Month: January 2023

Sustainable and chemoselective N-Boc protection of amines in biodegradable deep eutectic solvent was written by Azizi, Najmedin;Shirdel, Fatemeh. And the article was included in Monatshefte fuer Chemie in 2017.Name: tert-Butyl (4-chlorophenyl)carbamate This article mentions the following:

A green and practical approach for the chemoselective N-tert-butyloxycarbonylation of structurally diverse amines with di-tert-Bu dicarbonate (Boc₂O) is described. Selective N-Boc protection was achieved in excellent yields in urea-choline chloride deep eutectic solvent (DES) as the most promising environmentally benign and cost-effective solvent under mild reaction conditions. DES can protect various aromatic and aliphatic amines using Boc₂O in good to excellent yields in short reaction times without any side products. In the experiment, the researchers used many compounds, for example, tert-Butyl (4-chlorophenyl)carbamate (cas: 18437-66-6Name: tert-Butyl (4-chlorophenyl)carbamate).

tert-Butyl (4-chlorophenyl)carbamate (cas: 18437-66-6) belongs to organic chlorides. Chlorinated organic compounds are found in nearly every class of biomolecules and natural products including alkaloids, terpenes, amino acids, flavonoids, steroids, and fatty acids. Alkyl chlorides readily react with amines to give substituted amines. Alkyl chlorides are substituted by softer halides such as the iodide in the Finkelstein reaction.Name: tert-Butyl (4-chlorophenyl)carbamate

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Nitropyridines as 2π-Partners in 1,3-Dipolar Cycloadditions with N-Methyl Azomethine Ylide: An Easy Access to Condensed Pyrrolines was written by Bastrakov, Maxim A.;Fedorenko, Alexey K.;Starosotnikov, Alexey M.;Shakhnes, Alexander Kh.. And the article was included in Molecules in 2021.Reference of 59237-53-5 This article mentions the following:

1,3-Dipolar cycloaddition reactions of 2-substituted 5-R-3-nitropyridines and isomeric 3-R-5-nitropyridines with N-Me azomethine ylide were studied. The effect of the substituent at positions 2 and 5 of the pyridine ring on the possibility of the [3+2]-cycloaddition process was revealed. A number of new derivatives of pyrroline and pyrrolidine condensed with a pyridine ring were synthesized. In the experiment, the researchers used many compounds, for example, Methyl 6-chloro-5-nitronicotinate (cas: 59237-53-5Reference of 59237-53-5).

Methyl 6-chloro-5-nitronicotinate (cas: 59237-53-5) belongs to organic chlorides. Organochlorines are organic compounds having multiple chlorine atoms. They were the first synthetic pesticides that were used in agriculture. They are resistant to most microbial and chemical degradations. Aliphatic organochlorides are often alkylating agents as chlorine can act as a leaving group, which can result in cellular damage.Reference of 59237-53-5

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Combating multi-drug resistant malaria parasite by inhibiting falcipain-2 and heme-polymerization: Artemisinin-peptidyl vinyl phosphonate hybrid molecules as new antimalarials was written by Aratikatla, Eswar K.;Kalamuddin, Md;Rana, Kalpeshkumar C.;Datta, Gaurav;Asad, Mohd;Sundararaman, Srividhya;Malhotra, Pawan;Mohmmed, Asif;Bhattacharya, Asish K.. And the article was included in European Journal of Medicinal Chemistry in 2021.Recommanded Product: (Chloromethanetriyl)tribenzene This article mentions the following:

Artemisinin-based combination therapies (ACTs) have been able to reduce the clin. and pathol. malaria cases in endemic areas around the globe. However, recent reports have shown a progressive decline in malaria parasite clearance in South-east Asia after ACT treatment, thus envisaging a need for new artemisinin (ART) derivatives and combinations. To address the emergence of drug resistance to current antimalarials, here we report the synthesis of artemisinin-peptidyl vinyl phosphonate hybrid mols. that show superior efficacy than artemisinin alone against chloroquine-resistant as well as multidrug-resistant Plasmodium falciparum strains with EC₅₀ in pico-molar ranges. Further, the compounds effectively inhibited the survival of ring-stage parasite for laboratory-adapted artemisinin-resistant parasite lines as compared to artemisinin. These hybrid mols. showed complete parasite clearance in vivo using P. berghei mouse malaria model in comparison to artemisinin alone. Studies on the mode of action of hybrid mols. suggested that these artemisinin-peptidyl vinyl phosphonate hybrid mols. possessed dual activities: inhibited falcipain-2 (FP-2) activity, a P. falciparum cysteine protease involved in Hb degradation, and also blocked the hemozoin formation in the food-vacuole, a step earlier shown to be blocked by artemisinin. Since these hybrid mols. blocked multiple steps of a pathway and showed synergistic efficacies, we believe that these lead compounds can be developed as effective antimalarials to prevent the spread of resistance to current antimalarials. In the experiment, the researchers used many compounds, for example, (Chloromethanetriyl)tribenzene (cas: 76-83-5Recommanded Product: (Chloromethanetriyl)tribenzene).

(Chloromethanetriyl)tribenzene (cas: 76-83-5) belongs to organic chlorides. Organochlorines stimulate the central nervous system and cause convulsions, tremor, nausea, and mental confusion. Examples are dichlorodiphenyltrichloroethane (DDT), chlordane, lindane, endosulfan, and dieldrin. Organochlorine compounds are lipophylic, meaning they are more soluble in fat than in water. This gives them a high tenancy to accumulate in the food chain (biomagnification).Recommanded Product: (Chloromethanetriyl)tribenzene

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Sustainable electrospray polymerization fabrication of thin-film composite polyamide nanofiltration membranes for heavy metal removal was written by Ma, Zhongbao;Ren, Long-Fei;Ying, Diwen;Jia, Jinping;Shao, Jiahui. And the article was included in Desalination in 2022.Quality Control of Trimesoylchloride This article mentions the following:

Thin-film composite polyamide (TFC-PA) nanofiltration membrane is promising in heavy metal removal due to its excellent performance and high economic benefits. However, the common interfacial polymerization (IP) fabrication method requires abundant toxic and harmful solvents, causing harm to the environment and humans. Therefore, novel green, low-carbon and sustainable fabrication methods are urgently needed. Here, we reported a sustainable electrospray polymerization (SEP) technique for TFC-PA membrane preparation via electrospray featuring no toxic solvent, near-complete monomer conversion, and zero waste liquid discharge. In this process, 2-methyl-tetrahydrofuran and ethanol were used as green solvents, and its greenness was assessed by green metrics and toxicity bioassays. Phys. features and physicochem. properties of SEP membranes were characterized by SEM, TEM, AFM and XPS. Membranes with different surface charges and pore sizes could be tailored by varying the monomer concentration The optimal membrane exhibited excellent removal efficiency of toxic heavy metal ions, in which the rejection rates of Cu2+ and Ni2+ were higher than 97.0 %. In addition, the permeability and salt rejection of SEP membranes were better than those of IP membranes. Our sustainable electrospray polymerization method provides a versatile green platform for fabricating TFC membranes and may facilitate the development of sustainable nanofiltration membranes. In the experiment, the researchers used many compounds, for example, Trimesoylchloride (cas: 4422-95-1Quality Control of Trimesoylchloride).

Trimesoylchloride (cas: 4422-95-1) belongs to organic chlorides. An organic chloride is an organic compound containing at least one covalently bonded atom of chlorine. Their wide structural variety and divergent chemical properties lead to a broad range of names and applications. The haloform reaction, using chlorine and sodium hydroxide, is also able to generate alkyl halides from methyl ketones, and related compounds. Chloroform was formerly produced thus.Quality Control of Trimesoylchloride

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Effects of monomer rigidity on microstructures and properties of novel polyamide thin-film composite membranes prepared through interfacial polymerization for pervaporation dehydration was written by Lee, Jen-Yu;Huang, Ting-Yi;Belle Marie Yap Ang, Micah;Huang, Shu-Hsien;Tsai, Hui-An;Jeng, Ru-Jong. And the article was included in Journal of Membrane Science in 2022.Synthetic Route of C9H3Cl3O3 This article mentions the following:

In this study, thin-film composite (TFC) membranes were produced through interfacial polymerization between diamine and trimesoyl chloride on a polyetherimide (PEI) support. The TFC membranes with different diamines, 4,4′-((propane-2,2-diylbis(4,1-phenylene))bis(oxy))dianiline (BAPP), 4,4′-((methylene bis(4,1-phenylene))bis(oxy))dianiline (MPDA), and 6,6′-bis(4-aminopheoxy)-4,4,4′,4′,7,7′-hexamethyl-2,2′-spirobichroman (SBC), were denoted as TFC_PEI/B, TFC_PEI/M, and TFC_PEI/S, resp. These three aromatic diamines have different central moieties that affect reactivity during the interfacial polymerization reaction. The crosslinking degree of the TFC membranes increased in the following order: TFC_PEI/S < TFC_PEI/M < TFC_PEI/B. Positron annihilation lifetime spectroscopy anal. also unveils that TFC_PEI/B had the lowest free volume These results reveal that the appropriate steric structure of the diamine mols. can create less compact structure without impeding the formation of the crosslinked polyamide selective layer. Moreover, the TFC_PEI/B membrane had a flux of approx. 705±46 g•m^-2 h^-1, and the water concentration in the permeate was maintained at approx. 99.8% at 25° during the 70% isopropanol solution dehydration. Furthermore, the TFC_PEI/B membrane can be operated under broad operating conditions and possesses high long-term stability. In the experiment, the researchers used many compounds, for example, Trimesoylchloride (cas: 4422-95-1Synthetic Route of C9H3Cl3O3).

Trimesoylchloride (cas: 4422-95-1) belongs to organic chlorides. Chlorinated organic compounds are found in nearly every class of biomolecules and natural products including alkaloids, terpenes, amino acids, flavonoids, steroids, and fatty acids. The haloform reaction, using chlorine and sodium hydroxide, is also able to generate alkyl halides from methyl ketones, and related compounds. Chloroform was formerly produced thus.Synthetic Route of C9H3Cl3O3

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Simple Synthesis of Fused Thiazolo[4,5-b]pyridines through Successive SN Ar Processes was written by Starosotnikov, Alexey M.;Bastrakov, Maxim A.;Kachala, Vadim V.;Fedyanin, Ivan V.;Klimova, Tatyana A.;Ivanova, Victoria V.;Dalinger, Igor L.. And the article was included in Synlett in 2021.Application of 59237-53-5 This article mentions the following:

A convenient process is described for the synthesis of novel thiazolo[4,5-b]pyridines fused with triazole or pyrimidine rings. The base-promoted reactions of 2-chloro-3-nitropyridines with 1,3-( S, N)-binucleophiles (triazole-5-thiols, 4-oxopyrimidine-2-thiones) resulted in nucleophilic substitution of the chlorine atom and subsequent S-N-type Smiles rearrangement followed by nucleophilic substitution of the nitro group. Reactions with pyrimidine-2-thiones were carried out as one-pot processes while, in the case of triazole-5-thiols, isolation of intermediate substitution products was found to be preferable. In the experiment, the researchers used many compounds, for example, Methyl 6-chloro-5-nitronicotinate (cas: 59237-53-5Application of 59237-53-5).

Methyl 6-chloro-5-nitronicotinate (cas: 59237-53-5) belongs to organic chlorides. Chlorination modifies the physical properties of hydrocarbons in several ways. These compounds are typically denser than water due to the higher atomic weight of chlorine versus hydrogen. Aryl chlorides may be prepared by the Friedel-Crafts halogenation, using chlorine and a Lewis acid catalyst.Application of 59237-53-5

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Design, synthesis, and biological evaluation of a novel series of 2-(2,6-dioxopiperidin-3-yl)isoquinoline-1,3(2H,4H)-dione derivatives as cereblon modulators was written by Liu, Yilin;Song, Yuming;Xu, Yingju;Jiang, Meixu;Lu, Haibin. And the article was included in Journal of Enzyme Inhibition and Medicinal Chemistry in 2022.Quality Control of 2-Chloro-6-nitrobenzoic acid This article mentions the following:

In the current study, we designed and synthesized a novel series of 2-(2,6-dioxopiperidin-3-yl)isoquinoline-1,3(2H,4H)-dione derivatives as cereblon (CRBN) modulators. The results of the CCK8 assay revealed potent antiproliferative activity for the selected compound against NCI-H929 (IC50=2.25 μM) and U239 (IC50=5.86 μM) cell lines. Compound also can inhibit the TNF-α level (IC50=0.76 μM) in LPS stimulated PMBC and showed nearly no toxicity to this normal human cell line. The TR-FRET assay showed compound having potent inhibitory activity against CRBN (IC50=4.83 μM), and the docking study confirmed a nice fitting of into the active sites of CRBN. Further biol. studies revealed compound can increase the apoptotic events, arrest the NCI-H929 cells at G0/G1 cell cycle, and induce the ubiquitination degradation of IKZF1 and IKZF3 proteins by CRL4CRBN. These preliminary results suggested that compound could serve as a potential antitumor drug and worthy of further investigation. In the experiment, the researchers used many compounds, for example, 2-Chloro-6-nitrobenzoic acid (cas: 5344-49-0Quality Control of 2-Chloro-6-nitrobenzoic acid).

2-Chloro-6-nitrobenzoic acid (cas: 5344-49-0) belongs to organic chlorides. An organic chloride is an organic compound containing at least one covalently bonded atom of chlorine. Their wide structural variety and divergent chemical properties lead to a broad range of names and applications. Aryl chlorides may be prepared by the Friedel-Crafts halogenation, using chlorine and a Lewis acid catalyst.Quality Control of 2-Chloro-6-nitrobenzoic acid

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Cu-Catalysed intramolecular radical enantioconvergent tertiary β-C(sp³)-H amination of racemic ketones was written by Yang, Chang-Jiang;Zhang, Chi;Gu, Qiang-Shuai;Fang, Jia-Heng;Su, Xiao-Long;Ye, Liu;Sun, Yan;Tian, Yu;Li, Zhong-Liang;Liu, Xin-Yuan. And the article was included in Nature Catalysis in 2020.Electric Literature of C7H4ClF3O2S This article mentions the following:

Herein, the combination of decoupled hydrogen atom abstraction with asym. copper catalysis for enantioconvergent tertiary β-C(sp³)-H amination of racemic ketones was described. This method, when allied with follow-up transformations, provided facile access to a range of enantioenriched compounds I [R = t-Bu, Ph, 3-thienyl, etc.; R¹ = Me, CH₂CO₂Me, allyl, etc.; R² = Ph, 2-thienyl, 3-thienyl, 3-MeC₆H₄; Ar = Ph, 4-tolyl, 2-naphthyl, etc.] featuring quaternary stereocenters. In the experiment, the researchers used many compounds, for example, 3-(Trifluoromethyl)benzene-1-sulfonyl chloride (cas: 777-44-6Electric Literature of C7H4ClF3O2S).

3-(Trifluoromethyl)benzene-1-sulfonyl chloride (cas: 777-44-6) belongs to organic chlorides. Organochlorines stimulate the central nervous system and cause convulsions, tremor, nausea, and mental confusion. Examples are dichlorodiphenyltrichloroethane (DDT), chlordane, lindane, endosulfan, and dieldrin. Aryl chlorides may be prepared by the Friedel-Crafts halogenation, using chlorine and a Lewis acid catalyst.Electric Literature of C7H4ClF3O2S

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Synthesis, spectral characterization, docking studies and biological activity of urea, thiourea, sulfonamide and carbamate derivatives of imatinib intermediate was written by Chandrasekhar, Mandala;Prasad, Gandavaram Syam;Venkataramaiah, Chintha;Naga Raju, Chamarthi;Seshaiah, Kalluru;Rajendra, Wudayagiri. And the article was included in Molecular Diversity in 2019.HPLC of Formula: 777-44-6 This article mentions the following:

A series of new urea/thiourea derivatives I [R = 4-Cl, 3-Cl, 4-Br, 4-NO₂, 2,4-di-F; X = O; R = H, 4-F, 3-Cl, 3-Br, 3-CF₃; X = S] was synthesized by simple addition reaction of functionalized Ph isocyanates/isothiocyanates with N-(5-amino-2-methylphenyl)-4-(3-pyridyl)-2-pyrimidinamine (imatinib intermediate) in the presence of 1,4-di-Me piperazine (DMPZ) as a base and another series of new sulfonamide derivatives II [R¹ = 4-FC₆H₄, 4-O₂NC₆H₄, 3-F₃CC₆H₄, etc.] and carbamate derivatives III [R² = CH₂CH(CH₃)₂, CH₂CCl₃, 4-ClC₆H₄, etc.] were synthesized by reacting imatinib intermediate with various substituted aromatic sulfonyl chlorides and aromatic/aliphatic chloroformates in the presence of DMPZ as a base. Antimicrobial, antioxidant and in silico mol. docking studies were made against aromatase. In the experiment, the researchers used many compounds, for example, 3-(Trifluoromethyl)benzene-1-sulfonyl chloride (cas: 777-44-6HPLC of Formula: 777-44-6).

3-(Trifluoromethyl)benzene-1-sulfonyl chloride (cas: 777-44-6) belongs to organic chlorides. Organic chlorides can cause corrosion in pipelines, valves and condensers, and cause catalyst poisoning. The hydrocarbon processing industry (HPI) and others are affected by damage caused by these substances. Alkyl chlorides readily react with amines to give substituted amines. Alkyl chlorides are substituted by softer halides such as the iodide in the Finkelstein reaction.HPLC of Formula: 777-44-6

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Structure-Activity Relationships of the MEPicides: N-Acyl and O-Linked Analogs of FR900098 as Inhibitors of Dxr from Mycobacterium tuberculosis and Yersinia pestis was written by San Jose, Geraldine;Jackson, Emily R.;Haymond, Amanda;Johny, Chinchu;Edwards, Rachel L.;Wang, Xu;Brothers, R. Carl;Edelstein, Emma K.;Odom, Audrey R.;Boshoff, Helena I.;Couch, Robin D.;Dowd, Cynthia S.. And the article was included in ACS Infectious Diseases in 2016.Reference of 5335-05-7 This article mentions the following:

Despite continued research efforts, the threat of drug resistance from a variety of bacteria continues to plague clin. communities. Discovery and validation of novel biochem. targets will facilitate development of new drugs to combat these organisms. The methylerythritol phosphate (MEP) pathway to make isoprene units is a biosynthetic pathway essential to many bacteria. We and others have explored inhibitors of the MEP pathway as novel antibacterial agents. Mycobacterium tuberculosis, the causative agent of tuberculosis, and Yersinia pestis, resulting in the plague or “black death,” both rely on the MEP pathway for isoprene production 1-Deoxy-D-xylulose 5-phosphate reductoisomerase (Dxr) catalyzes the first committed step in the MEP pathway. We examined two series of Dxr inhibitors based on the parent structure of the retrohydroxamate natural product FR900098. The compounds contain either an extended N-acyl or O-linked alkyl/aryl group, and are designed to act as bisubstrate inhibitors of the enzyme. While nearly all of the compounds inhibited both Mtb and Yp Dxr to some extent, compounds generally displayed more potent inhibition against the Yp homolog, with the best analogs displaying nM IC₅₀ values. In bacterial growth inhibition assays, the phosphonic acids generally resulted in poor antibacterial activity, likely a reflection of inadequate permeability. Accordingly, di-Et and diPOM prodrug esters of these compounds were made. While the added lipophilicity did not enhance Yersinia activity, the compounds showed significantly improved antitubercular activities. The most potent compounds have Mtb MIC values of 3-12 μg/mL. Taken together, we have uncovered two series of analogs that potently inhibit Dxr homologs from Mtb and Yp. These inhibitors of the MEP pathway, termed MEPicides, serve as leads for future analog development. In the experiment, the researchers used many compounds, for example, Chloromethyl benzoate (cas: 5335-05-7Reference of 5335-05-7).

Chloromethyl benzoate (cas: 5335-05-7) belongs to organic chlorides. Organic chlorides are compounds containing a carbon-chlorine bond, which are widely used in the oil field as a wax dissolver. While alkyl bromides and iodides are more reactive, alkyl chlorides tend to be less expensive and more readily available. Alkyl chlorides readily undergo attack by nucleophiles.Reference of 5335-05-7

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics