Month: October 2022

Recommanded Product: 3,5,6-Trichloropicolinic acidOn March 31, 2009, Slotkin, Theodore A.; Seidler, Frederic J.; Wu, Changlong; MacKillop, Emiko A.; Linden, Karl G. published an article in Environmental Health Perspectives. The article was 《Ultraviolet photolysis of chlorpyrifos: developmental neurotoxicity modeled in PC12 cells》. The article mentions the following:

UV photodegradation products from pesticides form both in the field and during water treatment. We evaluated the photolytic breakdown of the organophosphate pesticide chlorpyrifos (CPF) in terms of both the chem. entities generated by low-pressure UV C irradiation and their potential as developmental neurotoxicants. We separated byproducts using high-performance liquid chromatog. and characterized them by gas chromatog./mass spectrometry. We assessed neurotoxicity in neuronotypic PC12 cells, both in the undifferentiated state and during differentiation. Photodegradation of CPF in methanol solution generated CPF oxon and trichloropyridinol, products known to retain developmental neurotoxicant actions, as well as a series of related organophosphate and phosphorothionate derivatives Exposure conditions that led to 50% degradation of CPF thus did not reduce developmental neurotoxicity. The degradation mixture inhibited DNA synthesis in undifferentiated cells to the same extent as native CPF. In differentiating cells, the products likewise retained the full ability to elicit shortfalls in cell number and corresponding effects on cell growth and neurite formation. When the exposure was prolonged to the point where 70% of the CPF was degraded, the adverse effects on PC12 cells were no longer evident; however, these conditions were sufficiently severe to generate toxic products from the methanol vehicle. Our results indicate that field conditions or remediation treatments that degrade a significant proportion of the CPF do not necessarily produce inactive products and, indeed, may elicit formation of even more toxic chems. that are more water soluble and thus have greater field mobility than CPF itself. The experimental part of the paper was very detailed, including the reaction process of 3,5,6-Trichloropicolinic acid(cas: 40360-44-9Recommanded Product: 3,5,6-Trichloropicolinic acid)

3,5,6-Trichloropicolinic acid(cas: 40360-44-9) belongs to pyridine. Pyridine, its benzo and pyridine-based compounds play diverse roles in organic chemistry. As ligands, solvents, and catalysts they facilitate reactions; thus descriptions of these new ligands and their applications abound each year.Recommanded Product: 3,5,6-Trichloropicolinic acid

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Cellier, Marie; Gignoux, Amandine; James, Arthur L.; Orenga, Sylvain; Perry, John D.; Robinson, Shaun N.; Stanforth, Stephen P.; Turnbull, Graeme published their research in Bioorganic & Medicinal Chemistry Letters on December 15 ,2015. The article was titled 《2-(Nitroaryl)benzothiazole and benzoxazole derivatives as fluorogenic substrates for the detection of nitroreductase activity in clinically important microorganisms》.Name: N-(2-Chloropyridin-3-yl)-2-nitrobenzamide The article contains the following contents:

A series of carboxy-substituted 2-(nitroaryl)benzothiazole derivatives and carboxy-substituted 2-(nitroaryl)benzoxazole derivatives were prepared and evaluated as potential nitroreductase substrates for the purpose of detecting clin. important microorganisms. Several of the substrates produced highly fluorescent colonies with the majority of a panel of 10 Gram-neg. bacteria and also with two of a panel of 8 Gram-pos. bacteria. In the experimental materials used by the author, we found N-(2-Chloropyridin-3-yl)-2-nitrobenzamide(cas: 1028-86-0Name: N-(2-Chloropyridin-3-yl)-2-nitrobenzamide)

N-(2-Chloropyridin-3-yl)-2-nitrobenzamide(cas: 1028-86-0) belongs to anime. To avoid the problem of multiple alkylation, methods have been devised for “blocking” substitution so that only one alkyl group is introduced. The Gabriel synthesis is one such method; it utilizes phthalimide, C6H4(CO)2NH, whose one acidic hydrogen atom has been removed upon the addition of a base such as KOH to form a salt.Name: N-(2-Chloropyridin-3-yl)-2-nitrobenzamide

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Ko, Young Kwan; Lee, Seung Chul; Koo, Dong Wan; Jung, Mankil; Kim, Dae-Whang published an article on February 20 ,2001. The article was titled 《A new and facile synthesis of 2-pyridones》, and you may find the article in Bulletin of the Korean Chemical Society.Related Products of 77837-09-3 The information in the text is summarized as follows:

Treating coumalic acid with MeCOCl gave di-Me 4-(methoxymethylene)-2-pentenedioate. Reaction of the diester with amines, followed by cyclization, gave 5-carbomethoxy-2-pyridones. In the experimental materials used by the author, we found Methyl 6-oxo-1-phenyl-1,6-dihydropyridine-3-carboxylate(cas: 77837-09-3Related Products of 77837-09-3)

Methyl 6-oxo-1-phenyl-1,6-dihydropyridine-3-carboxylate(cas: 77837-09-3) belongs to pyridine derivatives. Several pyridine derivatives play important roles in biological systems. While its biosynthesis is not fully understood, nicotinic acid (vitamin B3) occurs in some bacteria, fungi, and mammals. Related Products of 77837-09-3

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Wu, Zhibing; Park, Hyung-Yeon; Xie, Dewen; Yang, Jingxin; Hou, Shuaitao; Shahzad, Nasir; Kim, Chan Kyung; Yang, Song published an article on February 3 ,2021. The article was titled 《Synthesis, Biological Evaluation, and 3D-QSAR Studies of N-(Substituted pyridine-4-yl)-1-(substituted phenyl)-5-trifluoromethyl-1H-pyrazole-4-carboxamide Derivatives as Potential Succinate Dehydrogenase Inhibitors》, and you may find the article in Journal of Agricultural and Food Chemistry.Recommanded Product: 4-Amino-2-picoline The information in the text is summarized as follows:

To develop more potential succinate dehydrogenase (SDH) inhibitors, we designed and synthesized a novel series of N-(substituted pyridine-4-yl)-1-(substituted phenyl)-5-trifluoromethyl-1H-pyrazole-4-carboxamide derivatives, I [R1 = H, CH3, F, Cl; R2 = 2-pyridinyl, 4-pyridinyl, 2-CH3-4-pyridinyl, etc.]. The bioassay results demonstrated that some title compounds exhibited excellent antifungal activity against four tested phytopathogenic fungi (Gibberella zea, Fusarium oxysporum, Cytospora mandshurica, and Phytophthora infestans). The EC50 values were 1.8μg/mL for I [R1 = Cl; R2 = 4-pyridinyl] against G. zeae, 1.5 and 3.6μg/mL for I [R1 = Cl; R2 = 2-CH3-4-pyridinyl] against F. oxysporum and C. mandshurica, resp., and 6.8μg/mL for I [R1 = F; R2 = 2-CH3-4-pyridinyl] against P. infestans. The SDH enzymic activity testing revealed that the IC50 values of I [R1 = H; R2 = 4-pyridinyl], I [R1 = CH3; R2 = 4-pyridinyl], I [R1 = F; R2 = 2-CH3-4-pyridinyl], and penthiopyrad were 12.5, 135.3, 6.9, and 223.9μg/mL, resp. The mol. docking results of this series of title compounds with SDH model demonstrated that the compounds could completely locate inside of the pocket, the body fragment formed H bonds, and the Ph ring showed a π-π interaction with Arg59, suggesting that these novel 5-trifluoromethyl-pyrazole-4-carboxamide derivatives might target SDH. These results provided a benchmark for understanding the antifungal activity against the phytopathogenic fungus P. infestans and prompt us to discover more potent SDH inhibitors.4-Amino-2-picoline(cas: 18437-58-6Recommanded Product: 4-Amino-2-picoline) was used in this study.

4-Amino-2-picoline(cas: 18437-58-6) belongs to anime. Many important products require amines as part of their syntheses. Methylamine is utilized in the production of the analgesic meperidine (trade name Demerol) and the photographic developer Metol (trademark), and dimethylamine is used in the synthesis of the antihistamine diphenhydramine (trade name Benadryl), the solvent dimethylformamide (DMF), and the rocket propellant 1,1-dimethylhydrazine. The synthesis of the insect repellent N,N-diethyl-m-toluamide (DEET) incorporates diethylamine while that of the synthetic fibre Kevlar requires aromatic amines.Recommanded Product: 4-Amino-2-picoline

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

In 2009,Aoyagi, Yutaka; Adachi, Yoshiyuki; Akagi, Shunta; Ohno, Naohito; Takeya, Koichi published 《First asymmetric synthesis of CJ-14877 and its enantiomer and their interleukin-1β inhibitory activities》.Bioorganic & Medicinal Chemistry Letters published the findings.Electric Literature of C7H6BrNO2 The information in the text is summarized as follows:

A potent antiinflammatory Me picolinate alkaloid CJ-14877 [(+)-I] and its enantiomer (-)-II were synthesized in two steps starting from com. available Me 5-bromopicolinate. The synthesis includes microwave-assisted Suzuki coupling reaction and Sharpless asym. dihydroxylation. In the experiment, the researchers used many compounds, for example, Methyl 5-bromopicolinate(cas: 29682-15-3Electric Literature of C7H6BrNO2)

Methyl 5-bromopicolinate(cas: 29682-15-3) belongs to pyridine. Pyridines are often used as catalysts or reagents; particular notice has been paid recently to how pyridine coordinates to metal centers enabling a wide range of valuable reactions. Electric Literature of C7H6BrNO2

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

In 2013,Zhang, Xiaoyan; Zhang, Nanjing; Chen, Guangming; Turpoff, Anthony; Ren, Hongyu; Takasugi, James; Morrill, Christie; Zhu, Jin; Li, Chunshi; Lennox, William; Paget, Steven; Liu, Yalei; Almstead, Neil; George Njoroge, F.; Gu, Zhengxian; Komatsu, Takashi; Clausen, Valerie; Espiritu, Christine; Graci, Jason; Colacino, Joseph; Lahser, Fred; Risher, Nicole; Weetall, Marla; Nomeir, Amin; Karp, Gary M. published 《Discovery of novel HCV inhibitors: Synthesis and biological activity of 6-(indol-2-yl)pyridine-3-sulfonamides targeting hepatitis C virus NS4B》.Bioorganic & Medicinal Chemistry Letters published the findings.Reference of 5-Bromo-2-chloropyridine The information in the text is summarized as follows:

A novel series of 6-(indol-2-yl)pyridine-3-sulfonamides I [R1 = CHF2O, c-Pr; R2 = i-Pr, H, CH(CH2F)2, etc.] was prepared and evaluated for their ability to inhibit HCV RNA replication in the HCV replicon cell culture assay. Preliminary optimization of this series furnished compounds with low nanomolar potency against the HCV genotype 1b replicon. Among these, compound I [R1 = CHF2O; R2 = CH(CH2F)2] was identified as a potent HCV replicon inhibitor (EC50 = 4 nM) with a selectivity index with respect to cellular GAPDH of more than 2500. Further, compound I [R1 = CHF2O; R2 = CH(CH2F)2] had a good pharmacokinetic profile in rats with an IV half-life of 6 h and oral bioavailability (F) of 62%. Selection of HCV replicon resistance identified an amino acid substitution in HCV NS4B that confers resistance to these compounds These compounds hold promise as a new chemotype with anti-HCV activity mediated through an underexploited viral target. The experimental part of the paper was very detailed, including the reaction process of 5-Bromo-2-chloropyridine(cas: 53939-30-3Reference of 5-Bromo-2-chloropyridine)

5-Bromo-2-chloropyridine(cas: 53939-30-3) belongs to pyridine. Pyridines form stable salts with strong acids. Pyridine itself is often used to neutralize acid formed in a reaction and as a basic solvent. Reference of 5-Bromo-2-chloropyridine

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

In 2014,Hager, Dominik; MacMillan, David W. C. published 《Activation of C-H Bonds via the Merger of Photoredox and Organocatalysis: A Coupling of Benzylic Ethers with Schiff Bases》.Journal of the American Chemical Society published the findings.Name: 6-Bromopyridin-3-amine The information in the text is summarized as follows:

The photoredox-mediated coupling of benzylic ethers with Schiff bases has been accomplished. Direct benzylic C-H activation by a combination of a thiol catalyst with an iridium photocatalyst and subsequent radical-radical coupling with secondary aldimines affords a variety of β-amino ether products in good to excellent yields. Mechanistic studies suggest that a reductive quenching pathway of the photocatalyst is operable.6-Bromopyridin-3-amine(cas: 13534-97-9Name: 6-Bromopyridin-3-amine) was used in this study.

6-Bromopyridin-3-amine(cas: 13534-97-9) belongs to anime. Primary amines having a tertiary alkyl group (R3CNH2) are difficult to prepare with most methods but are made industrially by the Ritter reaction. In this method a tertiary alcohol reacts with hydrogen cyanide (HCN) in the presence of a concentrated strong acid; a formamide, RNH―CHO, is formed first, which then undergoes hydrolysis.Name: 6-Bromopyridin-3-amine

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

In 2014,Kedari, Chaitanya Kumar; Roy Choudhury, Nilanjana; Sharma, Sreevalli; Kaur, Parvinder; Guptha, Supreeth; Panda, Manoranjan; Mukerjee, Kakoli; Ramachandran, Vasanthi; Bandodkar, Balachandra; Ramachandran, Sreekanth; Tantry, Subramanyam J. published 《Biarylmethoxy Nicotinamides As Novel and Specific Inhibitors of Mycobacterium tuberculosis》.ACS Medicinal Chemistry Letters published the findings.Category: pyridine-derivatives The information in the text is summarized as follows:

A whole cell based screening effort on a focused library from corporate collection resulted in the identification of biarylmethoxy nicotinamides as novel inhibitors of M. tuberculosis (Mtu) H37Rv. The series exhibited tangible structure-activity relationships, and during hit to lead exploration, a cellular potency of 100 nM was achieved, which is an improvement of >200-fold from the starting point. The series is very specific to Mtu and noncytotoxic up to 250 μM as measured in the mammalian cell line THP-1 based cytotoxicity assay. This compound class retains its potency on several drug sensitive and single drug resistant clin. isolates, which indicate that the compounds could be acting through a novel mode of action. In the experimental materials used by the author, we found Methyl 5-bromopicolinate(cas: 29682-15-3Category: pyridine-derivatives)

Methyl 5-bromopicolinate(cas: 29682-15-3) belongs to pyridine. Pyridine’s structure is isoelectronic with that of benzene, but its properties are quite different. Pyridine is completely miscible with water, whereas benzene is only slightly soluble. Like all hydrocarbons, benzene is neutral (in the acid–base sense), but because of its nitrogen atom, pyridine is a weak base.Category: pyridine-derivatives

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

In 2014,Lee, Hong Geun; Milner, Phillip J.; Buchwald, Stephen L. published 《Pd-Catalyzed Nucleophilic Fluorination of Aryl Bromides》.Journal of the American Chemical Society published the findings.Quality Control of Methyl 5-bromopicolinate The information in the text is summarized as follows:

On the basis of mechanism-driven reaction design, a Pd-catalyzed nucleophilic fluorination of aryl bromides and iodides has been developed. The method exhibits a broad substrate scope, especially with respect to nitrogen-containing heteroaryl bromides, and proceeds with minimal formation of the corresponding reduction products. A facilitated ligand modification process was shown to be critical to the success of the reaction. In the part of experimental materials, we found many familiar compounds, such as Methyl 5-bromopicolinate(cas: 29682-15-3Quality Control of Methyl 5-bromopicolinate)

Methyl 5-bromopicolinate(cas: 29682-15-3) belongs to pyridine. When pyridine is adsorbed on oxide surfaces or in porous materials, the following species are commonly observed: (i) pyridine coordinated to Lewis acid sites, (ii) pyridine H-bonded to weakly acidic hydroxyls, and (iii) protonated pyridine. At high coverage, physisorbed pyridine and protonated dimers can also be observed.Quality Control of Methyl 5-bromopicolinate

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

In 2015,Mane, Madhav S.; Gavade, Sandeep; Mane, Dhananjay V. published 《Designing and synthesis of N-(6-phenylpyridin-2-yl) pyridine-2-amine derivatives as a novel antimicrobial agent》.Journal of Environmental Nanotechnology published the findings.Recommanded Product: 5-Bromo-2-chloropyridine The information in the text is summarized as follows:

A new series of N-(-6-phenylpyridin-2-yl) pyridine-2-amine derivatives were synthesized in satisfactory yield, through simple and greener methodol. using 2-Amino, 6-Chloro, Pyridines as a starting material. Some of the newly prepared compounds demonstrate potent inhibitory activity against Gram pos. bacteria, Gram neg. bacteria and fungai. The results are discussed in terms of structure-activity relationships and an attempt was made to define the structural features required for activity. After reading the article, we found that the author used 5-Bromo-2-chloropyridine(cas: 53939-30-3Recommanded Product: 5-Bromo-2-chloropyridine)

5-Bromo-2-chloropyridine(cas: 53939-30-3) belongs to pyridine. Pyridine is very deactivated towards electrophilic substitution with respect to benzene. For this reason classical formylation, using methods such as the Gattermann or Vilsmeier reactions, are not generally successful. Recommanded Product: 5-Bromo-2-chloropyridine

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem