Tag: M.W=250-300

Zhang, Jie-long published the artcileGreen synthesis of germicide Prochloraz, Category: chlorides-buliding-blocks, the publication is Huaxue Shiji (2010), 32(9), 856-858, database is CAplus.

Prochloraz is a broad-spectrum imidazole germicide. The synthesis of the target compound [i.e., N-propyl-N-[2-(2,4,6-trichlorophenoxy)ethyl]-1H-imidazole-1-carboxamide, Prochloraz, Mirage, Preclude, Sportake, etc.] was achieved using using 2,4,6-trichlorophenol, 1,2-ethanediol, imidazole and triphosgene as starting materials in an environmentally friendly synthetic sequence (green chem.).

Huaxue Shiji published new progress about 67747-01-7. 67747-01-7 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Amine,Benzene,Ether,Benzene Compounds, name is N-(2-(2,4,6-Trichlorophenoxy)ethyl)propan-1-amine, and the molecular formula is C4H7F3O2, Category: chlorides-buliding-blocks.

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

Fu, Ying published the artcileDiscovery of N-Aroyl Diketone/Triketone Derivatives as Novel 4-Hydroxyphenylpyruvate Dioxygenase Inhibiting-Based Herbicides, Application In Synthesis of 3919-74-2, the publication is Journal of Agricultural and Food Chemistry (2019), 67(43), 11839-11847, database is CAplus and MEDLINE.

4-Hydroxyphenylpyruvate dioxygenase (EC 1.13.11.27, HPPD) is one of the most promising targets for the discovery of new bleaching herbicides. To discover novel HPPD inhibitors with excellent herbicidal activity, a series of novel N-aroyl diketone/triketone derivatives were rationally designed by splicing active groups and bioisosterism. All the compounds were characterized by IR, ¹H and ¹³C NMR, and high-resolution mass spectrometry. Bioassays revealed that most of these derivatives displayed preferable herbicidal activity against Echinochloa crus-galli at 0.045 mmol/m² and Abutilon juncea at 0.090 mmol/m². In particular, compound (I) was more potent compared with the commercialized compound mesotrione. Mol. docking indicated that the corresponding active mols. of target compounds and mesotrione shared similar interplay with surrounding residues, which led to a perfect interaction with the active site of Arabidopsis thaliana HPPD. These promising findings demonstrate that these compounds could be considered as potential herbicide candidates for further development of novel HPPD inhibitors.

Journal of Agricultural and Food Chemistry published new progress about 3919-74-2. 3919-74-2 belongs to chlorides-buliding-blocks, auxiliary class Isoxazole,Fluoride,Chloride,Carboxylic acid,Benzene, name is 3-(2-Chloro-6-fluorophenyl)-5-methylisoxazole-4-carboxylic acid, and the molecular formula is C11H7ClFNO3, Application In Synthesis of 3919-74-2.

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

Wang, Yan-Guang published the artcileParallel synthesis of pyrazolines on soluble polymer support, Computed Properties of 7080-50-4, the publication is Synlett (2003), 1467-1468, database is CAplus.

An efficient parallel liquid-phase synthesis of pyrazolines I (R¹ = H, Me; R² = Ph, 4-MeOC₆H₄, 2-furyl; R³ = Ph, 4-MeC₆H₄, 4-FC₆H₄) has been developed. The one-pot three-component reaction of polyethylene glycol (PEG)-supported acrylate, arylaldehydes, and aryl hydrazines, in the presence of chloramine-T in methanol, gave the corresponding PEG-supported pyrazolines. Cleavage from the support under mild conditions afforded pyrazolines I in good yields and high purities.

Synlett published new progress about 7080-50-4. 7080-50-4 belongs to chlorides-buliding-blocks, auxiliary class Halogenation Reagent,Inhibitor, name is Sodium chloro(tosyl)amide trihydrate, and the molecular formula is C5H5NO3S, Computed Properties of 7080-50-4.

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

Nourry, Arnaud published the artcileBRAF inhibitors based on an imidazo[4,5]pyridin-2-one scaffold and a meta substituted middle ring, Application of 4-Chloro-3-(trifluoromethyl)benzenesulfonyl Chloride, the publication is Journal of Medicinal Chemistry (2010), 53(5), 1964-1978, database is CAplus and MEDLINE.

We recently reported on the development of a novel series of BRAF inhibitors based on a tripartite A-B-C system characterized by a para-substituted central aromatic core connected to an imidazo[4,5]pyridin-2-one scaffold and a substituted urea linker. Here, we present a new series of BRAF inhibitors in which the central Ph ring connects to the hinge binder and substrate pocket of BRAF with a meta-substitution pattern e. g. I. The optimization of this new scaffold led to the development of low-nanomolar inhibitors that permits the use of a wider range of linkers and terminal C rings while enhancing the selectivity for the BRAF enzyme in comparison to the para series.

Journal of Medicinal Chemistry published new progress about 32333-53-2. 32333-53-2 belongs to chlorides-buliding-blocks, auxiliary class Trifluoromethyl,Fluoride,Chloride,Sulfonyl chlorides,Benzene, name is 4-Chloro-3-(trifluoromethyl)benzenesulfonyl Chloride, and the molecular formula is C7H3Cl2F3O2S, Application of 4-Chloro-3-(trifluoromethyl)benzenesulfonyl Chloride.

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

Sbenati, Rawan M. published the artcileDesign, synthesis, biological evaluation, and modeling studies of novel conformationally-restricted analogues of sorafenib as selective kinase-inhibitory antiproliferative agents against hepatocellular carcinoma cells, Computed Properties of 32333-53-2, the publication is European Journal of Medicinal Chemistry (2021), 113081, database is CAplus and MEDLINE.

Sorafenib is one of the clin. used anticancer agents that inhibits several kinases. In this study, novel indole-based rigid analogs of sorafenib were designed and synthesized in order to enhance kinase selectivity and hence minimize the side effects associated with its use. The target compounds possess different linkers; urea, amide, sulfonamide, or thiourea, in addition to different terminal aryl moieties attached to the linker in order to investigate their impact on biol. activity. They were tested against Hep3B, Huh7, and Hep-G2 hepatocellular carcinoma (HCC) cell lines to study their potency. Among all the tested target derivatives, arylaminocarbonylaminoindolylpicolinamide I exerted superior antiproliferative potency against all the three tested HCC cell lines compared to sorafenib. Based on these preliminary results, I was selected for further biol. and in silico investigations. Up to 30μM, I did not inhibit 50% of the proliferation of WI-38 normal cells, which indicated promising selectivity against HCC cells than normal cells. In addition, I exerted superior kinase selectivity than sorafenib. It is selective for VEGFR2 and VEGFR3 angiogenesis-related kinases, while sorafenib is a multikinase inhibitor. Superior kinase selectivity of I to sorafenib can be attributed to its conformationally-restricted indole nucleus and the bulky N-methylpiperazinyl moiety. Western blotting was carried out and confirmed the ability of I to inhibit VEGFR2 kinase inside Hep-G2 HCC cells in a dose-dependent pattern. I induces apoptosis and necrosis in Hep-G2 cell line, as shown by caspase-3/7 and lactate dehydrogenase (LDH) release assays, resp. Moreover, I did not inhibit hERG. Thus, we could achieve a more selective kinase inhibitor than sorafenib with retained or even better antiproliferative potency against HCC cell lines. Furthermore, mol. docking and dynamic simulation studies were carried out to investigate its binding mode with VEGFR2 kinase. The mol. has a unique orientation upon binding with the kinase.

European Journal of Medicinal Chemistry published new progress about 32333-53-2. 32333-53-2 belongs to chlorides-buliding-blocks, auxiliary class Trifluoromethyl,Fluoride,Chloride,Sulfonyl chlorides,Benzene, name is 4-Chloro-3-(trifluoromethyl)benzenesulfonyl Chloride, and the molecular formula is C7H3Cl2F3O2S, Computed Properties of 32333-53-2.

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

Jiang, Jun published the artcileSynthesis of N-arylsulfonamides via Fe-promoted reaction of sulfonyl halides with nitroarenes in an aqueous medium, Application of ((1S,4R)-7,7-Dimethyl-2-oxobicyclo[2.2.1]heptan-1-yl)methanesulfonyl chloride, the publication is Organic & Biomolecular Chemistry (2018), 16(27), 5016-5020, database is CAplus and MEDLINE.

A fascinating Fe-promoted protocol for the synthesis of N-arylsulfonamides has been developed. Starting from com. available nitroarenes R¹NO₂ (R¹ = Ph, 2-ClC₆H₄, 4-HOC₆H₄, 1,2,4-triazol-3-yl, etc.) and sulfonyl chlorides R²SO₂Cl (R² = Me, Ph, 3-BrC₆H₄, 2-naphthyl, 2-thienyl, etc.), moderate to excellent yields of the corresponding N-arylsulfonamides R¹NHSO₂R² can be obtained. In particular, Fe dust serves as the sole reductant in the transformation and it can be easily performed on a large scale.

Organic & Biomolecular 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 C10H15ClO3S, Application of ((1S,4R)-7,7-Dimethyl-2-oxobicyclo[2.2.1]heptan-1-yl)methanesulfonyl chloride.

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

Dong, Xiao-Yang published the artcileCopper-Catalyzed Asymmetric Coupling of Allenyl Radicals with Terminal Alkynes to Access Tetrasubstituted Allenes, Computed Properties of 866-23-9, the publication is Angewandte Chemie, International Edition (2021), 60(4), 2160-2164, database is CAplus and MEDLINE.

In contrast to the wealth of asym. transformations for generating central chirality from alkyl radicals, the enantiocontrol over the allenyl radicals for forging axial chirality represents an uncharted domain. The challenge arises from the unique elongated linear configuration of the allenyl radicals that necessitates the stereo-differentiation of remote motifs away from the radical reaction site. We herein describe a copper-catalyzed asym. radical 1,4-carboalkynylation of 1,3-enynes via the coupling of allenyl radicals with terminal alkynes, providing diverse synthetically challenging tetrasubstituted chiral allenes. A chiral N,N,P-ligand is crucial for both the reaction initiation and the enantiocontrol over the highly reactive allenyl radicals. The reaction features a broad substrate scope, covering a variety of (hetero)aryl and alkyl alkynes and 1,3-enynes as well as radical precursors with excellent functional group tolerance.

Angewandte Chemie, International Edition published new progress about 866-23-9. 866-23-9 belongs to chlorides-buliding-blocks, auxiliary class Aliphatic Chain, name is Diethyltrichloromethylphosphonate, and the molecular formula is C5H10Cl3O3P, Computed Properties of 866-23-9.

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

Wang, Weiyi published the artcileStereodefined rhodium-catalysed 1,4-H/D delivery for modular syntheses and deuterium integration, Quality Control of 21286-54-4, the publication is Nature Catalysis (2021), 4(7), 586-594, database is CAplus.

Here, a 1,4-H delivery of allylic metallic species to provide a highly stereoselective and straightforward approach to 3-methyl-2(E)-enals or -enones from readily available 2,3-allenols and organoboronic acids was reported. The reaction accommodated many synthetically versatile functional groups as well as multi-pharmacophores, and was not limited to the formation of 3-Me derivatives By applying 1,4-H or D delivery, deuterium atom(s) from differently deuterated allenols was edited into the Me or methylene groups of versatile organic skeletons, resulting in the efficient formation of 4-monodeuterated, 1,4- and 4,4-doubly deuterated, and 4,4,4-triply deuterated 2(E)-enals or -enones. These powerful platform mols. was provide straightforward paths to other deuterated compounds for different purposes.

Nature Catalysis 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 C17H29BO2, Quality Control of 21286-54-4.

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

Zhang, Wen-Ming published the artcileThe synthesis and antistaphylococcal activity of N-sulfonaminoethyloxime derivatives of dehydroabietic acid, Related Products of chlorides-buliding-blocks, the publication is Bioorganic & Medicinal Chemistry Letters (2018), 28(10), 1943-1948, database is CAplus and MEDLINE.

A series of N-sulfonaminoethyloxime derivatives of dehydroabietic acid were synthesized and investigated for their antibacterial activity against Staphylococcus aureus Newman strain and multidrug-resistant strains (NRS-1, NRS-70, NRS-100, NRS-108 and NRS-271). Most of the target compounds having chloro, bromo, trifluoromethyl Ph moiety exhibited potent in vitro antistaphylococcal activity. The meta-CF3 Ph derivative T23 showed the highest activity with MIC of 0.390.78 μg/mL against S. aureus Newman, while several analogs showed similar potent antibacterial activity with MIC values between 0.78 and 1.56 μg/mL against fve multidrug-resistant S. aureus. The stability of T35 in plasma of SD rat and the cellular cytotoxicity were also evaluated.

Bioorganic & Medicinal Chemistry Letters published new progress about 32333-53-2. 32333-53-2 belongs to chlorides-buliding-blocks, auxiliary class Trifluoromethyl,Fluoride,Chloride,Sulfonyl chlorides,Benzene, name is 4-Chloro-3-(trifluoromethyl)benzenesulfonyl Chloride, and the molecular formula is C38H24F4O4P2, Related Products of chlorides-buliding-blocks.

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

Hasegawa, Futoshi published the artcileHighly Efficient Syntheses of C-N Axially Chiral 1-(ortho-hydroxyaryl)uracil using a Chiral Auxiliary and a Chiral Base, SDS of cas: 21286-54-4, the publication is Asian Journal of Organic Chemistry (2018), 7(8), 1648-1653, database is CAplus.

A highly diastereoselective synthesis of 1-aryl-6-aminouracils, which were C-N atropisomeric compounds, through the combined use of a chiral auxiliary and a chiral base under mild conditions was achieved. The (R)-5-allyl-2-oxabicyclo[3.3.0]oct-1-yl group was a good chiral auxiliary that, when combined with quinidine, efficiently afforded 1-aryl-6-aminouracils with high diastereoselectivity (up to 98 % ee after isolation). The chiral alc. moiety in quinidine appeared to be crucial for achieving stereoselectivity during cyclization. Furthermore, the chiral auxiliary was easily removed from the product under acidic conditions to provide the atropisomer with high enantiomeric excess (up to 96 % ee). The developed method was an efficient diastereoselective-cyclization method for the generation of C-N axial chirality.

Asian 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 C10H15ClO3S, SDS of cas: 21286-54-4.

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