Tag: 100-200

In 1959,Graner, R. Franquesa published 《Synthesis of 2-acetamido-5-nitrothiazole, an oral bactericide》.Galenica Acta published the findings.Application In Synthesis of Methyl 1H-pyrazole-3-carboxylate The information in the text is summarized as follows:

Tech. 2-aminothiazole-HCl was purified by neutralizing with NaOH at 50°, cooling with the addition of the solid amine to prevent supercooling, washing at pH 11-12, then with a saturated solution of NaCl, and then H2O. The solid was air-dried and distilled, b12 139-43°; 65% 2-aminothiazole (I) was recovered. Preparation of 2-acetamido-5-nitrothiazole (II) (CA 46, 10285h; 40, 40583) was accomplished by acetylation, then nitration of I (78.2% over-all yield), and by the reverse steps (62.8% over-all). Ac2O (1.3 mole), 1 mole I, and 0.1 mole H2SO4 was refluxed 10 min., poured on ice, and the solid recrystallized m. 209-10°, for a 92% yield of 2-acetamidothiazole (III). III (142 g.) was dissolved in 450 ml. concentrated H2SO4 at 10° with the addition of 46 ml. (d. 1.5) fuming HNO3 over 40 min.; allowing the temperature to reach 50° for 30 min., pouring on ice, filtering, and washing with water, EtOH, and recrystallizing from AcOH (50 ml./5 g.) gave 152 g. II, m. 265-6°. I (100 g.) was dissolved in 300 ml. concentrated H2SO4 at 10°, and 46 ml. (d. 1.5) fuming HNO3 was added dropwise with agitation at 12°. The temperature was kept 3 hrs. at 0°, then at 25° for 24 hrs. The mass was poured onto 5000 ml. icewater, and the filtrate neutralized with 600 g. Na2CO3 in 2000 ml. H2O. The product was water-washed, and recrystallized from EtOH (100 ml./5 g.) to give 100 g. 2-amino-5-nitrothiazole (IV), m. 202-3°. IV (7 g.), 50 ml. Ac2O, and 3 drops of concentrated H2SO4 were refluxed 7 min., and cooled to 0°. Recrystallization of the solid from AcOH gave 8.5 g. II, m. 265°. In the experiment, the researchers used Methyl 1H-pyrazole-3-carboxylate(cas: 15366-34-4Application In Synthesis of Methyl 1H-pyrazole-3-carboxylate)

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.Application In Synthesis of Methyl 1H-pyrazole-3-carboxylate

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

The author of 《A new synthesis of azolooxazines》 were Lupo, B.; Tarrago, G.. And the article was published in Synthetic Communications in 1982. COA of Formula: C5H8N2O The author mentioned the following in the article:

Pyrazolooxazine derivative I was prepared from 3(5)-hydroxymethyl-5(3)-methylpyrazole (II) in two steps. II was heated with propargyl bromide in DMF to yield a mixture of III (R = CH2OH, R1 = Me) and III (R = Me, R1 = CH2OH) (IV). A mixture of IV, Bu4N+ Br-, and NaOH in C6H6 was stirred 4 h at 60° to give I. In the experiment, the researchers used many compounds, for example, (3-methyl-1H-pyrazol-5-yl)methanol(cas: 29004-73-7COA of Formula: C5H8N2O)

(3-methyl-1H-pyrazol-5-yl)methanol(cas: 29004-73-7) 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. COA of Formula: C5H8N2O

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

《Pyrazole-3/5-carboxylic acids from 3/5-trifluoromethyl NH-pyrazoles》 was written by Ermolenko, Mikhail S.; Guillou, Sandrine; Janin, Yves L.. Safety of 3-(Trifluoromethyl)-1H-pyrazoleThis research focused ontrifluoromethylpyrazole pyrazole carboxylic acid preparation. The article conveys some information:

The transformations of substituted 3/5-trifluoromethylpyrazoles to the corresponding NH-pyrazole-3/5-carboxylic acids are reported. Moreover, from 4- or 5-iodinated-3/5-trifluoromethylpyrazoles building blocks and the use of Suzuki-Miyaura or Negishi reactions followed by the trifluoromethyl hydrolysis, we illustrate short and original accesses to many series of NH-pyrazole-3/5-carboxylic acids otherwise difficult to prepare After reading the article, we found that the author used 3-(Trifluoromethyl)-1H-pyrazole(cas: 20154-03-4Safety of 3-(Trifluoromethyl)-1H-pyrazole)

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.Safety of 3-(Trifluoromethyl)-1H-pyrazole

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

Related Products of 15366-34-4In 2001 ,《Synthesis of a terbium fluorescent chelate and its application to time-resolved fluoroimmunoassay》 was published in Analytical Chemistry. The article was written by Yuan, Jingli; Wang, Guilan; Majima, Keisuke; Matsumoto, Kazuko. The article contains the following contents:

A new nonadentate ligand, N, N, N1, N1-[2,6-bis(3′-aminomethyl-1′-pyrazolyl)-4-phenylpyridine]tetrakis(acetic acid) (BPTA) for a Tb3+ fluorescent complex was synthesized. The Tb3+ complex is strongly fluorescent, having a large fluorescence quantum yield of 1.00 and very long fluorescence lifetime of 2.681 ms in 0.05 M borate buffer of pH 9.1. Streptavidin (SA) was labeled with BPTA by using its succinimidyl monoester, and the BPTA-Tb3+-labeled SA was used in sandwich-type time-resolved fluoroimmunoassay (TR-FIA) of α-fetoprotein (AFP) and carcinoembryonic antigen (CEA) in human sera. The Tb3+-labeled SA was also used in competitive-type TR-FIA of bensulfuron-Me (BSM) in water. The detection limits of these assays are 42 pg/mL for AFP, 70 pg/mL for CEA, and 0.4 ng/mL for BSM. In addition, a new simultaneous measurement method for AFP and CEA in a human serum sample was developed by using 4,4′-bis(1”,1”,1”,2”,2”,3”,3” -heptafluoro-4”,6”-hexanedion-6”-yl)chlorosulfo-o-terphenyl (BHHCT)-Eu3+-labeled anti-AFP antibody, biotinylated anti-CEA antibody, and BPTA-Tb3+-labeled SA. The concentrations of AFP and CEA in 39 human serum samples were determined, and the results were compared with those of the independently determined AFP and CEA by TR-FIA with a single-label method. A good correlation was obtained with the correlation coefficients of 0.991 for AFP and 0.994 for CEA. The results came from multiple reactions, including the reaction of Methyl 1H-pyrazole-3-carboxylate(cas: 15366-34-4Related Products of 15366-34-4)

Methyl 1H-pyrazole-3-carboxylate(cas: 15366-34-4) 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.Related Products of 15366-34-4

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

Electric Literature of C4H3F3N2In 2016 ,《η1:η2-P-pyrazolylphosphaalkene complexes of ruthenium(0)》 appeared in Inorganics. The author of the article were Greenacre, Victoria K.; Crossley, Ian R.. The article conveys some information:

An extended range of novel ruthenium phosphaalkene complexes of the type [Ru{η1-N:η2-P,C-P(pz’):CH(SiMe2R)}(CO)(PPh3)2] (R = Tol, C6H4CF3-p; pz’ = pzMe2, pzCF3, pzMe,CF3; R = Me, C6H4CF3-p; pz’ = pzPh) have been prepared from the resp. ruthenaphosphaalkenyls [Ru{P:CH(SiMe2R)}Cl(CO)(PPh3)2] upon treatment with Lipz’. Where R = C6H4CF3-p and pz’ = pzMe2 the complex is characterized by single crystal x-ray diffraction, only the second example of such species being structurally characterized. This indicates enhanced pyramidalization of the alkenic carbon center when compared with precedent data (R = Me, pz’ = pz) implying an enhanced Ru→π*PC contribution, which can be correlated with the greater donor power of pzMe2. This is similarly reflected in spectroscopic data that reveal significant influence of the pyrazolyl substituents upon the phosphaalkene, stronger donors imparting significantly enhanced shielding to phosphorus; in contrast, a much lesser influence if noted for the silyl substituents. The results came from multiple reactions, including the reaction of 3-(Trifluoromethyl)-1H-pyrazole(cas: 20154-03-4Electric Literature 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.Electric Literature of C4H3F3N2

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

Formula: C5H6N2O2In 2019 ,《Annular tautomerism of 3(5)-disubstituted-1H-pyrazoles with ester and amide groups》 appeared in Molecules. The author of the article were Kusakiewicz-Dawid, Anna; Porada, Monika; Dziuk, Blazej; Siodlak, Dawid. The article conveys some information:

A series of disubstituted 1H-pyrazoles with Me (1), amino (2), and nitro (3) groups, as well as ester (a) or amide (b) groups in positions 3 and 5 was synthesized, and annular tautomerism was investigated using X-ray, theor. calculations, NMR, and FT-IR methods. The X-ray experiment in the crystal state showed for the compounds with Me (1a, 1b) and amino (2b) groups the tautomer with ester or amide groups at position 3 (tautomer 3), but for those with a nitro group (3b, 4), tautomer 5. Similar results were obtained in solution by NMR NOE experiments in CDCl3, DMSO-d6, and CD3OD solvents. However, tautomer equilibrium was observed for 2b in DMSO. The FT-IR spectra in chloroform and acetonitrile showed equilibrium, which can be ascribed to conformational changes of the cis/trans arrangement of the ester/amide group and pyrazole ring. Theor. anal. using the M06-2X/6-311++G(d,p) method (in vacuo, chloroform, acetonitrile, and water) and measurement of aromaticity (NICS) showed dependence on internal hydrogen bonds, the influence of the environment, and the effect of the substituent. These factors, pyrazole aromaticity and intra- and inter-mol. interactions, seem to have a considerable influence on the choice of tautomer. The results came from multiple reactions, including the reaction of Methyl 1H-pyrazole-3-carboxylate(cas: 15366-34-4Formula: C5H6N2O2)

Methyl 1H-pyrazole-3-carboxylate(cas: 15366-34-4) 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.Formula: C5H6N2O2

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

Pei, Congcong; Chen, Xiaoyu; Li, Linlin; Li, Jingya; Zou, Dapeng; Wu, Yangjie; Wu, Yusheng published their research in Tetrahedron Letters in 2021. The article was titled 《Copper-catalyzed C3-amination of quinoxalin-2(1H)-ones: Using Selectfluor as a mild oxidant》.Application In Synthesis of 3-(Trifluoromethyl)-1H-pyrazole The article contains the following contents:

A practical and efficient route for copper-catalyzed C-3 amination of quinoxalin-2(1H)-ones with easily available azoles as nitrogen sources and Selectfluor as mild oxidant was developed. The transformation featured at. economy, simple operation, broad substrate scope, and moderate to excellent yields. After reading the article, we found that the author used 3-(Trifluoromethyl)-1H-pyrazole(cas: 20154-03-4Application In Synthesis of 3-(Trifluoromethyl)-1H-pyrazole)

3-(Trifluoromethyl)-1H-pyrazole(cas: 20154-03-4) 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.Application In Synthesis of 3-(Trifluoromethyl)-1H-pyrazole

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

In 2014,Anderson, Erin D.; Duerfeldt, Adam S.; Zhu, Kaicheng; Glinkerman, Christopher M.; Boger, Dale L. published 《Cycloadditions of Noncomplementary Substituted 1,2,3-Triazines》.Organic Letters published the findings.Synthetic Route of C5H6N2O2 The information in the text is summarized as follows:

The scope of the [4 + 2] cycloaddition reactions of substituted 1,2,3-triazines, bearing noncomplementary substitution with electron-withdrawing groups at C4 and/or C6, is described. The studies define key electronic and steric effects of substituents impacting the reactivity, mode (C4/N1 vs C5/N2), and regioselectivity of the cycloaddition reactions of 1,2,3-triazines with amidines, enamines, and ynamines, providing access to highly functionalized heterocycles [e.g., Me 1,2,3-triazine-4-carboxylate + benzamidine → Me 2-phenylpyrimidine-4-carboxylate (71%)].Methyl 1H-pyrazole-3-carboxylate(cas: 15366-34-4Synthetic Route of C5H6N2O2) 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.Synthetic Route of C5H6N2O2

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

In 2011,Qiao, Jennifer X.; Wang, Tammy C.; Hu, Carol; Li, Jianqing; Wexler, Ruth R.; Lam, Patrick Y. S. published 《Transformation of Anionically Activated Trifluoromethyl Groups to Heterocycles under Mild Aqueous Conditions》.Organic Letters published the findings.Reference of 3-(Trifluoromethyl)-1H-pyrazole The information in the text is summarized as follows:

The (hetero)aromatic trifluoromethyl group is present in many biol. active mols. and is generally considered to be chem. stable. In this paper, a convenient one-step synthesis of C-C linked aryl-heterocycles or heteroaryl-heterocycles in good to excellent yields via the reaction of anionically activated trifluoromethyl groups with amino nucleophiles containing a second NH, OH, or SH nucleophile in 1 N sodium hydroxide is reported. The method has high functional group tolerability and is potentially useful in parallel synthesis. After reading the article, we found that the author used 3-(Trifluoromethyl)-1H-pyrazole(cas: 20154-03-4Reference of 3-(Trifluoromethyl)-1H-pyrazole)

3-(Trifluoromethyl)-1H-pyrazole(cas: 20154-03-4) 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 3-(Trifluoromethyl)-1H-pyrazole

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

In 1967,Micheel, Fritz; Dammert, Walter published 《Condensation products from trimethyl fluorotrimesate and α-amino-β-hydroxy compounds》.Chemische Berichte published the findings.Related Products of 15366-34-4 The information in the text is summarized as follows:

N-[6-carboxy-2,4-bis(methoxycarbonyl)phenyl]-DL-serinolactone (I) was treated with CH2N2 to form a pyrazoline which was converted to the corresponding cyclopropane derivative by elimination of N. The structures of the pyrazoline and cyclopropane derivatives were confirmed by degradation and synthesis. Condensates of DL-threonine and β-phenyl-DL-serine with methyl fluorotrimesate formed ester lactones, which on treatment with CH2N2 formed Me N-[2,4,6-(trimethoxycarbonyl)phenyl]-α-aminocrotonate and Me N-[2,4,6 (trimethoxycarbonyl)phenyl]-α-aminocinnamate, resp. In the experimental materials used by the author, we found Methyl 1H-pyrazole-3-carboxylate(cas: 15366-34-4Related Products of 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.Related Products of 15366-34-4

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