Month: October 2022

《Synthesis of novel pyridine and pyrimidine derivatives as potential inhibitors of HIV-1 reverse transcriptase using palladium-catalysed C-N cross-coupling and nucleophilic aromatic substitution reactions》 was published in ARKIVOC (Gainesville, FL, United States) in 2020. These research results belong to Changunda, Charles R. K.; Rousseau, Amanda L.; Basson, Adriaan E.; Bode, Moira L.. Electric Literature of C6H4Cl2N2O The article mentions the following:

Palladium-mediated cross-coupling reactions are used in the successful construction of a small library of flexible heteroatom-linked diarylpyridine target compounds I (R = H, cyano, cyclopropylamino; R1 = cyano, aminocarbonyl, cyclopropylamino; R2 = 4-chlorophenoxy, 2-cyano-5-methylphenyl, cyclohexylamino), including pyridines bearing a secondary amide substituent. Heteroatom-linked diarylpyrimidine derivatives II (R3 = 4-Cl, 2,4-Cl2, 3,5-Cl2, 4-F, 3-CF3; R4 = 5-methylpyridin-2-yl, 5-chloropyrimidin-2-yl, 2-cyano-5-methylphenyl) bearing a chlorine substituent are prepared by base-catalyzed nucleophilic aromatic substitution reactions without the need for palladium catalysis.2,6-Dichloroisonicotinamide(cas: 89281-13-0Electric Literature of C6H4Cl2N2O) was used in this study.

2,6-Dichloroisonicotinamide(cas: 89281-13-0) belongs to anime. Examples of direct uses of amines and their salts are as corrosion inhibitors in boilers and in lubricating oils (morpholine), as antioxidants for rubber and roofing asphalt (diarylamines), as stabilizers for cellulose nitrate explosives (diphenylamine), as protectants against damage from gamma radiation (diarylamines), as developers in photography (aromatic diamines), as flotation agents in mining, as anticling and waterproofing agents for textiles, as fabric softeners, in paper coating, and for solubilizing herbicides.Electric Literature of C6H4Cl2N2O

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Qin, Zengquan; Jennings, Michael C.; Puddephatt, Richard J. published their research in Chemical Communications (Cambridge, United Kingdom) on December 21 ,2001. The article was titled 《Stacked molecular triangles: self-assembly using coordination chemistry and hydrogen bonding》.HPLC of Formula: 64479-78-3 The article contains the following contents:

The combination of the cis-blocked platinum(II) unit (bu2bipy)Pt2+ with the unsym. bis(pyridine) ligand 4-NC5H4C(:O)NH-4-C5H4N (L) gives the mol. triangle complex [{Pt(bu2bipy)(μ-L)}3]6+, which forms stacked pairs in the solid state through intertriangle NH···OC hydrogen bonds and Pt···OC secondary bonds. The crystal structure of [{(bu2bipy)Pt(μ-L)}3](CF3SO3)6·Me2CO·3H2O was determined The analogous palladium(II) complex was prepared as the BF4- salt.N-(Pyridin-4-yl)isonicotinamide(cas: 64479-78-3HPLC of Formula: 64479-78-3) was used in this study.

N-(Pyridin-4-yl)isonicotinamide(cas: 64479-78-3) belongs to amides. Because of the greater electronegativity of oxygen, the carbonyl (C=O) is a stronger dipole than the N–C dipole. The presence of a C=O dipole and, to a lesser extent a N–C dipole, allows amides to act as H-bond acceptors.“,” In primary and secondary amides, the presence of N–H dipoles allows amides to function as H-bond donors as well. HPLC of Formula: 64479-78-3

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

The author of 《CuCl-catalyzed ortho trifluoromethylation of arenes and heteroarenes with a pivalamido directing group》 were Cai, Shangjun; Chen, Chao; Sun, Zelin; Xi, Chanjuan. And the article was published in Chemical Communications (Cambridge, United Kingdom) in 2013. Recommanded Product: 2,2-Dimehtyl-N-pyridin-3-yl-propionamide The author mentioned the following in the article:

The CuCl catalyzed direct trifluoromethylation of sp2 C-H bonds has been realized, using the Togni reagent as the CF3 source. This reaction achieves the goal of regio-selectively converting C-H into C-CF3 with ecol. and readily available starting materials. After reading the article, we found that the author used 2,2-Dimehtyl-N-pyridin-3-yl-propionamide(cas: 70298-88-3Recommanded Product: 2,2-Dimehtyl-N-pyridin-3-yl-propionamide)

2,2-Dimehtyl-N-pyridin-3-yl-propionamide(cas: 70298-88-3) belongs to anime. The methylamines occur in small amounts in some plants. Many polyfunctional amines (i.e., those having other functional groups in the molecule) occur as alkaloids in plants—for example, mescaline, 2-(3,4,5-trimethoxyphenyl)ethylamine; the cyclic amines nicotine, atropine, morphine, and cocaine; and the quaternary salt choline, N-(2-hydroxyethyl)trimethylammonium chloride, which is present in nerve synapses and in plant and animal cells.Recommanded Product: 2,2-Dimehtyl-N-pyridin-3-yl-propionamide

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

In 2012,Yu, Yanfei; Li, Zhengning; Jiang, Lan published 《A novel synthesis of 2-alkylthiobenzothiazoles and 2-alkylthiobenzoxazoles》.Phosphorus, Sulfur and Silicon and the Related Elements published the findings.Product Details of 71432-55-8 The information in the text is summarized as follows:

3H-Benzothiazole-2-thione and 3H-benzoxazole-2-thione were selectively S-alkylated by use of O-alkylisoureas as the alkylating reagents. The reactions could be performed under mild reaction conditions in short reaction times, and high yields were obtained using O-primary-alkylisoureas, whereas low yields were obtained with sec- and tert-alkylisoureas. In the experimental materials used by the author, we found tert-Butyl N,N’-diisopropylcarbamimidate(cas: 71432-55-8Product Details of 71432-55-8)

tert-Butyl N,N’-diisopropylcarbamimidate(cas: 71432-55-8) belongs to anime.Typically the presence of an amine functional group is deduced by a combination of techniques, including mass spectrometry as well as NMR and IR spectroscopies. 1H NMR signals for amines disappear upon treatment of the sample with D2O. In their infrared spectrum primary amines exhibit two N-H bands, whereas secondary amines exhibit only one.Product Details of 71432-55-8

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

《Escherichia coli γ-carbonic anhydrase: characterisation and effects of simple aromatic/heterocyclic sulphonamide inhibitors》 was written by Del Prete, Sonia; Bua, Silvia; Supuran, Claudiu T.; Capasso, Clemente. COA of Formula: C7H9NO2S And the article was included in Journal of Enzyme Inhibition and Medicinal Chemistry in 2020. The article conveys some information:

Carbonic anhydrases (CAs, EC 4.2.1.1) are ubiquitous metalloenzymes involved in biosynthetic processes, transport, supply, and balance of CO2/HCO3- into the cell. In Bacteria, CAs avoid the depletion of the dissolved CO2/HCO3- from the cell, providing them to the central metabolism that is compromised without the CA activity. The involvement of CAs in the survival, pathogenicity, and virulence of several bacterial pathogenic species is recent. Here, we report the kinetic properties of the recombinant γ-CA (EcoCAγ) encoded in the genome of Escherichia coli. EcoCAγ is an excellent catalyst for the physiol. CO2 hydration reaction to bicarbonate and protons, with a kcat of 5.7 × 105 s-1 and kcat/Km of 6.9 × 106 M-1s-1. The EcoCAγ inhibition profile with a broad series of known CA inhibitors, the substituted benzene-sulfonamides, and clin. licensed drugs was explored. Benzolamide showed a KI lower than 100 nM. Our study reinforces the hypothesis that the synthesis of new drugs capable of interfering selectively with the bacterial CA activity, avoiding the inhibition of the human α -CAs, is achievable and may lead to novel antibacterials. In the experiment, the researchers used many compounds, for example, 4-Methylbenzenesulfonamide(cas: 70-55-3COA of Formula: C7H9NO2S)

4-Methylbenzenesulfonamide(cas: 70-55-3) belongs to anime. Amines can be classified according to the nature and number of substituents on nitrogen. Aliphatic amines contain only H and alkyl substituents. Aromatic amines have the nitrogen atom connected to an aromatic ring.Important amines include amino acids, biogenic amines, trimethylamine, and aniline. Inorganic derivatives of ammonia are also called amines, such as monochloramine (NClH2).COA of Formula: C7H9NO2S

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

《Kinetics and mechanism of reversible, base-catalyzed ring closure of 3-(methoxycarbonyl)propionanilide and (methoxycarbonyl)methyl N-phenylcarbamate》 was written by Kavalek, Jaromir; Machacek, Vladimir; Svobodova, Gabriela; Sterba, Vojeslav. Formula: C8H9NO2 And the article was included in Collection of Czechoslovak Chemical Communications on April 30 ,1989. The article conveys some information:

The rate constants of reversible, base-catalyzed ring closure of 3-(methoxycarbonyl)propionanilide (I) and (methoxycarbonylmethyl) phenylcarbamate (II) to 1-phenyl-2,5-pyrrolidinedione (III) and 3-phenyl-2,4-oxazolidinedione (IV), resp., and the rates of solvolyses of III and IV in water and methanol have been determined In both cases, an equilibrium is established between the starting ester and the cyclization product in methoxide solutions, which is strongly shifted in favor of the starting ester. In the case of II in methoxide solutions, the cyclization is followed by a much slower splitting of the cyclization product to give glycolic acid anilide. The effects of X = NH, CH2, O, S in RNHCOXCH2COOMe on the rates of the cyclization and solvolysis of the cyclization products is discussed.2-Hydroxy-N-phenylacetamide(cas: 4746-61-6Formula: C8H9NO2) was used in this study.

2-Hydroxy-N-phenylacetamide(cas: 4746-61-6) belongs to amides. Because of the greater electronegativity of oxygen, the carbonyl (C=O) is a stronger dipole than the N–C dipole.Formula: C8H9NO2 The presence of a C=O dipole and, to a lesser extent a N–C dipole, allows amides to act as H-bond acceptors. In primary and secondary amides, the presence of N–H dipoles allows amides to function as H-bond donors as well.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Application In Synthesis of 2-Amino-N-(3-(2-chlorobenzoyl)-5-ethylthiophen-2-yl)acetamideOn March 31, 1984, Polivka, Zdenek; Holubek, Jiri; Svatek, Emil; Metys, Jan; Protiva, Miroslav published an article in Collection of Czechoslovak Chemical Communications. The article was 《Potential hypnotics and anxiolytics: synthesis of 2-bromo-4-(2-chlorophenyl)-9-[4-(2-methoxyethyl)piperazino]-6H-thieno[3,2-f]-1,2,4-triazolo[4,3-a]-1,4-diazepine and of some related compounds》. The article mentions the following:

Title compounds I (R = MeO, EtO, MeS, n = 2; R = MeO, n = 3) were prepared by alkylation of thienotriazolodiazepine II (R1 = R2 = Br) with substituted piperazines. I (R = PhO, PhS, n = 2) were prepared by alkylation of I (R1 = piperazino, R2 = Br). Cyclization of hydrazinothienodiazepine III with ClC(OEt)3 gave II (R1 = R2 = H), which could only be brominated to give I (R1 = Br, R2 = H). Some intermediates were prepared for the synthesis etizolam. I had less anticonvulsant activity than 8-chloro-6-(2-chlorophenyl)-1-piperazino-4H-s-triazolo[4,3-a]-1,4-benzodiazepines. The results came from multiple reactions, including the reaction of 2-Amino-N-(3-(2-chlorobenzoyl)-5-ethylthiophen-2-yl)acetamide(cas: 50509-09-6Application In Synthesis of 2-Amino-N-(3-(2-chlorobenzoyl)-5-ethylthiophen-2-yl)acetamide)

2-Amino-N-(3-(2-chlorobenzoyl)-5-ethylthiophen-2-yl)acetamide(cas: 50509-09-6) belongs to anime. Hydrogen peroxide (H2O2) and peroxy acids generally add an oxygen atom to the nitrogen of amines. With primary amines, this step is normally followed by further oxidation, leading to nitroso compounds, RNO, or nitro compounds, RNO2. Secondary amines are converted to hydroxylamines, R2NOH, and tertiary amines to amine oxides, R3NO.Application In Synthesis of 2-Amino-N-(3-(2-chlorobenzoyl)-5-ethylthiophen-2-yl)acetamide

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

The author of 《Simultaneous infrared-ultrasound irradiation in organic synthesis: acylation of amines alcohols and amino alcohols》 were Luna-Mora, Ricardo Alfredo; Ortega-Jimenez, Fernando; Rios-Guerra, Hulme; Garcia-Estrada, Jose Guadalupe; Perez-Flores, Francisco Javier; Gonzalez-Carrillo, Jessica; Torres-Reyes, Angeles; Moreno-Gonzalez, Linda; Martinez-Zaldivar, Alejandro; Penieres-Carrillo, Jose Guillermo. And the article was published in Journal of the Mexican Chemical Society in 2019. Product Details of 70298-88-3 The author mentioned the following in the article:

The acylation of both aliphatic and aromatic amines, alcs. and amino alcs. by simultaneous IR-ultrasound irradiation (SIUI) in solvent-free conditions in short reaction times and with good to excellent yields was achieved. The results obtained with SIUI and for thermal, IR and ultrasound energy sources are compared. This is the first report regarding to the application of SIUI in acylation reactions. In the part of experimental materials, we found many familiar compounds, such as 2,2-Dimehtyl-N-pyridin-3-yl-propionamide(cas: 70298-88-3Product Details of 70298-88-3)

2,2-Dimehtyl-N-pyridin-3-yl-propionamide(cas: 70298-88-3) belongs to anime. Acylation is one of the most important reactions of primary and secondary amines; a hydrogen atom is replaced by an acyl group (a group derived from an acid, such as RCOOH or RSO3H, by removal of ―OH, such as RC(=O)―, RS(O)2―, and so on). Reagents may be acid chlorides (RCOC1, RSO2C1), anhydrides ((RCO)2O), or even esters (RCOOR′); the products are amides of the corresponding acids.Product Details of 70298-88-3

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Synthetic Route of C7H9NO2SIn 2020 ,《Au(I)/Au(III)-Catalyzed C-N coupling》 appeared in Chemical Communications (Cambridge, United Kingdom). The author of the article were Rodriguez, Jessica; Adet, Nicolas; Saffon-Merceron, Nathalie; Bourissou, Didier. The article conveys some information:

Cycling between Au(I) and Au(III) is challenging, so gold-catalyzed cross-couplings are rare. The (MeDalphos)AuCl complex, which the authors showed was prone to undergo oxidative addition, is reported here to efficiently catalyze the C-N coupling of aryl iodides and amines. The transformation does not require an external oxidant or a directing group. It is robust and works with a wide scope of aryl iodides and N-nucleophiles under mild conditions. Mechanistic studies, including the NMR and MS characterization of a key aryl amido Au(III) complex, strongly support a 2e redox cycle in which oxidative addition precedes transmetalation and reductive elimination is the rate-determining step.4-Methylbenzenesulfonamide(cas: 70-55-3Synthetic Route of C7H9NO2S) was used in this study.

4-Methylbenzenesulfonamide(cas: 70-55-3) belongs to anime. The reaction of alkyl halides, R―X, where X is a halogen, or analogous reagents with ammonia (or amines) is useful with certain compounds. Not all alkyl halides are effective reagents; the reaction is sluggish with secondary alkyl groups and fails with tertiary ones. Its usefulness is largely confined to primary alkyl halides (those having two hydrogen atoms on the reacting site).Synthetic Route of C7H9NO2S

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Application In Synthesis of N-Methoxy-N-methylacetamideIn 2020 ,《Oral administration of royal jelly may improve the preservation of rooster spermatozoa》 was published in Journal of Animal Physiology and Animal Nutrition. The article was written by Rahnama, Golsomeh; Deldar, Hamid; Ansari Pirsaraei, Zarbakht; Kazemifard, Mohammad. The article contains the following contents:

The aim of the present study was to investigate the effect of dietary supplementation of royal jelly (RJ) on liquid and frozen storage of rooster spermatozoa. Twenty-five 30-wk-old of Mazandaran native breeder roosters were randomly divided into five treatments (n = 5 roosters/group). Exptl. treatments are designed to include a control group and various levels (0.0 (RJ0), 100 (RJ100), 200 (RJ200), 300 (RJ300) mg kg-1 BW-1) of royal jelly (RJ) that were fed to the roosters using force-feed method. The result of this study showed that the spermatozoa forward progressive motility, abnormality, membrane integrity, and viability were improved by the RJ100 group compared to the other groups after 24 and 48 h storage period at 4°C. The percentage of membrane integrity and forward progressive motility after freeze-thawing in the RJ100 group was significantly higher than the other groups, and the percentage of abnormal spermatozoa was lower. A significant decrease in semen quality parameters was seen after 24 and 48 h of refrigeration, but there was no observed change between 2 and 24 h in the RJ100. Moreover, after freeze-thawing, DNA integrity and mitochondrial activity in the RJ100 group were significantly higher than the other groups. According to our results, feeding of RJ at 100 mg kg-1 BW-1 to the roosters was improved spermatozoa characteristics during liquid and cryopreservation conditions. In the experiment, the researchers used N-Methoxy-N-methylacetamide(cas: 78191-00-1Application In Synthesis of N-Methoxy-N-methylacetamide)

N-Methoxy-N-methylacetamide(cas: 78191-00-1) belongs to anime. Milder oxidation, using reagents such as NaOCl, can remove four hydrogen atoms from primary amines of the type RCH2NH2 to form nitriles (R―C≡N), and oxidation with reagents such as MnO2 can remove two hydrogen atoms from secondary amines (R2CH―NHR′) to form imines (R2C=NR′). Tertiary amines can be oxidized to enamines (R2C=CHNR2) by a variety of reagents.Application In Synthesis of N-Methoxy-N-methylacetamide

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics