Tag: 200-300

Brown, Thomas H.; Blakemore, Robert C.; Durant, Graham J.; Emmett, John C.; Ganellin, C. Robin; Parsons, Michael E.; Rawlings, D. Anthony; Walker, Terence F. published their research in European Journal of Medicinal Chemistry on February 29 ,1988. The article was titled 《Isocytosine H2-receptor histamine antagonists. I. Oxmetidine and related compounds》.Name: Ethyl 3-(4-chlorophenyl)propanoate The article contains the following contents:

2-[2-(5-Methyl-4-imidazolylmethylthio)ethylamino]-4-pyrimidones I (R = H, Me, PhO, substituted benzyl, etc.; R1 = H, Me, Pr, PhCH2) were prepared via substitution of (methylthio)pyrimidinones with 5-methyl-4-[(2-aminomethyl)thiomethyl]imidazole. The model compound I (R = R1 = H) has modest H2-antagonist activity as shown by its ability to antagonize histamine-stimulated tachycardia in guinea pig right atrium in vitro and inhibit histamine-stimulated gastric acid secretion in the lumen-perfused stomach of the anesthetized rat. Investigation of the effect of substituents in the pyrimidone ring showed that suitable substitution at the 5-position gave compounds with greatly increased activity, whereas substituents at other positions in the ring were not favorable for activity. Some structure-activity and structure-toxicity correlations are discussed. The experimental part of the paper was very detailed, including the reaction process of Ethyl 3-(4-chlorophenyl)propanoate(cas: 7116-36-1Name: Ethyl 3-(4-chlorophenyl)propanoate)

Ethyl 3-(4-chlorophenyl)propanoate(cas: 7116-36-1) belongs to organochlorine compounds. Alkanes and aryl alkanes may be chlorinated under free radical conditions, with UV light. Name: Ethyl 3-(4-chlorophenyl)propanoate 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

Related Products of 203302-92-5On November 26, 2009 ,《Synthesis, Structure-Activity Relationships, and Characterization of Novel Nonsteroidal and Selective Androgen Receptor Modulators》 appeared in Journal of Medicinal Chemistry. The author of the article were Schlienger, Nathalie; Lund, Birgitte W.; Pawlas, Jan; Badalassi, Fabrizio; Bertozzi, Fabio; Lewinsky, Rasmus; Fejzic, Alma; Thygesen, Mikkel B.; Tabatabaei, Ali; Bradley, Stefania Risso; Gardell, Luis R.; Piu, Fabrice; Olsson, Roger. The article conveys some information:

Herein we describe the discovery of ACP-105 (I), a novel and potent nonsteroidal selective androgen receptor modulator (SARM) with partial agonist activity relative to the natural androgen testosterone. Compound I was developed from a series of compounds found in a HTS screen using the receptor selection and amplification technol. (R-SAT). In vivo, I improved anabolic parameters in a 2-wk chronic study in castrated male rats. In addition to compound I, a number of potent antiandrogens were discovered from the same series of compounds whereof one compound, II, had antagonist activity at the AR T877A mutant involved in prostate cancer. The experimental part of the paper was very detailed, including the reaction process of 3-Bromo-2-chloro-6-fluorotoluene(cas: 203302-92-5Related Products of 203302-92-5)

3-Bromo-2-chloro-6-fluorotoluene(cas: 203302-92-5) belongs to organochlorine compounds. Alkanes and aryl alkanes may be chlorinated under free radical conditions, with UV light. Related Products of 203302-92-5 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

Murthy, Indraganti Sreenivasa; Sireesha, Reddymasu; Deepti, Kolli; Srinivasa Rao, P.; Ramesh Raju, R. published their research in Chemical Data Collections in 2021. The article was titled 《Design, synthesis and biological evaluation of sulphonamide derivatives of benzofuran-imidazopyridines as anticancer agents》.Electric Literature of C6H4Cl2O2S The article contains the following contents:

A novel library of sulfonamide derivatives of benzofuran-imidazopyridines I [R = 4-methoxyphenyl, 4-bromophenyl, 2,6-dimethylpyridine-4-yl, etc.] were designed, synthesized and screened for their anticancer activity against four human cancer cell lines such as breast cancer (MCF-7), lung cancer (A549), colon cancer (Colo-205) and ovarian cancer (A2780) by employing MTT assay. The results were expressed with IC50 μM, which indicated that all of the compounds I showed good to moderate activity on tested cell lines. Among them, compound I [R = 4-methoxyphenyl] showed potent anticancer activities against MCF-7, A549, Colo-205 and A2780 cell lines with IC50 values of 0.011 ± 0.0075μM, 0.073 ± 0.0012μM, 0.10 ± 0.19μM and 0.034 ± 0.0041μM resp. In the experimental materials used by the author, we found 4-Chlorobenzenesulfonyl chloride(cas: 98-60-2Electric Literature of 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. Electric Literature of 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

《Design, synthesis, and anticancer evaluation of novel benzopyran 1,3,4-oxadiazole derivatives》 was published in Indian Journal of Heterocyclic Chemistry in 2020. These research results belong to Kumar, Piyush; Rahman, Azizur Md.; Wal, Pranay; Rawat, Pinki; Singh, Kuldeep. SDS of cas: 622-95-7 The article mentions the following:

Some new benzopyran 1,3,4-oxadiazole, derivatives I (R = H, benzyl, 4-chlorobenzyl, 3,4-dichlorobenzyl; R1 = benzyl, 4-chlorobenzyl, 3,4-dichlorobenzyl, 3-chlorobenzyl) were designed by docking, in silico absorption, distribution, metabolism, excretion (ADME) and predicted toxicity studies, and then synthesized by S-alkylation of a benzopyran 1,3,4-oxadiazole derivative with different chloro-substituted benzyl bromides. The synthesized compounds were tested for anticancer activity on the MCF-7 cell line. Docking study showed all compounds to have better docking scores than the standard, Adriamycin. In silico, ADME and toxicity studies were also found as significant for most of the compounds The majority of the compounds displayed good to potent anticancer activity on the MCF-7 cell line. The experimental part of the paper was very detailed, including the reaction process of 1-(Bromomethyl)-4-chlorobenzene(cas: 622-95-7SDS of cas: 622-95-7)

1-(Bromomethyl)-4-chlorobenzene(cas: 622-95-7) is a useful reagent for the preparation of panicinotam derivatives for use as anti-inflammatory agents or immunomodulators.SDS of cas: 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, Synthesis, Acaricidal Activities, and Structure-Activity Relationship Studies of Novel Oxazolines Containing Sulfonate Moieties》 were Chen, Shilin; Zhang, Yu; Liu, Yuxiu; Wang, Qingmin. And the article was published in Journal of Agricultural and Food Chemistry in 2019. Category: chlorides-buliding-blocks The author mentioned the following in the article:

With the ultimate goal of addressing pest-related constraints on global agricultural production, combination principles were used to design and synthesize 2,4-diphenyl-1,3-oxazolines I (R = Me, Et, cyclohexyl, 2-FC6H4, 1-naphthyl, etc.) containing a sulfonate moiety at the para-position of the 4-Ph group. The target compounds, which have strong affinity for lipids and can be expected to traverse cell membranes, were characterized by 1H and 13C NMR spectroscopy and high-resolution mass spectrometry. Their activities against the larvae and eggs of carmine spider mites (Tetranychus cinnabarinus) were determined by a leaf-dipping method and compared with the activity of the com. acaricide etoxazole. Most of the test compounds displayed good ovicidal and larvicidal activities. In particular, the compound I (R = 4-t-BuC6H4) possessed better larvicidal activity (LC50 = 0.022 ± 0.009 mg/L) and ovicidal activity (0.044 ± 0.020 mg/L) than etoxazole (0.091 ± 0.051 and 0.095 ± 0.059 mg/L, resp.). Given its outstanding bioactivities, this compound deserves further attention as a pesticide candidate. After reading the article, we found that the author used 4-Chlorobenzenesulfonyl chloride(cas: 98-60-2Category: chlorides-buliding-blocks)

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.Category: chlorides-buliding-blocks 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

In 2022,Hong, Feng-Lin; Shi, Chong-Yang; Hong, Pan; Zhai, Tong-Yi; Zhu, Xin-Qi; Lu, Xin; Ye, Long-Wu published an article in Angewandte Chemie, International Edition. The title of the article was 《Copper-Catalyzed Asymmetric Diyne Cyclization via [1,2]-Stevens-Type Rearrangement for the Synthesis of Chiral Chromeno[3,4-c]pyrroles》.COA of Formula: C7H6BrCl The author mentioned the following in the article:

Here, authors report a copper-catalyzed asym. cascade cyclization/[1,2]-Stevens-type rearrangement via a non-diazo approach, leading to the practical and atom-economic assembly of various valuable chiral chromeno[3,4-c]pyrroles bearing a quaternary carbon stereocenter in generally moderate to good yields with wide substrate scope and excellent enantioselectivities (up to 99% ee). Importantly, this protocol not only represents the first example of catalytic asym. [1,2]-Stevens-type rearrangement based on alkynes but also constitutes the first asym. formal carbene insertion into the Si-O bond.1-(Bromomethyl)-4-chlorobenzene(cas: 622-95-7COA of Formula: C7H6BrCl) 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.COA of Formula: C7H6BrCl 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

Ali, Eslam M. H.; El-Telbany, Rania Farag A.; Abdel-Maksoud, Mohammed S.; Ammar, Usama M.; Mersal, Karim I.; Zaraei, Seyed-Omar; El-Gamal, Mohammed I.; Choi, Se-In; Lee, Kyung-Tae; Kim, Hee-Kwon; Lee, Kwan Hyi; Oh, Chang-Hyun published an article in 2021. The article was titled 《Design, synthesis, biological evaluation, and docking studies of novel (imidazol-5-yl)pyrimidine-based derivatives as dual BRAFV600E/p38α inhibitors》, and you may find the article in European Journal of Medicinal Chemistry.Computed Properties of C6H4Cl2O2S The information in the text is summarized as follows:

In the present work, a new series of (imidazol-5-yl)pyrimidine I ( Ar = C6H5, 4-ClC6H4, 4-BrC6H4 etc.; X = F, Cl; R = OCH3, OH) was designed and synthesized as dual inhibitors of BRAFV600E and p38α kinases which are considered as key regulators in mitogen-activated protein kinase signalling pathway. The target compounds were evaluated for dual kinase inhibitory activity. The tested compounds exhibited nanomolar scale IC50 values against BRAFV600E and low to sub-micromolar IC50 range against p38α. Compound I (Ar = 4-OHC6H4; X = F; R = OH) was identified as the most potent dual BRAFV600E/p38α inhibitor with IC50 values of 2.49 and 85 nM, resp. Further deep investigation revealed that Compound I (Ar = 4-OHC6H5; X = F; R = OH) possesses inhibitory activity of TNF-α production in lipopolysaccharide-induced RAW 264.7 macrophages with IC50 value of 96.3 nM. Addnl., the target compounds efficiently frustrated the proliferation of LOX-IMVI melanoma cell line. Compound I (Ar = 4-OHC6H5; X = F; R = OH) showed a satisfactory antiproliferative activity with IC50 value of 13μM, while, compound I (Ar = 3-FC6H4; X = F; R = OCH3) exhibited the highest cytotoxicity potency with IC50 value of 0.9μM. Compound I (Ar = 3-FC6H4; X = F; R = OCH3) is 11.11-fold more selective toward LOX-IMVI melanoma cells than IOSE-80PC normal cells. The results came from multiple reactions, including the reaction 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

Name: Ethyl 3-(4-chlorophenyl)propanoateOn September 30, 2011 ,《Synthesis, antibacterial activities and molecular docking studies of ethyl 3-(4-substituted phenyl) propanoates as targeted antibiotics》 was published in Latin American Journal of Pharmacy. The article was written by Ramaraj, Sivakumar; Vasanthakumari, Pradeepchandran R.; Narasimha, Jayaveera K.; Rajarathnam, Vijaianand; Palani, Kumamallasivan; Panneerselvam, Arulraj; Ramasamy, Venkatnarayanan. The article contains the following contents:

The type II fatty acid synthesis (FAS II) pathway has been recently reported as an attractive target for their efficacy against infections caused by multistrain-resistant Gram-pos. and Gram-neg. bacteria. Among the related FAS II enzymes, beta keto acyl-acyl carrier protein synthase [KAS 3-oxoacyl-[acyl carrier protein] synthase ], is an essential target for novel antibacterial drug design. Several 3-(phenyl)propanoic acid esters (I) were designed, the synthesis of the target compounds was achieved by a multistep process and the products were characterized. I were screened for their inhibitory activity against Escherichia coli β-keto acyl-acyl carrier protein synthase III (ecKAS III) was investigated by mol. docking simulation. I which posses both good inhibitory activity and binding affinity were compared their antibacterial activities against Gram-neg. and Gram-pos. bacterial strains, expecting to discover broad-spectrum antibacterial activity. I displayed significant activity and Et 3-(4-chlorophenyl)propanaoate exhibited the highest antibacterial activity against all tested bacteria. The results came from multiple reactions, including the reaction of Ethyl 3-(4-chlorophenyl)propanoate(cas: 7116-36-1Name: Ethyl 3-(4-chlorophenyl)propanoate)

Ethyl 3-(4-chlorophenyl)propanoate(cas: 7116-36-1) belongs to organochlorine compounds. Alkanes and aryl alkanes may be chlorinated under free radical conditions, with UV light. 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.Name: Ethyl 3-(4-chlorophenyl)propanoate

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

Neerathilingam, Nalladhambi; Bhargava Reddy, Mandapati; Anandhan, Ramasamy published their research in Journal of Organic Chemistry in 2021. The article was titled 《Regioselective Synthesis of 2° Amides Using Visible-Light-Induced Photoredox-Catalyzed Nonaqueous Oxidative C-N Cleavage of N,N-Dibenzylanilines》.Recommanded Product: 622-95-7 The article contains the following contents:

A visible-light-driven photoredox-catalyzed nonaqueous oxidative C-N cleavage of N,N-dibenzylanilines to 2° amides is reported. Further, this protocol is applied on 2-(dibenzylamino)benzamide to afford quinazolinones with (NH4)2S2O8 as an additive has been applied. Mechanistic studies imply that the reaction might underwent in situ generation of α-amino radical to imine by C-N bond cleavage followed by the addition of superoxide ion to form amides. In the experiment, the researchers used many compounds, for example, 1-(Bromomethyl)-4-chlorobenzene(cas: 622-95-7Recommanded Product: 622-95-7)

1-(Bromomethyl)-4-chlorobenzene(cas: 622-95-7) is a useful reagent for the preparation of panicinotam derivatives for use as anti-inflammatory agents or immunomodulators.Recommanded Product: 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 《Unprecedented Reactivity of β-Iodovinyl Sulfones: An Efficient Synthesis of β-Keto Sulfones and β-Keto Thiosulfones》 were Reddy, Raju Jannapu; Kumar, Jangam Jagadesh; Kumari, Arram Haritha. And the article was published in European Journal of Organic Chemistry in 2019. Reference of 4-Chlorobenzenesulfonyl chloride The author mentioned the following in the article:

An unprecedented reactivity of (E)-β-iodovinyl sulfones in the presence of NaOAc is reported. The (E)-β-iodovinyl sulfones were treated with NaOAc in DMSO/H2O to yield β-keto sulfones in moderate to high yields. A novel oxidative difunctionalization of β-iodovinyl sulfones with thiosulfonates and NaOAc in DMF has been developed. This metal-free oxosulfenylation is an operationally simple to access a wide range of β-keto thiosulfones (α-thioaryl-β-keto sulfones) in moderate to high yields. The transformations were reliable at gram-scale, thus illustrating its efficiency and practicality. A plausible mechanism for the protocol is also proposed. In the experiment, the researchers used 4-Chlorobenzenesulfonyl chloride(cas: 98-60-2Reference of 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.Reference of 4-Chlorobenzenesulfonyl chloride

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