Tag: 200-300

In 2022,Xie, Dandan; Hu, Xin; Ren, Xiaoli; Yang, Zaiping published an article in Frontiers in Chemistry (Lausanne, Switzerland). The title of the article was 《Synthesis and bioactivities of novel piperonylic acid derivatives containing a sulfonic acid ester moiety》.Formula: C6H4Cl2O2S The author mentioned the following in the article:

In order to develop efficient, broad-spectrum and structurally simple agricultural bactericide, the structure of piperonylic acid was modified and a series of novel piperonylic acid derivatives I [R = Ph, 2-naphthyl, benzyl, etc.] containing a sulfonic acid ester moiety was synthesized. Bioassay results indicated the compounds I exhibited significantly antibacterial activities. Among them, compound I [R = phenyl] exhibited excellent antibacterial activities against Pseudomonas syringae pv. Actinidiae (Psa), with inhibitory value 99 and 85% at 100μg/mL and 50μg/mL, resp., which was higher than that of thiodiazole-copper (84 and 77%) and bismerthiazol (96 and 78%). In addition, some compounds also showed moderate insecticidal activity against Spodoptera frugiperda. The above mentioned results confirm the broadening of the application of piperonylic acid, with reliable support for the development of novel agrochem. bactericide. The experimental process involved the reaction of 4-Chlorobenzenesulfonyl chloride(cas: 98-60-2Formula: C6H4Cl2O2S)

4-Chlorobenzenesulfonyl chloride(cas: 98-60-2) belongs to organochlorine compounds. Alkanes and aryl alkanes may be chlorinated under free radical conditions, with UV light. Formula: C6H4Cl2O2S However, the extent of chlorination is difficult to control. Aryl chlorides may be prepared by the Friedel-Crafts halogenation, using chlorine and a Lewis acid catalyst.

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

Rambo, Raoni S.; Waldow, Etienne C.; Abaddi, Bruno L.; Silveira, Maiele D.; Dadda, Adilio S.; Sperotto, Nathalia; Bizarro, Cristiano V.; Basso, Luiz Augusto; Machado, Pablo published their research in Journal of the Brazilian Chemical Society in 2021. The article was titled 《Design, synthesis and antitubercular activity of 2-(benzylthio)-1H-benzo[d]imidazoles》.Application of 622-95-7 The article contains the following contents:

Using mol. simplification and mol. hybridization approaches, a series of 2-(benzylthio)-1H-benzo[d]imidazoles I [R = H, MeO; R1 = H, F, 3,4-(Cl)2, etc.] was synthesized and evaluated as in-vitro inhibitors of Mycobacterium tuberculosis (M. tuberculosis) growth. Compounds I [R = H, MeO; R1 = 3,5-(NO)2] were considered the lead compounds from this series of mols., with minimal inhibitory concentration (MIC) values of 6.9 and 3.8μM against M. tuberculosis H37Rv, resp. Addnl., the leading compounds were active against multidrug-resistant strains and were devoid of apparent toxicity to Vero and HepG2 cells, from 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) and neutral red assays. Finally, the compounds I presented good aqueous solubility and high plasma stability. These data together indicated that this class of mols. may furnish new anti-tuberculosis drug candidates for future development. In addition to this study using 1-(Bromomethyl)-4-chlorobenzene, there are many other studies that have used 1-(Bromomethyl)-4-chlorobenzene(cas: 622-95-7Application of 622-95-7) was used in this study.

1-(Bromomethyl)-4-chlorobenzene(cas: 622-95-7) may be used to synthesize 1-(4-chlorobenzyl)-2-(pyrrolidin-1-yl-methyl)-1H-benzimidazole dihydrochloride.Application of 622-95-7 It can be synthesized by reacting 4-chlorobenzyl alcohol with bromodimethylsulfonium bromide (BDMS) It can also be synthesized by refluxing a mixture of 4-chlorobenzaldehyde, chlorotrimethylsilane, 1,1,3,3-tetramethyldisiloxane and lithium bromide.

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

Electric Literature of C11H13ClO2On October 13, 2006 ,《Biocatalytic racemization of (hetero)aryl-aliphatic α-hydroxycarboxylic acids by Lactobacillus spp. proceeds via an oxidation-reduction sequence》 was published in European Journal of Organic Chemistry. The article was written by Nestl, Bettina M.; Glueck, Silvia M.; Hall, Melanie; Kroutil, Wolfgang; Stuermer, Rainer; Hauer, Bernhard; Faber, Kurt. The article contains the following contents:

The biocatalytic racemization of a range of (hetero)aryl- and (di)aryl-aliphatic α-hydroxycarboxylic acids has been achieved by using whole resting cells of Lactobacillus spp. The essentially mild (physiol.) reaction conditions ensure the suppression of undesired side reactions, such as elimination, decomposition or condensation. Cofactor/inhibitor studies using a cell-free extract of Lactobacillus paracasei DSM 20207 reveal that the addition of redox cofactors (NAD+/NADI-I) leads to a distinct increase in the racemization rate, while strong inhibition is observed in the presence of Thio-NAD+, which suggests that the racemization proceeds by an oxidation-reduction sequence rather than involvement of a “”racemase”” enzyme. In the experimental materials used by the author, we found Ethyl 3-(4-chlorophenyl)propanoate(cas: 7116-36-1Electric Literature of C11H13ClO2)

Ethyl 3-(4-chlorophenyl)propanoate(cas: 7116-36-1) belongs to organochlorine compounds. Many organochlorine compounds have been isolated from natural sources ranging from bacteria to humans. Electric Literature of C11H13ClO2 Chlorinated organic compounds are found in nearly every class of biomolecules and natural products including alkaloids, terpenes, amino acids, flavonoids, steroids, and fatty acids.

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

Category: chlorides-buliding-blocksIn 2020 ,《Design, synthesis, and evaluation of new 2-(quinoline-4-yloxy)acetamide-based antituberculosis agents》 appeared in European Journal of Medicinal Chemistry. The author of the article were Borsoi, Ana Flavia; Paz, Josiane Delgado; Abbadi, Bruno Lopes; Macchi, Fernanda Souza; Sperotto, Nathalia; Pissinate, Kenia; Rambo, Raoni S.; Ramos, Alessandro Silva; Machado, Diana; Viveiros, Miguel; Bizarro, Cristiano Valim; Basso, Luiz Augusto; Machado, Pablo. The article conveys some information:

Using a classical mol. simplification approach, a series of 36 quinolines I [R1 = H, Me; R2 = Ph, 4-MeC6H4, 4-FC6H4, etc.] and II [R3 = Ph, Bn, 2-naphthyl, etc.] were synthesized and evaluated as in vitro inhibitors of Mycobacterium tuberculosis (M. tuberculosis) growth. Structure-activity relationship (SAR) studies leaded to potent antitubercular agents, with min. inhibitory concentration (MIC) values as low as 0.3μM against M. tuberculosis H37Rv reference strain. Furthermore, the lead compounds were active against multidrug-resistant strains, without cross-resistance with some first- and second-line drugs. Testing the mols. against a spontaneous mutant strain containing a single mutation in the qcrB gene (T313A) indicated that the synthesized quinolines targeted the cytochrome bc1 complex. In addition, leading compounds were devoid of apparent toxicity to HepG2 and Vero cells and showed moderate elimination rates in human liver S9 fractions. Finally, the selected structures inhibited M. tuberculosis growth in a macrophage model of tuberculosis infection. Taken together, these data indicated that this class of compounds may furnish candidates for the future development of antituberculosis drugs. In the part of experimental materials, we found many familiar compounds, such as 1-(Bromomethyl)-4-chlorobenzene(cas: 622-95-7Category: chlorides-buliding-blocks)

1-(Bromomethyl)-4-chlorobenzene(cas: 622-95-7) undergoes carbonylation in the presence of dimer of chloro(1,5-cyclooctadiene)rhodium(I) to yield the corresponding phenylacetic acid.Category: chlorides-buliding-blocks It can be synthesized by reacting 4-chlorobenzyl alcohol with bromodimethylsulfonium bromide (BDMS) It can also be synthesized by refluxing a mixture of 4-chlorobenzaldehyde, chlorotrimethylsilane, 1,1,3,3-tetramethyldisiloxane and lithium bromide.

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

Category: chlorides-buliding-blocksIn 2019 ,《Anticancer profile of newly synthesized BRAF inhibitors possess 5-(pyrimidin-4-yl)imidazo[2,1-b]thiazole scaffold》 appeared in Bioorganic & Medicinal Chemistry. The author of the article were Abdel-Maksoud, Mohammed S.; Ammar, Usama M.; Oh, Chang-Hyun. The article conveys some information:

In this work, a new series of imidazo[2,1-b]thiazole was designed and synthesized. The new compounds are having 3-fluorophenyl at position 6 of imidazo[2,1-b]thiazole and pyrimidine ring at position 5. The pyrimidine ring containing either amide or sulfonamide moiety attached to a linker (Et or propyl) at position 2 of the pyrimidine ring. The final compounds were selected by NCI for in vitro cytotoxicity screening. Most derivatives showed cytotoxic activity against colon cancer and melanoma cell lines. In addition, IC50s of the target compounds were determined over A375 and SK-MEL-28 cell lines using sorafenib as pos. control. Compounds12b, 12c, 12e, 12f, 15a, 15d, 15f, 14g and 15h exhibited superior activity when compared to sorafenib. The most potent compounds were tested against wild type BRAF, v600e BRAF, and CRAF. Compound 15h exhibited a potential inhibitory effect againstV600EBRAF (IC50 = 9.3 nM). In the experimental materials used by the author, we found 4-Chlorobenzenesulfonyl chloride(cas: 98-60-2Category: chlorides-buliding-blocks)

4-Chlorobenzenesulfonyl chloride(cas: 98-60-2) belongs to organochlorine compounds. Many organochlorine compounds have been isolated from natural sources ranging from bacteria to humans. Chlorinated organic compounds are found in nearly every class of biomolecules and natural products including alkaloids, terpenes, amino acids, flavonoids, steroids, and fatty acids. Category: chlorides-buliding-blocks

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

Computed Properties of C6H4Cl2O2SIn 2022 ,《Synthesis and bioactivity of novel sulfonate scaffold-containing pyrazolecarbamide derivatives as antifungal and antiviral agents》 appeared in Frontiers in Chemistry (Lausanne, Switzerland). The author of the article were Lei, Zhi-Wei; Yao, Jianmei; Liu, Huifang; Ma, Chiyu; Yang, Wen. The article conveys some information:

Novel I [R = Ph, 4-methylphenyl, 2-chlorophenyl, etc] bearing a sulfonate fragment were synthesized to identify potential antifungal and antiviral agents. All the structures of the key intermediates and target compounds were confirmed by NMR and high-resolution mass spectrometry. The single-crystal X-ray diffraction of the compound I [R = 3-trifluoromethyl phenyl] showed that pyrazole carbamide is a sulfonate. The in vitro antifungal activities of the target compounds against Colletotrichum camelliae, Pestalotiopsis theae, Gibberella zeae, and Rhizoctonia solani were evaluated at 50μg/mL. Among the four pathogens, the target compounds exhibited the highest antifungal activity against Rhizoctonia solani. The compound I [R = phenylethyl] (EC50 = 0.45 mg/L) had higher antifungal activity than the com. fungicide hymexazol (EC50 = 10.49 mg/L) against R. solani, almost similar to bixafen (EC50 = 0.25 mg/L). Addnl., the target compounds exhibited protective effects in vivo against TMV. Thus, this study reveals that I. bearing a sulfonate fragment exhibited potential antifungal and antiviral activities. The experimental part of the paper was very detailed, including the reaction process of 4-Chlorobenzenesulfonyl chloride(cas: 98-60-2Computed Properties of C6H4Cl2O2S)

4-Chlorobenzenesulfonyl chloride(cas: 98-60-2) belongs to organochlorine compounds. The wide structural variety and divergent chemical properties of organochlorides lead to a broad range of names, applications, and properties.Computed Properties of C6H4Cl2O2S Organochlorine compounds have wide use in many applications, though some are of profound environmental concern, with TCDD being one of the most notorious.

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

Nasrollahzadeh, Mahmoud; Nezafat, Zahra; Pakzad, Khatereh; Ahmadpoor, Fatemeh published an article in 2021. The article was titled 《Synthesis of magnetic chitosan supported metformin-Cu(II) complex as a recyclable catalyst for N-arylation of primary sulfonamides》, and you may find the article in Journal of Organometallic Chemistry.Recommanded Product: 4-Chlorobenzenesulfonyl chloride The information in the text is summarized as follows:

Immobilization of a copper complex on the magnetic chitosan bearing metformin ligand was developed through immobilizing structurally defined metformin with long tail of (3-chloropropyl)trimethoxysilane (TMOS). The synthesized Fe3O4-chitosan@metformin-Cu(II) complex (Fe3O4-CS@Met-Cu(II)) were used as an effective, reusable and magnetic catalyst in the N-arylation of different derivatives of primary sulfonamides with arylboronic acids in ethanol. The primary sulfonamides were prepared from the reaction of sulfonyl chlorides with sodium cyanate in water under ultrasonic irradiation Utilizing a wide variety of substrates in EtOH as a green solvent, high yields of the primary and secondary sulfonamides, easy work-up along with the excellent recovery and reusability of the catalyst, make this process a simple, economic and environmentally benign method. The synthesized Fe3O4-CS@Met-Cu(II) were characterized using various techniques such as XRD (X-ray diffraction), EDS (energy-dispersive X-ray spectroscopy), elemental mapping, TEM (transmission electron microscopy), FESEM (field emission SEM), VSM (vibrating sample magnetometer), ICP-MS (inductively coupled plasma mass spectroscopy), TGA (thermogravimetric anal.) and FT-IR (Fourier-transform IR spectroscopy) analyses. The catalyst was recycled and reused 5 times with no considerable loss of catalytic activity. The experimental process involved the reaction of 4-Chlorobenzenesulfonyl chloride(cas: 98-60-2Recommanded Product: 4-Chlorobenzenesulfonyl chloride)

4-Chlorobenzenesulfonyl chloride(cas: 98-60-2) belongs to organochlorine compounds. Alkanes and aryl alkanes may be chlorinated under free radical conditions, with UV light. However, the extent of chlorination is difficult to control. Aryl chlorides may be prepared by the Friedel-Crafts halogenation, using chlorine and a Lewis acid catalyst.Recommanded Product: 4-Chlorobenzenesulfonyl chloride

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

Samanta, Partha Kumar; Biswas, Rima; Bhaduri, Samanka Narayan; Ray, Shounak; Biswas, Papu published their research in Microporous and Mesoporous Materials in 2021. The article was titled 《Copper(0) nanoparticles immobilized on SBA-15: a versatile recyclable heterogeneous catalyst for solvent and ligand free C-S coupling reaction from diverse substrates》.HPLC of Formula: 622-95-7 The article contains the following contents:

A SBA-15 supported copper(0) nanoparticles based catalyst (Cu(0)MS) has been prepared using wet impregnation method. The catalyst was thoroughly characterized by several techniques including powder X-ray diffraction, nitrogen adsorption-desorption, field emission SEM-energy dispersive X-ray, transmission electron microscopy, high angle annular dark field scanning transmission electron microscopy and inductively coupled plasma-optical emission spectrometry. This mesoporous silica supported copper(0) nanoparticles had been exploited as a catalyst for ligand-free and solvent-free C-S cross-coupling reactions. Sym./unsym. aryl/alkyl sulfides R1SR2 (R1 = Ph, 2-MeOC6H4, PhCH2, PhCH:CH, 2-thienyl, etc.; R2 = Ph, n-octyl, PhCH2CH2, 2-pyridyl, etc.) had been synthesized by the S-arylation of aromatic, heteroaromatic and aliphatic thiols R2SH with aryl, heteroaryl or vinyl halides R1X (X = I, Br). Aryl chlorides also responded the reaction very well to produce aryl sulfides. The applicability of the current protocol had also been explored for the synthesis of the starting materials of different C-S bond containing pharmaceuticals. In addition, the present catalytic system was also suitable for the synthesis of a variety of sym. diaryl sulfides from aryl halides using thiourea as a sulfur source. Furthermore, it was also found that the Cu(0)MS catalyst could be reused five times without substantial loss in activity. In the experiment, the researchers used many compounds, for example, 1-(Bromomethyl)-4-chlorobenzene(cas: 622-95-7HPLC of Formula: 622-95-7)

1-(Bromomethyl)-4-chlorobenzene(cas: 622-95-7) may be used to synthesize 1-(4-chlorobenzyl)-2-(pyrrolidin-1-yl-methyl)-1H-benzimidazole dihydrochloride.HPLC of Formula: 622-95-7 It can be synthesized by reacting 4-chlorobenzyl alcohol with bromodimethylsulfonium bromide (BDMS) It can also be synthesized by refluxing a mixture of 4-chlorobenzaldehyde, chlorotrimethylsilane, 1,1,3,3-tetramethyldisiloxane and lithium bromide.

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

The author of 《Design and synthesis of pyridin-2-ylmethylaminopiperidin-1-ylbutyl amide CCR5 antagonists that are potent inhibitors of M-tropic (R5) HIV-1 replication》 were Skerlj, Renato; Bridger, Gary; Zhou, Yuanxi; Bourque, Elyse; McEachern, Ernest; Langille, Jonathan; Harwig, Curtis; Veale, Duane; Yang, Wen; Li, Tongshong; Zhu, Yongbao; Bey, Michael; Baird, Ian; Sartori, Michael; Metz, Markus; Mosi, Renee; Nelson, Kim; Bodart, Veronique; Wong, Rebecca; Fricker, Simon; MacFarland, Ron; Huskens, Dana; Schols, Dominique. And the article was published in Bioorganic & Medicinal Chemistry Letters in 2011. Reference of Ethyl 6-chloro-2,4-dimethylnicotinate The author mentioned the following in the article:

A series of CCR5 antagonists, e.g. I, were optimized for potent inhibition of R5 HIV-1 replication in peripheral blood mononuclear cells. Compounds that met acceptable ADME criteria, selectivity, human plasma protein binding, potency shift in the presence of α-glycoprotein were evaluated in rat and dog pharmacokinetics. In the experimental materials used by the author, we found Ethyl 6-chloro-2,4-dimethylnicotinate(cas: 54453-94-0Reference of Ethyl 6-chloro-2,4-dimethylnicotinate)

Ethyl 6-chloro-2,4-dimethylnicotinate(cas: 54453-94-0) 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.Reference of Ethyl 6-chloro-2,4-dimethylnicotinate

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

In 1976,European Journal of Medicinal Chemistry included an article by Flammang, Michel; Wermuth, Camille G.. Quality Control of Ethyl 3-(4-chlorophenyl)propanoate. The article was titled 《2,3-Benzodiazepine systems. II. 4-Oxo-3,5-dihydro(4H)-2,3-benzodiazepines. Synthesis and pharmacological study》. The information in the text is summarized as follows:

Benzodiazepinones I (R = H, Cl; R1 = H, Me; R2 = H, Me, morpholinoethyl, morpholinopropyl, pyrrolidinoethyl; R3 = H, OMe, Cl) (11 compounds) were prepared by treating 4-RC6H4CHO with CH2(CO2H)2, cyclizing 4-RC6H4CH:CHCO2H, treating II (X = O) with 4-R3C6H4MgBr, dehydrating II (X = OH,C6H4R3-4), oxidizing the indenes, and condensing 4,2-R(4-R3C6H4CO)C6H3CH2CO2H with R2NHNH2. I had much lower tranquilizing activity than diazepam. In the experimental materials used by the author, we found Ethyl 3-(4-chlorophenyl)propanoate(cas: 7116-36-1Quality Control of Ethyl 3-(4-chlorophenyl)propanoate)

Ethyl 3-(4-chlorophenyl)propanoate(cas: 7116-36-1) belongs to organochlorine compounds. The wide structural variety and divergent chemical properties of organochlorides lead to a broad range of names, applications, and properties. Organochlorine compounds have wide use in many applications, though some are of profound environmental concern, with TCDD being one of the most notorious.Quality Control of Ethyl 3-(4-chlorophenyl)propanoate

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