Tag: 100-200

Identification of the novel N-phenylbenzenesulfonamide derivatives as potent HIV inhibitors was written by Sun, Yong;Lu, Cui-Lin;Wang, Chang-Yuan;Wang, Rui-Rui;Liu, Ke-Xin;Yang, Liu-Meng;Zhen, Yu-Hong;Zhang, Hou-Li;Wang, Chao;Zheng, Yong-Tang;Ma, Xiao-Dong. And the article was included in Chinese Chemical Letters in 2015.Synthetic Route of C7H10N2O2S This article mentions the following:

Searching for more safe and effective agents for HIV treatments is still an urgent topic worldwide. Based on our continuous modifications on the benzophenone derivatives as HIV-1 reverse transcriptase (RT) inhibitors, a new template bearing N-phenylbenzenesulfonamide (PBSA) structure was designed to enhance the interactions with HIV-1 RT. In this manuscript, a series of PBSA derivatives were synthesized and evaluated for their anti-HIV-1 activity. The preliminary test showed that these compounds were potent to inhibit wild-type HIV-1 with EC₅₀ values ranging of 0.105-14.531 μmol/L. In particular, compound 13f not only has high anti-HIV-1 activity (0.108 μmol/L), but also possesses low toxicity with a TI value of 1816.6. Furthermore, the major interactions of the inhibitor 13f with HIV-1 RT were also investigated using the mol. modeling. Our discovered structure-activity relationships (SARs) of these analogs may serve as an important clue for further optimizations. In the experiment, the researchers used many compounds, for example, 4-Amino-3-methylbenzenesulfonamide (cas: 53297-70-4Synthetic Route of C7H10N2O2S).

4-Amino-3-methylbenzenesulfonamide (cas: 53297-70-4) belongs to amides. Amides can be viewed as a derivative of a carboxylic acid RC(=O)OH with the hydroxyl group –OH replaced by an amine group −NR′R″; or, equivalently, an acyl (alkanoyl) group RC(=O)− joined to an amine group. Amides can be freed from solvent or water by drying below their melting points. These purifications can also be used for sulfonamides and acid hydrazides.Synthetic Route of C7H10N2O2S

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

Ce(III) immobilised on aminated epichlorohydrin-activated agarose matrix – “green” and efficient catalyst for transamidation of carboxamides was written by Zarei, Zeinab;Akhlaghinia, Batool. And the article was included in Chemical Papers in 2015.Recommanded Product: 2670-38-4 This article mentions the following:

The present study reports the preparation and characterization of Ce(III) immobilized on an aminated epichlorohydrin-activated agarose matrix (CAEA) as a green catalyst. The catalyst was synthesized by the reaction of the epichlorohydrin-activated agarose matrix with ammonia solution, which was then treated with Ce(NO₃)₃·6H₂O. The catalyst (CAEA) was characterized by FT-IR, far IR, elemental anal., XRD, TGA and ICP techniques. CAEA was found to be an effective and reusable heterogeneous catalyst for the transamidation of carboxamides with amines under solvent-free conditions. The catalyst was successfully applied to the synthesis of a wide range of aromatic and aliphatic amides. High efficiency, mild reaction conditions, easy work-up and simple separation were the important advantages of this catalyst. In the experiment, the researchers used many compounds, for example, 3,4-Dichlorobenzamide (cas: 2670-38-4Recommanded Product: 2670-38-4).

3,4-Dichlorobenzamide (cas: 2670-38-4) belongs to amides. Compared to amines, amides are very weak bases and do not have clearly defined acid–base properties in water. On the other hand, amides are much stronger bases than esters, aldehydes, and ketones. Ionic, or saltlike, amides are strongly alkaline compounds ordinarily made by treating ammonia, an amine, or a covalent amide with a reactive metal such as sodium.Recommanded Product: 2670-38-4

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

Palladium-Catalyzed One-Pot Synthesis of Quinazolinones via tert-Butyl Isocyanide Insertion was written by Jiang, Xiao;Tang, Ting;Wang, Jin-Mei;Chen, Zhong;Zhu, Yong-Ming;Ji, Shun-Jun. And the article was included in Journal of Organic Chemistry in 2014.Quality Control of 2-Amino-4-fluorobenzamide This article mentions the following:

A novel palladium-catalyzed three-component reaction for the synthesis of quinazolin-4(3H)-ones from readily available 2-aminobenzamides and aryl halides via a palladium-catalyzed isocyanide insertion/cyclization sequence has been developed. This methodol. efficiently constructs quinazolin-4(3H)-ones in moderate to excellent yields with the advantages of operational simplicity. E.g., in presence of PdCl₂, DPPP, CaCl₂, and t-BuONa in toluene at 145 °C, reaction of IPh, anthranilamide, and t-BuNC gave 93% quinazolin-4(3H)-one derivative (I). In the experiment, the researchers used many compounds, for example, 2-Amino-4-fluorobenzamide (cas: 119023-25-5Quality Control of 2-Amino-4-fluorobenzamide).

2-Amino-4-fluorobenzamide (cas: 119023-25-5) belongs to amides. Amides include many other important biological compounds, as well as many drugs like paracetamol, penicillin and LSD. Low-molecular-weight amides, such as dimethylformamide, are common solvents. The presence of the amide group –C(=O)N– is generally easily established, at least in small molecules. It can be distinguished from nitro and cyano groups in IR spectra. Amides exhibit a moderately intense νCO band near 1650 cm−1. By 1H NMR spectroscopy, CONHR signals occur at low fields. In X-ray crystallography, the C(=O)N center together with the three immediately adjacent atoms characteristically define a plane.Quality Control of 2-Amino-4-fluorobenzamide

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

A formal synthesis of althiomycin was written by Toogood, Peter L.;Hollenbeck, Jessica J.;Lam, Huong M.;Li, Li. And the article was included in Bioorganic & Medicinal Chemistry Letters in 1996.HPLC of Formula: 61189-99-9 This article mentions the following:

The thiazolecarboxylate and amine fragments previously used in the preparation of althiomycin were prepared in a formal synthesis of althiomycin for studies of its interaction with prokaryotic ribosomes. In the experiment, the researchers used many compounds, for example, 2,2-Diethoxyacetamide (cas: 61189-99-9HPLC of Formula: 61189-99-9).

2,2-Diethoxyacetamide (cas: 61189-99-9) belongs to amides. The solubilities of amides and esters are roughly comparable. Typically amides are less soluble than comparable amines and carboxylic acids since these compounds can both donate and accept hydrogen bonds. Tertiary amides, with the important exception of N,N-dimethylformamide, exhibit low solubility in water. Ionic, or saltlike, amides are strongly alkaline compounds ordinarily made by treating ammonia, an amine, or a covalent amide with a reactive metal such as sodium.HPLC of Formula: 61189-99-9

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

Stereoselective Synthesis of the γ-Lactam Hydrolysate of the Thiopeptide Cyclothiazomycin was written by Bagley, Mark C.;Xiong, Xin. And the article was included in Organic Letters in 2004.Related Products of 61189-99-9 This article mentions the following:

Chiral nonracemic thiazolylpropynone enamine I undergoing Bohlmann-Rahtz pyridine synthesis afforded a pyridine-containing γ-amino acid II in high optical purity that proceeded with total control of regiochem. and with minimal racemization. II was further modified to γ-lactam III, hydrolyzate of the macrocyclic thiopeptide antibiotic cyclothiazomycin, a selective renin inhibitor. Thus, III was synthesized in only four steps with 30% overall yield and 88% enantiomeric excess. In the experiment, the researchers used many compounds, for example, 2,2-Diethoxyacetamide (cas: 61189-99-9Related Products of 61189-99-9).

2,2-Diethoxyacetamide (cas: 61189-99-9) belongs to amides. The solubilities of amides and esters are roughly comparable. Typically amides are less soluble than comparable amines and carboxylic acids since these compounds can both donate and accept hydrogen bonds. Tertiary amides, with the important exception of N,N-dimethylformamide, exhibit low solubility in water. Amides are stable compounds. The lower-melting members (such as acetamide) can be readily purified by fractional distillation. Most amides are solids which have low solubilities in water.Related Products of 61189-99-9

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

Expeditious and Chemoselective Synthesis of α-Aryl and α-Alkyl Selenomethylketones via Homologation Chemistry was written by Senatore, Raffaele;Castoldi, Laura;Ielo, Laura;Holzer, Wolfgang;Pace, Vittorio. And the article was included in Organic Letters in 2018.Application of 226260-01-1 This article mentions the following:

Diselenoacetals, previously considered byproducts in homologation tactics en route to α-selenoketones, are herein found to be excellent starting materials for this purpose. The easy selenium/lithium exchange they undergo affords seleno carbanions which are smoothly added to Weinreb amides to chemoselectively prepare α-aryl- and α-alkyl seleno methylketones through a single chem. operation. No racemization events are observed in the presence of optically pure starting materials. In the experiment, the researchers used many compounds, for example, 3-Fluoro-N-methoxy-N-methylbenzamide (cas: 226260-01-1Application of 226260-01-1).

3-Fluoro-N-methoxy-N-methylbenzamide (cas: 226260-01-1) belongs to amides. The solubilities of amides and esters are roughly comparable. Typically amides are less soluble than comparable amines and carboxylic acids since these compounds can both donate and accept hydrogen bonds. Tertiary amides, with the important exception of N,N-dimethylformamide, exhibit low solubility in water. Amides can be recrystallised from large quantities of water, ethanol, ethanol/ether, aqueous ethanol, chloroform/toluene, chloroform or acetic acid. The likely impurities are the parent acids or the alkyl esters from which they have been made. The former can be removed by thorough washing with aqueous ammonia followed by recrystallisation, whereas elimination of the latter is by trituration or recrystallisation from an organic solvent.Application of 226260-01-1

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

3-(7-Azaindolyl)-4-arylmaleimides as potent, selective inhibitors of glycogen synthase kinase-3 was written by Zhang, Han-Cheng;Ye, Hong;Conway, Bruce R.;Derian, Claudia K.;Addo, Michael F.;Kuo, Gee-Hong;Hecker, Leonard R.;Croll, Diane R.;Li, Jian;Westover, Lori;Xu, Jun Z.;Look, Richard;Demarest, Keith T.;Andrade-Gordon, Patricia;Damiano, Bruce P.;Maryanoff, Bruce E.. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2004.Electric Literature of C8H8ClNO This article mentions the following:

A novel series of acyclic 3-(7-azaindolyl)-4-(aryl/heteroaryl)maleimides, e.g., I and II, was synthesized and evaluated for activity against GSK-3β and selectivity vs. PKC-βII, as well as a broad panel of protein kinases. Compounds I and II potently inhibited GSK-3β (IC₅₀=7 and 26 nM, resp.) and exhibited excellent selectivity over PKC-βII (325 and >385-fold, resp.). Compound I was also highly selective against 68 other protein kinases. In a cell-based functional assay, both I and II effectively increased glycogen synthase activity by inhibiting GSK-3β. In the experiment, the researchers used many compounds, for example, 2-(2-Chlorophenyl)acetamide (cas: 10268-06-1Electric Literature of C8H8ClNO).

2-(2-Chlorophenyl)acetamide (cas: 10268-06-1) belongs to amides. In primary and secondary amides, the presence of N–H dipoles allows amides to function as H-bond donors as well. Thus amides can participate in hydrogen bonding with water and other protic solvents; the oxygen atom can accept hydrogen bonds from water and the N–H hydrogen atoms can donate H-bonds. Amides are stable compounds. The lower-melting members (such as acetamide) can be readily purified by fractional distillation. Most amides are solids which have low solubilities in water.Electric Literature of C8H8ClNO

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

Indicators for the Exposure Assessment of Transformation Products of Organic Micropollutants was written by Gasser, Lukas;Fenner, Kathrin;Scheringer, Martin. And the article was included in Environmental Science & Technology in 2007.Reference of 2670-38-4 This article mentions the following:

Environmental transformation products of organic trace pollutants have the potential to be similarly or even more mobile, persistent, or toxic than their parent compounds They should, therefore, be included in chem. hazard and risk assessment procedures, as well as in the assessment of soil and water quality. To fulfill this requirement most efficiently, screening approaches that select relevant transformation products for detailed assessment are needed. This paper presents two process-based multimedia, multispecies models that allow us to quant. estimate the environmental fate of transformation products. The resulting exposure patterns are assessed with two indicators: joint persistence (JP), which describes the temporal extent of environmental exposure to a parent compound and its transformation products, and the predicted relative aquatic concentrations (RACs), which estimate the relative concentrations of parent compounds and their transformation products in surface water bodies. As a case study, JP and RAC are calculated for 16 pesticides and their relevant transformation products. The results for the JP indicator confirm the importance of considering transformation products in the assessment of overall persistence; for example, in the context of PBT (physiol. based toxicokinetics) assessments. Comparison of RAC results with monitoring data on herbicides and their transformation products shows the suitability of our approach for estimating relative concentrations in surface water, and, as a consequence, its usefulness in identifying transformation products for future water quality monitoring programs. Transformation products of triketones and other highly used acidic herbicides are specifically identified as targets. In the experiment, the researchers used many compounds, for example, 3,4-Dichlorobenzamide (cas: 2670-38-4Reference of 2670-38-4).

3,4-Dichlorobenzamide (cas: 2670-38-4) belongs to amides. Amides can be viewed as a derivative of a carboxylic acid RC(=O)OH with the hydroxyl group –OH replaced by an amine group −NR′R″; or, equivalently, an acyl (alkanoyl) group RC(=O)− joined to an amine group. Ionic, or saltlike, amides are strongly alkaline compounds ordinarily made by treating ammonia, an amine, or a covalent amide with a reactive metal such as sodium.Reference of 2670-38-4

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

Organophotocatalytic selective deuterodehalogenation of aryl or alkyl chlorides was written by Li, Yanjun;Ye, Ziqi;Lin, Yu-Mei;Liu, Yan;Zhang, Yumeng;Gong, Lei. And the article was included in Nature Communications in 2021.Quality Control of 6-Chloro-N,N-dimethylnicotinamide This article mentions the following:

A photocatalytic system consisting of an aryl-amine photocatalyst and a disulfide co-catalyst in the presence of sodium formate as an electron and hydrogen donor was developed. Accordingly, many aryl chlorides, alkyl chlorides, and other halides were converted to deuterated products at room temperature in air (>90 examples, up to 99% D-incorporation). The mechanistic studies revealed that the aryl amine served as reducing photoredox catalyst to initiate cleavage of the C-Cl bond, at the same time as energy transfer catalyst to induce homolysis of the disulfide for consequent deuterium transfer process. This economic and environmentally-friendly method could be used for site-selective D-labeling of a number of bioactive mols. and direct H/D exchange of some drug mols. In the experiment, the researchers used many compounds, for example, 6-Chloro-N,N-dimethylnicotinamide (cas: 54864-83-4Quality Control of 6-Chloro-N,N-dimethylnicotinamide).

6-Chloro-N,N-dimethylnicotinamide (cas: 54864-83-4) belongs to amides. Amides are pervasive in nature and technology. Proteins and important plastics like Nylons, Aramid, Twaron, and Kevlar are polymers whose units are connected by amide groups (polyamides); these linkages are easily formed, confer structural rigidity, and resist hydrolysis. Amides are stable compounds. The lower-melting members (such as acetamide) can be readily purified by fractional distillation. Most amides are solids which have low solubilities in water.Quality Control of 6-Chloro-N,N-dimethylnicotinamide

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

Bronsted acid-assisted N-alkylation of sulfonamides using ethers as the alkylation reagents was written by Shi, Wei;Bai, Chun-Mei;Zhu, Kai;Cui, Dong-Mei;Zhang, Chen. And the article was included in Tetrahedron in 2014.Application of 5339-69-5 This article mentions the following:

N-Alkylation of sulfonamides using cyclic ethers as alkylation reagents and Bronsted acid as a catalyst produced pyrrolidine and piperidine derivatives in good yields. When using sym. and unsym. ethers as alkylation reagents, mono-N-alkylation of sulfonamides took place to afford the corresponding products. In the experiment, the researchers used many compounds, for example, N-Isopropylbenzenesulfonamide (cas: 5339-69-5Application of 5339-69-5).

N-Isopropylbenzenesulfonamide (cas: 5339-69-5) belongs to amides. In primary and secondary amides, the presence of N–H dipoles allows amides to function as H-bond donors as well. Thus amides can participate in hydrogen bonding with water and other protic solvents; the oxygen atom can accept hydrogen bonds from water and the N–H hydrogen atoms can donate H-bonds. Amides can be recrystallised from large quantities of water, ethanol, ethanol/ether, aqueous ethanol, chloroform/toluene, chloroform or acetic acid. The likely impurities are the parent acids or the alkyl esters from which they have been made. The former can be removed by thorough washing with aqueous ammonia followed by recrystallisation, whereas elimination of the latter is by trituration or recrystallisation from an organic solvent.Application of 5339-69-5

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