui; Zhuang, Lin published an article in 2022. The article was titled 《From N-H Nitration to Controllable Aromatic Mononitration and Dinitration-The Discovery of a Versatile and Powerful N-Nitropyrazole Nitrating Reagent》, and you may find the article in JACS Au.Reference of Methyl 1H-pyrazole-3-carboxylate The information in the text is summarized as follows:

Herein,the identification of a powerful nitrating reagent, 5-methyl-1,3-dinitro-1H-pyrazole, from the N-nitro-type reagent library constructed using a practical N-H nitration method was reported. This nitrating reagent behaved as a controllable source of the nitronium ion, enabling mild and scalable nitration of a broad range of (hetero)arenes with good functional group tolerance. Of note, this nitration method was controlled by manipulating the reaction conditions to furnish mononitrated or dinitrated product selectively. The value of this method in medicinal chem. was well established by its efficient late-stage C-H nitration of complex biorelevant mols. D. functional theory (DFT) calculations and preliminary mechanistic studies reveal that the powerfulness and versatility of this nitrating reagent were due to the synergistic “”nitro effect”” and “”methyl effect””.Methyl 1H-pyrazole-3-carboxylate(cas: 15366-34-4Reference of Methyl 1H-pyrazole-3-carboxylate) was used in this study.

Methyl 1H-pyrazole-3-carboxylate(cas: 15366-34-4) belongs to pyrazoles. The application of pyrazole derivatives in the development of anticancer agents has been thoroughly investigated and verified. Moreover, the medicinal features of a number of natural products incorporating pyrazole moiety such as pyrazofurin, pyrazofurin B, pyrazole-3(5)-carboxylic acid and 4-methylpyrazole-3(5)-carboxylic acid have been reported.Reference of Methyl 1H-pyrazole-3-carboxylate

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

The author of 《Intramolecular Cyclization of Vinyldiazoacetates as a Versatile Route to Substituted Pyrazoles》 were Drikermann, Denis; Kerndl, Valerie; Goerls, Helmar; Vilotijevic, Ivan. And the article was published in Synlett in . Category: pyrazoles-derivatives The author mentioned the following in the article:

Vinyldiazo compounds undergo a thermal electrocyclization to form pyrazoles in yields of up to 95%. The reactions are operationally simple, use readily available starting materials, require no intervention of a catalyst, and enable the synthesis of mono-, di- and tri-substituted pyrazoles. With the ability to produce highly substituted pyrazoles and the flexibility in installing various types of substituents, this method constitutes a new entry to this valuable heterocyclic scaffold and may be of interest to all branches of the chem. industry. In addition to this study using Methyl 3-(p-tolyl)-1H-pyrazole-5-carboxylate, there are many other studies that have used Methyl 3-(p-tolyl)-1H-pyrazole-5-carboxylate(cas: 192701-73-8Category: pyrazoles-derivatives) was used in this study.

Methyl 3-(p-tolyl)-1H-pyrazole-5-carboxylate(cas: 192701-73-8) belongs to pyrazoles. Pyrazoles are commonly used scaffold molecules in drug discovery projects. The use of pyrazole derivatives is based on their analgesic, monoamine oxidase inhibitory, anti-inflammatory, antipyretic, neuroleptic, anticonvulsant, antiarrhythmic, sedative, muscle relaxant, antidiabetic and antibacterial activities. Category: pyrazoles-derivatives

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

Synthetic Route of C4H3F3N2In 2019 ,《Phosphine Ligand-Free Ruthenium Complexes as Efficient Catalysts for the Synthesis of Quinolines and Pyridines by Acceptorless Dehydrogenative Coupling Reactions》 appeared in ChemCatChem. The author of the article were Guo, Bin; Yu, Tian-Qi; Li, Hong-Xi; Zhang, Shi-Qi; Braunstein, Pierre; Young, David J.; Li, Hai-Yan; Lang, Jian-Ping. The article conveys some information:

A series of phosphine-free Ru(III)/Ru(II) complexes of NH functionalized N N N pincer ligands exhibit excellent activity for acceptorless dehydrogenative coupling (ADC) of secondary alcs. RCH(OH)CH2R1 [R = Ph, thiophen-2-yl, Et, etc.; R1 = H, Me, Et, n-Pr; RR1 = -(CH2)4-] and bicyclo[2.2.1]heptan-2-ol with 2-aminobenzyl 2-NH2-R3C6H3CH(R2)OH [R2 = H, Me; R3 = H, 5-Me, 4-Cl] or γ-amino alcs. R4CH(NH2)(CH2)2OH (R4 = Ph, Me) to quinolines I (R5 = H, 6-Me, 7-Cl), 1,2,3,4-tetrahydro-1,4-methanoacridine and pyridines II. Ru(III) complexes [LRuCl3] III (R6 = R7 = R8 = H, R9 = Cl; R6 = H, R7 = R8 = Me, R9 = Cl; R6 = R7 = H, R8 = Ph, R9 = Cl, etc.) were obtained by refluxing RuCl3.xH2O with the corresponding ligand in EtOH. Five Ru(II) complexes [LRu(DMSO-κS)Cl2] III [R9 = S(CH3)2(O)] were formed by reducing the corresponding Ru(III) complex in refluxing EtOH. The latter complexes could also be prepared directly by refluxing Ru(DMSO)4Cl2 with the corresponding ligand in EtOH. These Ru(III) and Ru(II) complexes, especially III exhibited high catalytic efficiency and broad functional group tolerance in ADC reactions of secondary alcs. with 2-aminobenzyl or γ-amino alcs. to quinolines I and pyridines II. A detail mechanistic study indicated that the Ru(III) complex III (R9 = Cl) was reduced into the Ru(II) species III (R9 = S(CH3)2(O)), which was the active catalytic center for ADC via a Ru-H/N-H bifunctional outer-sphere mechanism. This protocol provides a reliable, atom-economical and environmentally benign procedure for C-N and C-C bond formation. In the experimental materials used by the author, we found 3-(Trifluoromethyl)-1H-pyrazole(cas: 20154-03-4Synthetic Route of C4H3F3N2)

3-(Trifluoromethyl)-1H-pyrazole(cas: 20154-03-4) belongs to pyrazoles. Pyrazole derivatives have been reported to exhibit a wide range of applications in medicinal chemistry and pharmacology. A large number of drugs incorporating pyrazole structure have been utilized as partial agonists for nicotinic acid receptors, antidepressants, antimicrobial agents, antiviral agents, and antifungal agents solely or along with the combination of other structural motifs.Synthetic Route of C4H3F3N2

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

In 2015,Huang, Qi; Tran, Gael; Gomez Pardo, Domingo; Tsuchiya, Tomoki; Hillebrand, Stefan; Vors, Jean-Pierre; Cossy, Janine published 《Palladium-catalyzed phosphonylation of pyrazoles substituted by electron-withdrawing groups》.Tetrahedron published the findings.SDS of cas: 20154-03-4 The information in the text is summarized as follows:

A series of bromopyrazoles substituted by electron-withdrawing groups such as an ester, a trifluoromethyl group or a cyano group was involved in Pd-catalyzed phosphonylation. Moderate to good yields were obtained in the corresponding phosphonylated pyrazoles. In the experimental materials used by the author, we found 3-(Trifluoromethyl)-1H-pyrazole(cas: 20154-03-4SDS of cas: 20154-03-4)

3-(Trifluoromethyl)-1H-pyrazole(cas: 20154-03-4) belongs to pyrazoles. Pyrazole derivatives have been reported to exhibit a wide range of applications in medicinal chemistry and pharmacology. A large number of drugs incorporating pyrazole structure have been utilized as partial agonists for nicotinic acid receptors, antidepressants, antimicrobial agents, antiviral agents, and antifungal agents solely or along with the combination of other structural motifs.SDS of cas: 20154-03-4

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

《Gas Chromatography-Mass Spectrometry Quantification of 1,1-Dimethylhydrazine Transformation Products in Aqueous Solutions: Accelerated Water Sample Preparation》 was published in Molecules in 2021. These research results belong to Popov, Mark S.; Ul’yanovskii, Nikolay V.; Kosyakov, Dmitry S.. Safety of 1-Methylpyrazole The article mentions the following:

The use of highly toxic rocket fuel based on 1,1-dimethylhydrazine (UDMH) in many types of carrier rockets poses a threat to environment and human health associated with an ingress of UDMH into wastewater and natural reservoirs and its transformation with the formation of numerous toxic nitrogen-containing products. Their GC-MS quantification in aqueous samples requires matrix change and is challenging due to high polarity of analytes. To overcome this problem, accelerated water sample preparation (AWASP) based on the complete removal of water with anhydrous sodium sulfate and transferring analytes into dichloromethane was used. Twenty-nine UDMH transformation products including both the acyclic and heterocyclic compounds of various classes were chosen as target analytes. AWASP ensured attaining near quant. extraction of 23 compounds with sample preparation procedure duration of no more than 5 min. Combination of AWASP with gas chromatog.-mass spectrometry and using pyridine-d5 as an internal standard allowed for developing the rapid, simple, and low-cost method for simultaneous quantification of UDMH transformation products with detection limits of 1-5 μg L-1 and linear concentration range covering 4 orders of magnitude. The method has been validated and successfully tested in the anal. of aqueous solutions of rocket fuel subjected to oxidation with atm. oxygen, as well as pyrolytic gasification in supercritical water modeling wastewater from carrier rockets launch sites. The experimental part of the paper was very detailed, including the reaction process of 1-Methylpyrazole(cas: 930-36-9Safety of 1-Methylpyrazole)

1-Methylpyrazole(cas: 930-36-9) belongs to pyrazoles. Pyrazole derivatives have been reported to exhibit a wide range of applications in medicinal chemistry and pharmacology. A large number of drugs incorporating pyrazole structure have been utilized as partial agonists for nicotinic acid receptors, antidepressants, antimicrobial agents, antiviral agents, and antifungal agents solely or along with the combination of other structural motifs.Safety of 1-Methylpyrazole

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

《Structure-antitumor activity relationship of hybrid acetogenins focusing on connecting groups between heterocycles and the linker moiety》 was published in RSC Advances in 2022. These research results belong to Ohta, Kaito; Fushimi, Tetsuya; Okamura, Mutsumi; Akatsuka, Akinobu; Dan, Shingo; Iwasaki, Hiroki; Yamashita, Masayuki; Kojima, Naoto. Electric Literature of C4H6N2 The article mentions the following:

We studied hybrid mols. of annonaceous acetogenins and mitochondrial complex I-inhibiting insecticides to develop a novel anticancer agent. A structure-antitumor activity relationship study focusing on the connecting groups between the heterocycles and the linker moiety bearing the THF moiety was conducted. Eleven hybrid acetogenins with 1-methylpyrazole instead of γ-lactone were synthesized and their growth inhibitory activities against 39 human cancer cell lines were evaluated. The nitrogen atom at the 2′-position of the linker moiety was essential for inhibiting cancer growth. The 1-methylpyrazole-5-sulfonamide analog showed potent growth inhibition of NCI-H23, a human lung cancer cell line, in a xenograft mouse assay without critical toxicity. Hence, the results of this study may pave the way for the development of novel anticancer agents, with both selective and broad anticancer activities. In the experiment, the researchers used 1-Methylpyrazole(cas: 930-36-9Electric Literature of C4H6N2)

1-Methylpyrazole(cas: 930-36-9) belongs to pyrazoles. Pyrazole derivatives have been reported to exhibit a wide range of applications in medicinal chemistry and pharmacology. A large number of drugs incorporating pyrazole structure have been utilized as partial agonists for nicotinic acid receptors, antidepressants, antimicrobial agents, antiviral agents, and antifungal agents solely or along with the combination of other structural motifs.Electric Literature of C4H6N2

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

Li, Guangbin; Field, James A.; Zeng, Chao; Madeira, Camila Leite; Nguyen, Chi Huynh; Jog, Kalyani Vikas; Speed, David; Sierra-Alvarez, Reyes published their research in Chemosphere on February 29 ,2020. The article was titled 《Diazole and triazole inhibition of nitrification process in return activated sludge》.Category: pyrazoles-derivatives The article contains the following contents:

Azoles are emerging contaminants that are resistant to biodegradation during wastewater treatment. Their presence has been widely reported in wastewater effluents and receiving waters. In this work, the potential inhibition of nitrification process by six different azole compounds in wastewater treatment plants was investigated in batch bioassays. The azoles studied included three diazoles: pyrazole (Pz); 1-methylpyrazole (MePz); 3,5-dimethylpyrazole (DMePz); and three triazoles: 1,2,4-triazole (Tz); benzotriazole (BTz); and 5-Me benzotriazole (MeBTz). The concentration of azoles causing 50% inhibition (IC50) increased (azoles became less inhibitory) in the following order (mg L-1): BTz (1.99) < MeBTz (2.18) < Pz (2.69) < Tz (3.53) < DMePz (17.3) < MePz (49.6). No clear structure-inhibitory relationships were found using Log P and pKa as structural properties. The toxicity of any given azole may be related to the role of substituent groups on disabling/enabling binding to the active sites of metallo-enzymes in nitrifying microorganisms. This is exemplified by the low toxicity of MePz, which has a cyclic N blocked by a Me group. The observed inhibition caused to nitrifying bacteria is more severe than their cytotoxicity to other target organisms (e.g., methanogens and heterotrophic bacteria), suggesting a specific inhibition to the copper-containing enzyme, ammonium monooxygenase, in ammonia oxidizing nitrifying microorganisms. The experimental part of the paper was very detailed, including the reaction process of 1-Methylpyrazole(cas: 930-36-9Category: pyrazoles-derivatives)

1-Methylpyrazole(cas: 930-36-9) belongs to pyrazoles. Pyrazoles and their related multiring analogs are common elements of a wide variety of bioactive compounds. These ring structures are rare in nature. A consequence of this is that they have previously been thought to be poor moieties to include in potential new drugs. Category: pyrazoles-derivatives

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

《Highly active hybrid mesoporous silica-supported base organocatalysts for C-C bond formation》 was written by Erigoni, A.; Hernandez-Soto, M. C.; Rey, F.; Segarra, C.; Diaz, U.. Recommanded Product: 930-36-9 And the article was included in Catalysis Today on April 1 ,2020. The article conveys some information:

New base hybrid catalysts, based on silyl-derivatives of mols. carrying amino, diamino, pyrrolidine, pyrazolium and imidazolium functionalities were successfully achieved through post synthetic grafting onto M41S-type support. Different characterization techniques were implemented to study the characteristics of the materials, such as elemental anal., solid state MAS NMR and FTIR spectroscopies, X-ray diffraction (XRD), thermogravimetric and differential thermal analyses (TGA-DTA) and textural properties through N2 physisorption anal. The catalytic activity and recyclability of these compounds as base catalysts was demonstrated for C-C bond forming reactions such as Knoevenagel condensations and Michael additions rationalizing the differences observed as function of the reaction mechanisms. An enamine mechanism was proposed for Knoevenagel condensations and an enolate mechanism for Michael additions The experimental process involved the reaction of 1-Methylpyrazole(cas: 930-36-9Recommanded Product: 930-36-9)

1-Methylpyrazole(cas: 930-36-9) belongs to pyrazoles. Pyrazole derivatives have been reported to exhibit a wide range of applications in medicinal chemistry and pharmacology. A large number of drugs incorporating pyrazole structure have been utilized as partial agonists for nicotinic acid receptors, antidepressants, antimicrobial agents, antiviral agents, and antifungal agents solely or along with the combination of other structural motifs.Recommanded Product: 930-36-9

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

Category: pyrazoles-derivativesOn October 16, 2020 ,《Stereodivergent Synthesis of Alkenylpyridines via Pd/Cu Catalyzed C-H Alkenylation of Pyridinium Salts with Alkynes》 was published in Organic Letters. The article was written by Li, Wenjing; Tang, Juan; Li, Shun; Zheng, Xueli; Yuan, Maolin; Xu, Bin; Jiang, Weidong; Haiyan Fu; Li, Ruixiang; Chen, Hua. The article contains the following contents:

The first Pd/Cu catalyzed selective C2-alkenylation of pyridines with internal alkynes has been developed via the pyridinium salt activation strategy. Importantly, the configuration of the product alkenylpyridines could be tuned by the choice of the proper N-alkyl group of the pyridinium salts, thus allowing for both the Z- and E-alkenylpyridines synthesized with good regio- and stereoselectivity. A plausible mechanism was proposed based on the Hammett study and KIE experiment In addition to this study using 1-Methylpyrazole, there are many other studies that have used 1-Methylpyrazole(cas: 930-36-9Category: pyrazoles-derivatives) was used in this study.

1-Methylpyrazole(cas: 930-36-9) belongs to pyrazoles. Pyrazoles and their related multiring analogs are common elements of a wide variety of bioactive compounds. These ring structures are rare in nature. A consequence of this is that they have previously been thought to be poor moieties to include in potential new drugs. Category: pyrazoles-derivatives

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