Category: chlorides-buliding-blocks

Xu, Shengtao published the artcileA Novel Potent Anticancer Compound Optimized from a Natural Oridonin Scaffold Induces Apoptosis and Cell Cycle Arrest through the Mitochondrial Pathway, Application In Synthesis of 6313-54-8, the publication is Journal of Medicinal Chemistry (2017), 60(4), 1449-1468, database is CAplus and MEDLINE.

The cytotoxicity of the natural ent-kaurene diterpenoid, oridonin, has been extensively studied. However, the application of oridonin for cancer therapy was hampered primarily by its moderate potency. In this study, a series of oridonin A-ring modified analogs, and their derivatives bearing various substituents on 14-OH position, were designed, synthesized and evaluated for anticancer efficacy. Some of the derivatives were significantly more potent than oridonin against both drug-sensitive and drug-resistant cancer cells. The most potent compound, I, was 200-fold more efficacious than oridonin in MCF-7 cancer cells. Furthermore, I induced apoptosis and cell cycle arrest at the G2/M phase. A decrease in mitochondrial membrane potential and increased Bax/Bcl-2 ratio, accompanied by activated caspase-3 cleavage, were observed in MCF-7 cells after treatment with I, suggesting that the mitochondrial pathway was involved in the I-mediated apoptosis. Moreover, I significantly inhibited tumor growth in mouse xenograft models and had no observable toxic effect.

Journal of Medicinal Chemistry published new progress about 6313-54-8. 6313-54-8 belongs to chlorides-buliding-blocks, auxiliary class Pyridine,Chloride,Carboxylic acid, name is 2-Chloroisonicotinic acid, and the molecular formula is C5H7FO2, Application In Synthesis of 6313-54-8.

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

Wang, Qi published the artcilePalladium-catalyzed aminocarbonylative cyclization of benzyl chlorides with 2-nitroaryl alkynes to construct indole derivatives, Application of 3-Chlorobenzylchloride, the publication is Molecular Catalysis (2022), 112302, database is CAplus.

A palladium-catalyzed aminocarbonylative cyclization of benzyl chlorides RCH₂Cl (R = Ph, 3,5-dichlorophenyl, naphthalen-1-yl, etc.) with 2-nitroaryl alkynes 2-NO₂-4-R¹-5-R²C₆H₂CCR³ (R¹ = H, Me, F; R² = H, Cl; R³ = Ph, n-Bu, cyclopropyl, etc.) has been developed for the rapid construction of indole skeletons I. The reaction utilized nitroarenes as the nitrogen source, Mo(CO)₆ as both the CO surrogate and the reductant to furnish various indole derivatives I in moderate to high yields.

Molecular Catalysis published new progress about 620-20-2. 620-20-2 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Benzyl chloride,Benzene, name is 3-Chlorobenzylchloride, and the molecular formula is C17H14N2O2, Application of 3-Chlorobenzylchloride.

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

Wang, Qi published the artcilePalladium-catalyzed aminocarbonylative cyclization of benzyl chlorides with 2-nitroaryl alkynes to construct indole derivatives, Related Products of chlorides-buliding-blocks, the publication is Molecular Catalysis (2022), 112302, database is CAplus.

A palladium-catalyzed aminocarbonylative cyclization of benzyl chlorides RCH₂Cl (R = Ph, 3,5-dichlorophenyl, naphthalen-1-yl, etc.) with 2-nitroaryl alkynes 2-NO₂-4-R¹-5-R²C₆H₂CCR³ (R¹ = H, Me, F; R² = H, Cl; R³ = Ph, n-Bu, cyclopropyl, etc.) has been developed for the rapid construction of indole skeletons I. The reaction utilized nitroarenes as the nitrogen source, Mo(CO)₆ as both the CO surrogate and the reductant to furnish various indole derivatives I in moderate to high yields.

Molecular Catalysis 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 C4H10BBrO2, Related Products of chlorides-buliding-blocks.

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

Wang, Qi published the artcileAdditive-Controlled Divergent Synthesis of Indole and 4H-Benzo[d][1,3]oxazine Derivatives: Palladium-Catalyzed Carbonylative Cyclization of 2-Alkynylanilines and Benzyl Chlorides, Quality Control of 939-99-1, the publication is Journal of Organic Chemistry, database is CAplus and MEDLINE.

A palladium-catalyzed divergent carbonylative synthesis of indoles and 4H-benzo[d][1,3]oxazines from 2-alkynylanilines and benzyl chlorides with benzene-1,3,5-triyl triformate (TFBen) as the CO source was developed. The reaction using AlCl₃ as the additive produced various indoles in high yields, while a series of 4H-benzo[d][1,3]oxazines were achieved in moderate yields with AcOH as the additive.

Journal of Organic 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 C13H14N2O, Quality Control of 939-99-1.

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

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

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

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

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 I–III (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

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

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