Tag: M.W=200-250

Gensini, Martina; Battaglia, Gianluca; Nannicini, Rossano; Guerri, Annalisa; Altamura, Maria; Quartara, Laura published the artcile< Solvent-dependent benzylic radical bromination in aromatic sulfonyl chlorides>, Computed Properties of 42413-03-6, the main research area is bromination toluenesulfonyl chloride derivative solvent effect; bromomethylphenylsulfonyl chloride derivative preparation x ray; crystal structure bromomethylphenylsulfonyl chloride derivative; mol structure bromomethylphenylsulfonyl chloride derivative.

The title reaction of sulfonyl chloride I (R = H) in MeCN gave I (R = Br) with high yield and reproducibility and no byproducts. Three analogs of I (R = H) were similarly brominated.

Letters in Organic Chemistry published new progress about Arenesulfonyl chlorides Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 42413-03-6 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H6Cl2O2S, Computed Properties of 42413-03-6.

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

Liu, Kevin G.; Kim, Ji-In; Olszewski, Kellen; Barsotti, Anthony M.; Morris, Koi; Lamarque, Christophe; Yu, Xuemei; Gaffney, Jack; Feng, Xiao-Jiang; Patel, Jeegar P.; Poyurovsky, Masha V. published the artcile< Discovery and Optimization of Glucose Uptake Inhibitors>, Safety of 2,6-Dichloro-9-methyl-9H-purine, the main research area is glucose transporters inhibitors GLUT1 GLUT3 bioavailable ADME SAR.

Aerobic glycolysis, originally identified by Warburg as a hallmark of cancer, has recently been implicated in immune cell activation and growth. Glucose, the starting material for glycolysis, is transported through the cellular membrane by a family of glucose transporters (GLUTs). Therefore, targeting glucose transporters to regulate aerobic glycolysis is an attractive approach to identify potential therapeutic agents for cancers and autoimmune diseases. Herein, we describe the discovery and optimization of a class of potent, orally bioavailable inhibitors of glucose transporters, targeting both GLUT1 and GLUT3.

Journal of Medicinal Chemistry published new progress about Autoimmune disease. 2382-10-7 belongs to class chlorides-buliding-blocks, and the molecular formula is C6H4Cl2N4, Safety of 2,6-Dichloro-9-methyl-9H-purine.

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

Imanishi, Masashi; Tomishima, Yasuyo; Itou, Shinji; Hamashima, Hitoshi; Nakajima, Yutaka; Washizuka, Kenichi; Sakurai, Minoru; Matsui, Shigeo; Imamura, Emiko; Ueshima, Koji; Yamamoto, Takao; Yamamoto, Nobuhiro; Ishikawa, Hirofumi; Nakano, Keiko; Unami, Naoko; Hamada, Kaori; Matsumura, Yasuhiro; Takamura, Fujiko; Hattori, Kouji published the artcile< Discovery of a Novel Series of Biphenyl Benzoic Acid Derivatives as Potent and Selective Human β3-Adrenergic Receptor Agonists with Good Oral Bioavailability. Part I>, Synthetic Route of 603122-80-1, the main research area is biphenyl benzoic acid derivative preparation beta adrenergic receptor agonist.

A novel class of biphenyl analogs containing a benzoic acid moiety based on lead compound I have been identified as potent and selective human β3 adrenergic receptor (β3-AR) agonists with good oral bioavailability and long plasma half-life. After further substituent effects were investigated at the terminal Ph ring of lead compound I, it has been discovered that more lipophilic substitution at the R position improved potency and selectivity. As a result of these studies, II and III were identified as the leading candidates with the best balance of potency, selectivity, and pharmacokinetic profiles. In addition, compounds II and III were evaluated to be efficacious for a carbachol-induced increase of intravesical pressure, such as an overactive bladder model in anesthetized dogs. This represents the first demonstrated result dealing with β3-AR agonists.

Journal of Medicinal Chemistry published new progress about Homo sapiens. 603122-80-1 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H8BClO4, Synthetic Route of 603122-80-1.

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

Miyagawa, Masayoshi; Akiyama, Toshiyuki; Mikamiyama-Iwata, Minako; Hattori, Kazunari; Kurihara, Naoko; Taoda, Yoshiyuki; Takahashi-Kageyama, Chika; Kurose, Noriyuki; Mikamiyama, Hidenori; Suzuki, Naoyuki; Takaya, Kenji; Tomita, Kenji; Matsuo, Kenji; Morimoto, Kenji; Yoshida, Ryu; Shishido, Takao; Yoshinaga, Tomokazu; Sato, Akihiko; Kawai, Makoto published the artcile< Discovery of novel 5-hydroxy-4-pyridone-3-carboxy acids as potent inhibitors of influenza Cap-dependent endonuclease>, HPLC of Formula: 16799-05-6, the main research area is hydroxy pyridonecarboxy acid preparation influenza Cap endonuclease inhibitor; Anti-influenza drug; Cap-dependent endonuclease; Chelator; Pyridone; Virtual modeling.

We report the discovery of a novel series of influenza Cap-dependent EndoNuclease (CEN) inhibitors based on the 4-pyridone-carboxylic acid (PYXA) scaffold, which were found from our chelate library. Our SAR research revealed the lipophilic domain to be the key to CEN inhibition. In particular, the position between the chelate and the lipophilic domain in the derivatives was essential for enhancing the potency. Our study, based on virtual modeling, led to the identification of 2y as a potent CEN inhibitor with an IC50 of 5.12 nM.

Bioorganic & Medicinal Chemistry Letters published new progress about Antiviral agents. 16799-05-6 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H8BrCl, HPLC of Formula: 16799-05-6.

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

Saito, Masato; Kawamata, Yu; Meanwell, Michael; Navratil, Rafael; Chiodi, Debora; Carlson, Ethan; Hu, Pengfei; Chen, Longrui; Udyavara, Sagar; Kingston, Cian; Tanwar, Mayank; Tyagi, Sameer; McKillican, Bruce P.; Gichinga, Moses G.; Schmidt, Michael A.; Eastgate, Martin D.; Lamberto, Massimiliano; He, Chi; Tang, Tianhua; Malapit, Christian A.; Sigman, Matthew S.; Minteer, Shelley D.; Neurock, Matthew; Baran, Phil S. published the artcile< N-Ammonium Ylide Mediators for Electrochemical C-H Oxidation>, Product Details of C8H4ClF3O2, the main research area is ketone preparation regioselective chemoselective; aldehyde preparation regioselective chemoselective; hydrocarbon electrochem oxidation; ammonium ylide preparation.

Herein, a rationally designed platform that provides a step toward this challenge using N-ammonium ylides e.g., acetamidotrimethylazanium-tetrafluoroboranuide as electrochem. driven oxidants for site-specific, chemoselective C(sp3)-H oxidn was presented. By taking a first-principles approach guided by computation, these new mediators were identified and rapidly expanded into a library using ubiquitous building blocks and trivial synthesis techniques. The ylide-based approach to C-H oxidation exhibits tunable selectivity that is often exclusive to this class of oxidants and can be applied to real-world problems in the agricultural and pharmaceutical sectors.

Journal of the American Chemical Society published new progress about Acid chlorides Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 162046-61-9 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H4ClF3O2, Product Details of C8H4ClF3O2.

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

Zhang, Wei; Xiang, Xin-Xin; Chen, Junyi; Yang, Chen; Pan, Yu-Liang; Cheng, Jin-Pei; Meng, Qingbin; Li, Xin published the artcile< Direct C-H difluoromethylation of heterocycles via organic photoredox catalysis>, Reference of 2382-10-7, the main research area is difluoromethylation regioselective organic photoredox catalysis; heteroarene sodium difluoromethanesulfinate difluoromethylation aerobic.

The discovery of modern medicine relies on the sustainable development of synthetic methodologies to meet the needs associated with drug mol. design. Heterocycles containing difluoromethyl groups are an emerging but scarcely investigated class of organofluoro mols. with potential applications in pharmaceutical, agricultural and material science. Herein, authors developed an organophotocatalytic direct difluoromethylation of heterocycles using O2 as a green oxidant. The C-H oxidative difluoromethylation obviates the need for pre-functionalization of the substrates, metals and additives. The operationally straightforward method enriches the efficient synthesis of many difluoromethylated heterocycles in moderate to excellent yields. The direct difluoromethylation of pharmaceutical moleculars demonstrates the practicability of this methodol. to late-stage drug development. Moreover, 2′-deoxy-5-difluoromethyluridine exhibits promising activity against some cancer cell lines, indicating that the difluoromethylation methodol. might provide assistance for drug discovery.

Nature Communications published new progress about Antitumor agents. 2382-10-7 belongs to class chlorides-buliding-blocks, and the molecular formula is C6H4Cl2N4, Reference of 2382-10-7.

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

Hong, Cynthia M.; Whittaker, Aaron M.; Schultz, Danielle M. published the artcile< Nucleophilic Fluorination of Heteroaryl Chlorides and Aryl Triflates Enabled by Cooperative Catalysis>, Synthetic Route of 2382-10-7, the main research area is heteroaryl chloride crown ether catalyst nucleophilic fluorination; heteroaromatic fluoride preparation; phenyl triflate crown ether catalyst nucleophilic fluorination; fluorobenzene preparation.

A new approach that leverages the cooperative action of 18-crown-6 ether and tetramethylammonium chloride to catalytically access the reactivity of tetramethylammonium fluoride and achieve halex fluorinations under mild conditions with operational ease was reported. The described methodol. readily converts both heteroaryl chlorides and aryl triflates to their corresponding (hetero)aryl fluorides in high yields and purities.

Journal of Organic Chemistry published new progress about Aryl chlorides Role: RCT (Reactant), RACT (Reactant or Reagent). 2382-10-7 belongs to class chlorides-buliding-blocks, and the molecular formula is C6H4Cl2N4, Synthetic Route of 2382-10-7.

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

Gutorov, L. A.; Golovchinskaya, E. S. published the artcile< Syntheses in the purine series. XXXIV. Transformations of N,N'-dimethylxanthines in the reaction with phosphoryl chloride in the presence of tert-amines>, Electric Literature of 2382-10-7, the main research area is xanthine reaction phosphorus oxychloride; purine chloro methyl.

Purine derivative (I; X = OPOCl2) (II) was obtained in ∼18% yield by boiling theobromine with POCl3 in Me2NH for 8 hr. Hydrolysis of II with aqueous NaOH gave purine (I; X = Cl). Boiling the latter with PhCl afforded purine (III; R = p-Me2N- C6H4). III (R = Cl) was obtained in ∼90% yield by boiling theobromine with POCl3 containing Et3N·HCl.

Khimiko-Farmatsevticheskii Zhurnal published new progress about 2382-10-7. 2382-10-7 belongs to class chlorides-buliding-blocks, and the molecular formula is C6H4Cl2N4, Electric Literature of 2382-10-7.

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

Shinde, Popat S.; Patil, Nitin T. published the artcile< Gold-Catalyzed Dehydrazinative C(sp)-S Coupling Reactions of Arylsulfonyl Hydrazides with Ethynylbenziodoxolones for Accessing Alkynyl Sulfones>, Related Products of 42413-03-6, the main research area is alkynyl sulfone preparation; arylsulfonyl hydrazide preparation ethynylbenziodoxolone dehydrazinative coupling reaction gold catalyst.

A gold(III)-catalyzed dehydrazinative coupling reaction between arylsulfonyl hydrazides RS(O)2NHNH2 (R = C6H5CH2, 5-bromothiophen-2-yl, naphthalen-2-yl, etc.) and ethynylbenziodoxolone reagents I [R1 = Si(CH(CH3)2)3, Si(CH3)2C(CH3)3, Si(C6H5)2C(CH3)3] was realized for the synthesis of alkynyl sulfones RS(O)2CCR1. The scope and versatility of the reaction were demonstrated by the efficient synthesis of 23 derivatives with diverse structural features.

European Journal of Organic Chemistry published new progress about Coupling reaction (C-S). 42413-03-6 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H6Cl2O2S, Related Products of 42413-03-6.

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

Lu, Yuhan; Han, Yingzhi; Sun, Yadong; Abdukader, Ablimit; Wang, Duozhi; Liu, Chenjiang published the artcile< Application of iodobenzene acetate promoted oxidation in the synthesis of 2-amino-1,3,4-thiadiazole molecules>, Computed Properties of 70057-67-9, the main research area is iodobenzene acetate oxidation amino thiadiazole synthesis.

A highly method for intramol. oxidative coupling reaction of thiosemicarbazone promoted by hypervalent iodine reagent was reported. 2-Amino-1,3,4-thiadiazole derivatives could be synthesized effectively. Hypervalent iodine could be used as a mild reagent with low toxicity, low cost, easy circulation and operation. The reaction had the advantages of easy preparation of raw materials, simple operation and better performance. The applicability of substrates and the reaction mechanism were also preliminarily studied.

Youji Huaxue published new progress about Oxidative coupling reaction catalysts. 70057-67-9 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H6ClN3S, Computed Properties of 70057-67-9.

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