Sasaki, Shigeru’s team published research in Bulletin of the Chemical Society of Japan in 88 | CAS: 5860-95-7

Bulletin of the Chemical Society of Japan published new progress about 5860-95-7. 5860-95-7 belongs to chlorides-buliding-blocks, auxiliary class Trifluoromethyl,Fluoride,Chloride,Benzene,Ketone, name is 1-(2-Chlorophenyl)-2,2,2-trifluoroethanone, and the molecular formula is C8H4ClF3O, Application of 1-(2-Chlorophenyl)-2,2,2-trifluoroethanone.

Sasaki, Shigeru published the artcileBisoxazoline-catalyzed asymmetric nucleophilic addition of diethyl zinc to fluorinated alkyl ketones: enantiofacial control by changing the bisoxazoline substituent, Application of 1-(2-Chlorophenyl)-2,2,2-trifluoroethanone, the publication is Bulletin of the Chemical Society of Japan (2015), 88(1), 200-208/1-200-208/9, 9 pp., database is CAplus.

Bisoxazoline (BOX)-catalyzed asym. nucleophilic addition of di-Et zinc to fluorinated alkyl ketones successfully afforded enantioenriched fluorinated alkyl tertiary alcs. The effect of the size of the substituent on the oxazoline ring on the stereoselectivity of the reaction was investigated. Furthermore, the enantioselectivity could be reversed by altering the BOX bridge structure while retaining the C-4 substituent on the oxazoline ring.

Bulletin of the Chemical Society of Japan published new progress about 5860-95-7. 5860-95-7 belongs to chlorides-buliding-blocks, auxiliary class Trifluoromethyl,Fluoride,Chloride,Benzene,Ketone, name is 1-(2-Chlorophenyl)-2,2,2-trifluoroethanone, and the molecular formula is C8H4ClF3O, Application of 1-(2-Chlorophenyl)-2,2,2-trifluoroethanone.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Matheny, Jonathon P.’s team published research in RSC Advances in 10 | CAS: 21286-54-4

RSC Advances published new progress about 21286-54-4. 21286-54-4 belongs to chlorides-buliding-blocks, auxiliary class Chiral,Chloride,Sulfonyl chlorides,Aliphatic cyclic hydrocarbon,Ketone, name is ((1S,4R)-7,7-Dimethyl-2-oxobicyclo[2.2.1]heptan-1-yl)methanesulfonyl chloride, and the molecular formula is C10H15ClO3S, SDS of cas: 21286-54-4.

Matheny, Jonathon P. published the artcileFacile assembly of 1,5-diazocan-2-ones via cyclization of tethered sulfonamides to cyclopropenes, SDS of cas: 21286-54-4, the publication is RSC Advances (2020), 10(72), 44183-44190, database is CAplus and MEDLINE.

The sulfonamide moiety was evaluated as an activating and stabilizing functional group in the metal-templated strain release-driven intramol. nucleophilic addition of amines to cyclopropenes to generate 1,5-diazocan-2-ones I [R = Me, 4-BrC6H4, 2-naphthyl, etc.].

RSC Advances published new progress about 21286-54-4. 21286-54-4 belongs to chlorides-buliding-blocks, auxiliary class Chiral,Chloride,Sulfonyl chlorides,Aliphatic cyclic hydrocarbon,Ketone, name is ((1S,4R)-7,7-Dimethyl-2-oxobicyclo[2.2.1]heptan-1-yl)methanesulfonyl chloride, and the molecular formula is C10H15ClO3S, SDS of cas: 21286-54-4.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Sameshima, Tomoya’s team published research in Biochemistry in 57 | CAS: 350-30-1

Biochemistry published new progress about 350-30-1. 350-30-1 belongs to chlorides-buliding-blocks, auxiliary class Fluoride,Chloride,Nitro Compound,Benzene, name is 3-Chloro-4-fluoronitrobenzene, and the molecular formula is C6H3ClFNO2, Recommanded Product: 3-Chloro-4-fluoronitrobenzene.

Sameshima, Tomoya published the artcileDiscovery of an Irreversible and Cell-Active BCL6 Inhibitor Selectively Targeting Cys53 Located at the Protein-Protein Interaction Interface, Recommanded Product: 3-Chloro-4-fluoronitrobenzene, the publication is Biochemistry (2018), 57(8), 1369-1379, database is CAplus and MEDLINE.

B-cell lymphoma 6 (BCL6) is the most frequently involved oncogene in diffuse large B-cell lymphomas (DLBCLs). BCL6 shows potent transcriptional repressor activity through interactions with its corepressors, such as BCL6 corepressor (BCOR). The inhibition of the protein-protein interaction (PPI) between BCL6 and its corepressors suppresses the growth of BCL6-dependent DLBCLs, thus making BCL6 an attractive drug target for lymphoma treatments. However, potent small-mol. PPI inhibitor identification remains challenging because of the lack of deep cavities at PPI interfaces. This paper reports the discovery of a potent, cell-active, small-mol. BCL6 inhibitor, BCL6-i (8), that operates through irreversible inhibition. First, we synthesized an irreversible lead compound 4, which targets Cys53 in a cavity on the BCL6 BTB domain dimer by introducing an irreversible warhead to a high-throughput screening hit compound 1. Further chem. optimization of 4 based on kinact/KI evaluation produced BCL6-i with a kinact/KI value of 1.9 × 104 M-1s-1, corresponding to a 670-fold improvement in potency compared to 4. By exploiting the property of irreversible inhibition, engagement of BCL6-i to intracellular BCL6 was confirmed. BCL6-i showed intracellular PPI inhibitory activity between BCL6 and its corepressors, thus resulting in BCL6-dependent DLBCL cell-growth inhibition. BCL6-i is a cell-active chem. probe with the most potent BCL6 inhibitory activity reported to date. The discovery process of BCL6-i illustrates the utility of irreversible inhibition for identifying potent chem. probes for intractable target proteins.

Biochemistry published new progress about 350-30-1. 350-30-1 belongs to chlorides-buliding-blocks, auxiliary class Fluoride,Chloride,Nitro Compound,Benzene, name is 3-Chloro-4-fluoronitrobenzene, and the molecular formula is C6H3ClFNO2, Recommanded Product: 3-Chloro-4-fluoronitrobenzene.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Usui, Kazuteru’s team published research in Journal of Organic Chemistry in 80 | CAS: 21286-54-4

Journal of Organic Chemistry published new progress about 21286-54-4. 21286-54-4 belongs to chlorides-buliding-blocks, auxiliary class Chiral,Chloride,Sulfonyl chlorides,Aliphatic cyclic hydrocarbon,Ketone, name is ((1S,4R)-7,7-Dimethyl-2-oxobicyclo[2.2.1]heptan-1-yl)methanesulfonyl chloride, and the molecular formula is C14H21BO3S, Related Products of chlorides-buliding-blocks.

Usui, Kazuteru published the artcileSynthesis and Resolution of Substituted [5]Carbohelicenes, Related Products of chlorides-buliding-blocks, the publication is Journal of Organic Chemistry (2015), 80(12), 6502-6508, database is CAplus and MEDLINE.

Three types of racemic [5]helicenyl acetates [I (R = Ac), II, and III (R = Ac)] were synthesized. The synthesis of II was achieved by regioselective oxidation using o-iodoxybenzoic acid. The enzymic kinetic resolution of IIII (R = Ac) was studied. The conversion with the highest rate and ee was obtained using I (R = Ac) as the substrate and lipase Amano PS-IM as the enzyme. The two enantiomers of 1-[5]helicenol III (R = H) were separated using (1S)-10-camphorsulfonyl chloride as the chiral resolving agent.

Journal of Organic Chemistry published new progress about 21286-54-4. 21286-54-4 belongs to chlorides-buliding-blocks, auxiliary class Chiral,Chloride,Sulfonyl chlorides,Aliphatic cyclic hydrocarbon,Ketone, name is ((1S,4R)-7,7-Dimethyl-2-oxobicyclo[2.2.1]heptan-1-yl)methanesulfonyl chloride, and the molecular formula is C14H21BO3S, Related Products of chlorides-buliding-blocks.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Kanno, Hideo’s team published research in Chemical & Pharmaceutical Bulletin in 40 | CAS: 116850-28-3

Chemical & Pharmaceutical Bulletin published new progress about 116850-28-3. 116850-28-3 belongs to chlorides-buliding-blocks, auxiliary class Fluoride,Chloride,Benzene, name is 2-Chloro-1-fluoro-3-methylbenzene, and the molecular formula is C7H6ClF, Quality Control of 116850-28-3.

Kanno, Hideo published the artcileSynthesis and antihypertensive activity of 1,4-dihydropyridine derivatives with a 4-(disubstituted phenyl) ring and an aminoalkyl ester group: highly potent and long-lasting calcium antagonists, Quality Control of 116850-28-3, the publication is Chemical & Pharmaceutical Bulletin (1992), 40(8), 2049-54, database is CAplus and MEDLINE.

New 1,4-dihydropyridine derivatives I (R = Cl, F, NO2; R1, R2 = H, Cl, F, NO2; X = CH2, CMe2CH2), bearing a 4-(disubstituted phenyl) ring and an aminoethyl ester or an amino-2,2-dimethylpropyl ester, were synthesized and their antihypertensive activities were examined in normotensive rats and spontaneously hypertensive rats. The effects of Ph substituents and ester groups on the antihypertensive activity are discussed. Several compounds showed a more potent antihypertensive activity than nicardipine and most compounds had a longer duration of action. Among them, I (R = F, R1 = H, R2 = NO2, X = CMe2CH2).HCl showed highly potent and long-lasting activity and was selected as a candidate for further pharmacol. investigations.

Chemical & Pharmaceutical Bulletin published new progress about 116850-28-3. 116850-28-3 belongs to chlorides-buliding-blocks, auxiliary class Fluoride,Chloride,Benzene, name is 2-Chloro-1-fluoro-3-methylbenzene, and the molecular formula is C7H6ClF, Quality Control of 116850-28-3.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Sone, Toshihiko’s team published research in Journal of the American Chemical Society in 130 | CAS: 5034-06-0

Journal of the American Chemical Society published new progress about 5034-06-0. 5034-06-0 belongs to chlorides-buliding-blocks, auxiliary class Salt,Aliphatic hydrocarbon chain, name is trimethyloxosulphonium chloride, and the molecular formula is C19H14O2, Formula: C3H9ClOS.

Sone, Toshihiko published the artcileCatalytic Asymmetric Synthesis of 2,2-Disubstituted Terminal Epoxides via Dimethyloxosulfonium Methylide Addition to Ketones, Formula: C3H9ClOS, the publication is Journal of the American Chemical Society (2008), 130(31), 10078-10079, database is CAplus and MEDLINE.

Catalytic asym. Corey-Chaykovsky epoxidation of ketones with dimethyloxosulfonium methylide using an La-Li3-tris(binaphthoxide) + Ar3P:O (Ar = 2,4,6-trimethoxyphenyl) complex proceeded smoothly at room temperature, and 2,2-disubstituted terminal epoxides were obtained with high enantioselectivity (91-97%) and yield (>88-99%) from a broad range of Me ketones with 1-5 mol% catalyst loading. The use of achiral additive Ar3P:O was important to achieve high enantioselectivity.

Journal of the American Chemical Society published new progress about 5034-06-0. 5034-06-0 belongs to chlorides-buliding-blocks, auxiliary class Salt,Aliphatic hydrocarbon chain, name is trimethyloxosulphonium chloride, and the molecular formula is C19H14O2, Formula: C3H9ClOS.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Sone, Toshihiko’s team published research in Molecules in 17 | CAS: 5034-06-0

Molecules published new progress about 5034-06-0. 5034-06-0 belongs to chlorides-buliding-blocks, auxiliary class Salt,Aliphatic hydrocarbon chain, name is trimethyloxosulphonium chloride, and the molecular formula is C6H8N2, Recommanded Product: trimethyloxosulphonium chloride.

Sone, Toshihiko published the artcileEnantioselective synthesis of 2,2-disubstituted terminal epoxides via catalytic asymmetric Corey-Chaykovsky epoxidation of ketones, Recommanded Product: trimethyloxosulphonium chloride, the publication is Molecules (2012), 1617-1634, database is CAplus and MEDLINE.

Catalytic asym. Corey-Chaykovsky epoxidation of various ketones RCOR1 (R = Ph, 1-naphthyl, n-octyl, etc., R1 = Me; R = Ph, 4-ClC6H4, 3-pyridyl, etc., R1 = ET, n-Pr, CHMe2) with dimethyloxosulfonium methylide using a heterobimetallic La-Li3-BINOL complex (LLB) is described. The reaction proceeded smoothly at room temperature in the presence of achiral phosphine oxide additives, and 2,2-disubstituted terminal epoxides I were obtained in high enantioselectivity (97%-91% ee) and yield (>99%-88%) from a broad range of Me ketones with 1-5 mol% catalyst loading. Enantioselectivity was strongly dependent on the steric hindrance, and other ketones, such as Et ketones and Pr ketones resulted in slightly lower enantioselectivity (88%-67% ee).

Molecules published new progress about 5034-06-0. 5034-06-0 belongs to chlorides-buliding-blocks, auxiliary class Salt,Aliphatic hydrocarbon chain, name is trimethyloxosulphonium chloride, and the molecular formula is C6H8N2, Recommanded Product: trimethyloxosulphonium chloride.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Palii, G. K.’s team published research in Genetika (Moscow) in 10 | CAS: 38146-42-8

Genetika (Moscow) published new progress about 38146-42-8. 38146-42-8 belongs to chlorides-buliding-blocks, auxiliary class Achiral Phase-Transfer Catalysts, name is N1,N10-Bis(2-((2-isopropyl-5-methylcyclohexyl)oxy)-2-oxoethyl)-N1,N1,N10,N10-tetramethyldecane-1,10-diaminium chloride, and the molecular formula is C38H74Cl2N2O4, Formula: C38H74Cl2N2O4.

Palii, G. K. published the artcileCytogenetic effect of etonium, decamethoxin, and a hexamethylenediamine derivative, Formula: C38H74Cl2N2O4, the publication is Genetika (Moscow) (1974), 10(1), 171-2, database is CAplus.

When added to a human embryonic fibroblast culture, etonium [21954-74-5], decamethoxin (I) [38146-42-8], or a hexamethylenediamine derivative decreased the mitotic activity and induced chromosome aberrations in the cells. Etonium had the strongest mutagenic effect.

Genetika (Moscow) published new progress about 38146-42-8. 38146-42-8 belongs to chlorides-buliding-blocks, auxiliary class Achiral Phase-Transfer Catalysts, name is N1,N10-Bis(2-((2-isopropyl-5-methylcyclohexyl)oxy)-2-oxoethyl)-N1,N1,N10,N10-tetramethyldecane-1,10-diaminium chloride, and the molecular formula is C38H74Cl2N2O4, Formula: C38H74Cl2N2O4.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Narjes, Frank’s team published research in Journal of Medicinal Chemistry in 61 | CAS: 915763-60-9

Journal of Medicinal Chemistry published new progress about 915763-60-9. 915763-60-9 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Nitrile,Boronic acid and ester,Benzene,Boronic Acids,Boronic acid and ester, name is (3-Chloro-5-cyanophenyl)boronic acid, and the molecular formula is C7H5BClNO2, COA of Formula: C7H5BClNO2.

Narjes, Frank published the artcilePotent and Orally Bioavailable Inverse Agonists of RORγt Resulting from Structure-Based Design, COA of Formula: C7H5BClNO2, the publication is Journal of Medicinal Chemistry (2018), 61(17), 7796-7813, database is CAplus and MEDLINE.

Retinoic acid receptor related orphan receptor γt (RORγt), has been identified as the master regulator of TH17-cell function and development, making it an attractive target for the treatment of autoimmune diseases by a small-mol. approach. Herein, we describe our investigations on a series of 4-aryl-thienyl acetamides, which were guided by insights from X-ray cocrystal structures. Efforts in targeting the cofactor-recruitment site from the 4-aryl group on the thiophene led to a series of potent binders with nanomolar activity in a primary human-TH17-cell assay. The observation of a DMSO mol. binding in a subpocket outside the LBD inspired the introduction of an acetamide into the benzylic position of these compounds Hereby, a hydrogen-bond interaction of the introduced acetamide oxygen with the backbone amide of Glu379 was established. This greatly enhanced the cellular activity of previously weakly cell-active compounds The best compounds combined potent inhibition of IL-17 release with favorable PK in rodents, with compound 32 representing a promising starting point for future investigations.

Journal of Medicinal Chemistry published new progress about 915763-60-9. 915763-60-9 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Nitrile,Boronic acid and ester,Benzene,Boronic Acids,Boronic acid and ester, name is (3-Chloro-5-cyanophenyl)boronic acid, and the molecular formula is C7H5BClNO2, COA of Formula: C7H5BClNO2.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Kong, Deyu’s team published research in Journal of Medicinal Chemistry in 62 | CAS: 939-99-1

Journal of Medicinal Chemistry published new progress about 939-99-1. 939-99-1 belongs to chlorides-buliding-blocks, auxiliary class Fluoride,Chloride,Benzyl chloride,Benzene, name is 1-(Chloromethyl)-4-(trifluoromethyl)benzene, and the molecular formula is C8H6ClF3, Synthetic Route of 939-99-1.

Kong, Deyu published the artcileOptimization of P2Y12 Antagonist Ethyl 6-(4-((Benzylsulfonyl)carbamoyl)piperidin-1-yl)-5-cyano-2-methylnicotinate (AZD1283) Led to the Discovery of an Oral Antiplatelet Agent with Improved Druglike Properties, Synthetic Route of 939-99-1, the publication is Journal of Medicinal Chemistry (2019), 62(6), 3088-3106, database is CAplus and MEDLINE.

P2Y12 antagonists are widely used as antiplatelet agents for the prevention and treatment of arterial thrombosis. Based on the scaffold of a known P2Y12 antagonist AZD1283 (I), a series of novel bicyclic pyridine derivatives were designed and synthesized. The cyclization of the ester substituent on the pyridine ring to the ortho-Me group led to lactone analogs of AZD1283 that showed significantly enhanced metabolic stability in subsequent structure-pharmacokinetic relationship studies. The metabolic stability was further enhanced by adding a 4-Me substituent to the piperidinyl moiety. Compound II displayed potent inhibition of platelet aggregation in vitro as well as antithrombotic efficacy in a rat ferric chloride model. Moreover, II showed a safety profile that was superior to what was observed for clopidogrel in a rat tail-bleeding model. These results support the further evaluation of compound II as a promising drug candidate.

Journal of Medicinal Chemistry published new progress about 939-99-1. 939-99-1 belongs to chlorides-buliding-blocks, auxiliary class Fluoride,Chloride,Benzyl chloride,Benzene, name is 1-(Chloromethyl)-4-(trifluoromethyl)benzene, and the molecular formula is C8H6ClF3, Synthetic Route of 939-99-1.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics