Category: chlorides-buliding-blocks

Harada, Hiroshi published the artcileDevelopment of potent serotonin-3 (5-HT₃) receptor antagonists. I. Structure-activity relationships of 2-alkoxy-4-amino-5-chlorobenzamide derivatives, Related Products of chlorides-buliding-blocks, the publication is Chemical & Pharmaceutical Bulletin (1995), 43(8), 1364-78, database is CAplus and MEDLINE.

A new series of 2-alkoxy-4-amino-5-chlorobenzamide derivatives bearing five- to seven-membered heteroalicyclic rings in the amine moiety was synthesized and evaluated for serotonin-3 (5-HT₃) receptor antagonistic activity by assaying the ability to antagonize the von Bezold-Jarisch reflex in rats. The five- to seven-membered heterocycles comprise pyrrolidine, morpholine, 1,4-thiazine, piperidine, piperazine, 1,4-oxazepine, 1,4-thiazepine, azepine, and 1,4-diazepine rings. Among them, some benzamide derivatives having a 1,4-diazepine ring showed a potent 5-HT₃ receptor antagonistic activity. In particular, 4-amino-5-chloro-N-(1,4-dimethylhexahydro-1H-1,4-diazepin-6-yl)-2-ethoxybenzamide and the 1-benzyl-4-methylhexahydro-1H-1,4-diazepine analog showed potent 5-HT₃ receptor antagonist activity without 5-HT₄ receptor binding affinity.

Chemical & Pharmaceutical Bulletin published new progress about 36335-47-4. 36335-47-4 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Carboxylic acid,Benzene,Ether, name is 3-Chloro-2,6-dimethoxybenzoic acid, and the molecular formula is C9H9ClO4, Related Products of chlorides-buliding-blocks.

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

Kawanishi, Hiroyuki published the artcileStereoselective synthesis of antifungal sulfoximines, novel triazoles II, Safety of trimethyloxosulphonium chloride, the publication is Heterocycles (1998), 181-190, database is CAplus.

Novel triazole derivatives I (R = H, MeCO, MeNHCO, Me, MeO₂CCH₂) with an N-substituted sulfoximine moiety were synthesized and evaluated for antifungal activity. These compounds showed significantly weaker activity than I (R = H); the N-H moiety of the sulfoximine was extremely important for the activity. A practical and effective stereoselective synthesis of (-)-I (R = H), considered to be the most promising antifungal compound, has been developed. (-)-I (R = H) is prepared in seven steps, including two resolution steps, from the methylthiodifluoropropiophenone II, by epoxidation with Me₃SO⁺ Cl^–, diastereoselective sulfimine formation with chloramine T, addition of 1,2,4-triazole to the epoxide, oxidation of the sulfimine, acid hydrolysis of toluenesulfonyl group of the sulfoximine, and resolution with the novel resolving agent 1-(2,3,4-trichlorophenyl)ethanesulfonic acid [(+)-TCPES] III.

Heterocycles 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 C3H9ClOS, Safety of trimethyloxosulphonium chloride.

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

Hayashi, Koichiro published the artcileChemoselective Synthesis of Folic Acid-Functionalized Magnetite Nanoparticles via Click Chemistry for Magnetic Hyperthermia, HPLC of Formula: 18791-02-1, the publication is Chemistry of Materials (2009), 21(7), 1318-1325, database is CAplus.

Folic acid-functionalized Fe₃O₄ nanoparticles (FA-Fe₃O₄ NPs) were synthesized from iron(III) 3-allylacetylacetonate (IAA) through in situ hydrolysis and ligand modification, by applying the principle of click chem. The γ-carboxylic acid of FA was successfully bound to the ligand of the Fe₃O₄ NPs without the loss of the α-carboxylic acid group of folic acid (FA), which has an affinity for folate receptors (FRs) expressed on tumor cells. The Fe₃O₄ NPs were monodisperse, and their size was controlled by varying the conditions of IAA hydrolysis. The FA-Fe₃O₄ NPs, which had diameters of 8 nm, exhibited superparamagnetic behavior and a relatively high magnetization at room temperature The blocking temperature is 220 K, and the magnetization curve exhibited a remanence of 19 emu/g and a coercivity of 550 Oe at 5 K. The specific absorption rate (SAR) was dependent on the size of the FA-Fe₃O₄ NPs and the strength of the applied magnetic field. The SAR of the 8-nm FA-Fe₃O₄ NPs was 670 W/g in a 230 kHz alternating magnetic field and 100 Oe. The chemoselective surface modification of magnetite particles with FA yielded a novel cancer-targeting system for use in hyperthermia treatment.

Chemistry of Materials published new progress about 18791-02-1. 18791-02-1 belongs to chlorides-buliding-blocks, auxiliary class Aliphatic Chain, name is 2,3-Dibromopropionylchloride, and the molecular formula is C3H3Br2ClO, HPLC of Formula: 18791-02-1.

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

Takano, Seiichi published the artcileChiral synthesis of both enantiomers of 1,4-dideoxy-1,4-iminolyxitol and 1,4-dideoxy-1,4-iminoribitol, Synthetic Route of 18791-02-1, the publication is Tetrahedron: Asymmetry (1992), 3(6), 681-4, database is CAplus.

Reaction of 2,3-dibromopropionyl chloride with 4-methoxyphenol and (S)-1-methylbenzylamine yielded a 4:5 mixture of readily separable diastereomeric aziridine esters I (R = C₆H₄OMe-4) in an excellent yield. Thermal intermol. 1,3-dipolar cycloaddition of both diastereomers with vinylene carbonate, furnished four readily separable diastereomeric pyrrolidine esters, resp., which were transformed into both enantiomers of title compounds

Tetrahedron: Asymmetry published new progress about 18791-02-1. 18791-02-1 belongs to chlorides-buliding-blocks, auxiliary class Aliphatic Chain, name is 2,3-Dibromopropionylchloride, and the molecular formula is C14H22O2, Synthetic Route of 18791-02-1.

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

Fager, Diana C. published the artcileRegio- and Enantioselective Synthesis of Trifluoromethyl-Substituted Homoallylic α-Tertiary NH₂-Amines by Reactions Facilitated by a Threonine-Based Boron-Containing Catalyst, Product Details of C8H4ClF3O, the publication is Angewandte Chemie, International Edition (2020), 59(28), 11448-11455, database is CAplus and MEDLINE.

A method for catalytic regio- and enantioselective synthesis of trifluoromethyl-substituted and aryl-, heteroaryl-, alkenyl-, and alkynyl-substituted homoallylic α-tertiary NH₂-amines is introduced. Easy-to-synthesize and robust N-silyl ketimines are converted to NH-ketimines in situ, which then react with a Z-allyl boronate. Transformations are promoted by a readily accessible L-threonine-derived aminophenol-based boryl catalyst, affording the desired products in up to 91% yield, >98:2 α:γ selectivity, >98:2 Z:E selectivity, and >99:1 enantiomeric ratio. A com. available aminophenol may be used, and allyl boronates, which may contain an alkyl-, a chloro-, or a bromo-substituted Z-alkene, can either be purchased or prepared by catalytic stereoretentive cross-metathesis. In addition, Z-trisubstituted allyl boronates may be used. Various chemo-, regio-, and diastereoselective transformations of the α-tertiary homoallylic NH₂-amine products highlight the utility of the approach; this includes diastereo- and regioselective epoxide formation/trichloroacetic acid cleavage to generate differentiated diol derivatives

Angewandte Chemie, International Edition 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, Product Details of C8H4ClF3O.

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

Balaraman, Kaluvu published the artcileOrganocatalytic Decarboxylative Cyanomethylation of Difluoromethyl and Trifluoromethyl Ketones, Computed Properties of 5860-95-7, the publication is Advanced Synthesis & Catalysis (2018), 360(24), 4705-4709, database is CAplus and MEDLINE.

An efficient organocatalytic method for the synthesis of difluoromethyl and trifluoromethyl substituted β-hydroxynitriles RC(OH)(CXF₂)CH₂CN (R = Ph, cyclohexyl, furan-2-yl, etc.; X = H, F) is introduced. The decarboxylative cyanomethylation of fluorinated ketones RC(O)CXF₂ with readily available cyanoacetic acid gives a variety of tertiary alcs. in high yields and without concomitant water elimination. The reaction occurs in the presence of catalytic amounts of triethylamine, and can be upscaled and applied to chlorofluoromethyl ketones and difluoromethyl ketimines.

Advanced Synthesis & Catalysis 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, Computed Properties of 5860-95-7.

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

Skerratt, Sarah E. published the artcileIdentification of false positives in “HTS hits to lead”: The application of Bayesian models in HTS triage to rapidly deliver a series of selective TRPV4 antagonists, Related Products of chlorides-buliding-blocks, the publication is MedChemComm (2013), 4(1), 244-251, database is CAplus.

Herein, we describe the discovery and optimization of a series of potent and selective TRPV4 antagonists. The application of a variety of computational techniques (including Bayesian modeling) at the HTS triage stage enabled the early deprioritisation of likely frequent hitters. The use of methods to pos. prioritise compounds for follow-up screening allowed the rapid identification of a number of interesting TRPV4 antagonist series. The hit-to-lead efforts in one such series, the hydroxypiperidines, will be described.

MedChemComm published new progress about 254749-11-6. 254749-11-6 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Nitrile,Benzene, name is 2-Chloro-4-cyanobenzene-1-sulfonyl chloride, and the molecular formula is C10H14O, Related Products of chlorides-buliding-blocks.

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

Xu, Xiao published the artcileVisible light-promoted umpolung coupling of aryl tri-/difluoroethanones with 2-alkenylpyridines, SDS of cas: 5860-95-7, the publication is Chemical Communications (Cambridge, United Kingdom) (2018), 54(78), 11017-11020, database is CAplus and MEDLINE.

Using an umpolung strategy, herein the first intermol. reductive cross-coupling of aryl tri-/difluoroethanones with 2-alkenylpyridines with the aid of a Bronsted acid catalyst upon visible-light irradiation is reported. This metal-free reaction is operationally simple and performed at ambient temperature, allowing access to desired tertiary alcs. with tri-/difluoromethyl groups in moderate to excellent yields. The com. available and easily handled Hantzsch ester effectively serves as an electron donor, as well as a hydrogen atom source.

Chemical Communications (Cambridge, United Kingdom) 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 C30H24BrCuN2P, SDS of cas: 5860-95-7.

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

Safonova, T. S. published the artcileRelation of the antitumor activity of spirobromine analogs to their structure, Application of 2,3-Dibromopropionylchloride, the publication is Khimiko-Farmatsevticheskii Zhurnal (1984), 18(12), 1437-40, database is CAplus.

The dispiropiperazines I [R = CHBrCH₂Br, CH:CH₂, CHMeCH₂Br, CH₂CH₂NHCH₂Ph, (CH₂)₃Ph, (CH₂)₃C₆H₄NO₂–p, and (CH₂)₃C₆H₄N(CH₂CH₂Cl)₂–p] were prepared and tested along with spirobromine (I, R = CH₂CH₂Br) [86641-76-1] and 8 dipiperazinylalkanes II (R = Me, H; X = Cl, Br; n = 2, 3, 6, 10) for antitumor activity in sarcoma-bearing rats. Although spirobromine itself showed high antitumor activity, its analogs were only ∼33% as active or completely inactive. Three dipiperazinylalkanes showed very high activity; the others were inactive. Structure-activity relations are discussed.

Khimiko-Farmatsevticheskii Zhurnal published new progress about 18791-02-1. 18791-02-1 belongs to chlorides-buliding-blocks, auxiliary class Aliphatic Chain, name is 2,3-Dibromopropionylchloride, and the molecular formula is C3H3Br2ClO, Application of 2,3-Dibromopropionylchloride.

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

Matsuyama, Naoki published the artcileNickel-Catalyzed Ring-Opening C-O Functionalization of peri-Xanthenoxanthenes for 8-Substituted Binaphthol Synthesis, Computed Properties of 21286-54-4, the publication is Organic Letters (2021), 23(10), 3908-3912, database is CAplus and MEDLINE.

Herein, authors disclose the Ni-catalyzed ring-opening C-O functionalization of peri-xanthenoxanthenes using Grignard reagents that forms 8-mono-functionalized binaphthols. 1,2-Bis(dicyclohexylphosphino)ethane was the best ligand for alkylations and ICy for arylation. After mechanistic investigations, authors assumed that the reaction proceeds via C-O reduction and subsequent C-O functionalization. To verify the mechanism, the intermediate after reduction was isolated. Moreover, the asym. addition, using 8-octylbinaphthol after optical resolution, was studied.

Organic Letters 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, Computed Properties of 21286-54-4.

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