Category: 10602-04-7

Kim, Seon Woong; Lee, Taeho; Lee, Joo-Youn; Kim, Sanghee; Jun, Hee-Sook; Park, Eun-Young; Baek, Dong Jae published the artcile< Synthesis and Biological Evaluation of PF-543 Derivative>, Related Products of 10602-04-7, the main research area is phenylsulfonylmethylphenethyl benzylpyrrolidinyl methanol preparation antitumor mol docking sphingosine kinase.

Compared PF-543 I and synthesized a newly designed derivative of PF-543 II in which two aromatic structures were connected in para-form. The synthesized derivative II showed inhibitory effect on SK1, similar to that of PF-543 I. However, it was more cytotoxic to HT29, AGS, and PC3 cells than PF-543 I. Also carried out a docking study for SK1 and demonstrated that the synthesized derivative II showed interaction with SK1 similar to PF-543 I. Results obtained from this study suggest that the structure of II may be well substituted for the structure of PF-543 I in terms of biol. activity, providing important structural information for the design of new derivatives of PF-543 II.

Letters in Organic Chemistry published new progress about Antitumor agents. 10602-04-7 belongs to class alcohols-buliding-blocks, and the molecular formula is C9H8O, Related Products of 10602-04-7.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Li, Qi; Wang, Zi-Lu; Lu, Huan-Xuan; Xu, Yun-He published the artcile< Copper-Catalyzed Enantioselective 1,4-Protosilylation of Alkynyl-substituted Enones to Synthesize the Highly Diastereomeric Chiral Homoallenylsilanes>, Electric Literature of 10602-04-7, the main research area is copper catalyzed enantioselective protosilylation alkynyl enone; diastereomeric enantioselective chiral homoallenylsilane preparation crystal mol structure.

A copper-catalyzed 1,4-protosilylation of α-alkynyl-enones to form the functionalized chiral homoallenylsilanes was developed. In the presence of a chiral monopyridine oxazoline ligand, a variety of trisubstituted allene derivatives bearing a contiguous stereogenic center and axis were prepared in good yields with excellent enantioselectivities and diastereoselectivities.

Organic Letters published new progress about Allenes Role: PRP (Properties), RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 10602-04-7 belongs to class alcohols-buliding-blocks, and the molecular formula is C9H8O, Electric Literature of 10602-04-7.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Kirsch, Philine; Jakob, Valentin; Oberhausen, Kevin; Stein, Saskia C.; Cucarro, Ivano; Schulz, Thomas F.; Empting, Martin published the artcile< Fragment-Based Discovery of a Qualified Hit Targeting the Latency-Associated Nuclear Antigen of the Oncogenic Kaposi's Sarcoma-Associated Herpesvirus/Human Herpesvirus 8>, Formula: C9H8O, the main research area is Kaposi sarcoma human herpesvirus 8 antiviral LANA.

The latency-associated nuclear antigen (LANA) is required for latent replication and persistence of Kaposi’s sarcoma-associated herpesvirus/human herpesvirus 8. It acts via replicating and tethering the virus episome to the host chromatin and exerts other functions. We conceived a new approach for the discovery of antiviral drugs to inhibit the interaction between LANA and the viral genome. We applied a biophys. screening cascade and identified the first LANA binders from small, structurally diverse compound libraries. Starting from a fragment-sized scaffold, we generated optimized hits via fragment growing using a dedicated fluorescence-polarization-based assay as the structure-activity-relationship driver. We improved compound potency to the double-digit micromolar range. Importantly, we qualified the resulting hit through orthogonal methods employing EMSA, STD-NMR, and MST methodologies. This optimized hit provides an ideal starting point for subsequent hit-to-lead campaigns providing evident target-binding, suitable ligand efficiencies, and favorable physicochem. properties.

Journal of Medicinal Chemistry published new progress about Antiviral agents. 10602-04-7 belongs to class alcohols-buliding-blocks, and the molecular formula is C9H8O, Formula: C9H8O.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Bae, Kideog; Zheng, Wei; Ma, Ying; Huang, Zhiwei published the artcile< Real-Time Monitoring of Pharmacokinetics of Mitochondria-Targeting Molecules in Live Cells with Bioorthogonal Hyperspectral Stimulated Raman Scattering Microscopy>, HPLC of Formula: 10602-04-7, the main research area is raman scattering microscopy mitochondria pharmacokinetics live cells.

The dynamics of mitochondria in live cells play a pivotal role in biol. events such as cell metabolism, early stage apoptosis, and cell differentiation. Triphenylphosphonium (TPP) is a commonly used mitochondria-targeting agent for mitochondrial studies. However, there has been a lack of understanding in intracellular behaviors of TPP in the course of targeting mitochondria due to the difficulty in tracking and quantifying small mols. in a biol. environment. Here, we report the utility of hyperspectral stimulated Raman scattering (SRS) microscopy associated with a Raman tag synthesized for real-time visualization and quantitation of TPP dynamics within live cells at the subcellular level. With the myriad of merits offered by a synthesized aryl-diyne-based Raman tag such as excellent photostability, negligible background interferences, and a linear dependence of the SRS signal on the TPP concentration, we successfully establish a quant. model to associate the mitochondrial membrane potential with the key pharmacokinetic parameters of TPP inside the live cells. The model reveals that reduction in the mitochondrial membrane potential leads to significant decreases in both the uptake rate and intracellular concentrations of TPP. Further, on the basis of the multiplexed SRS images concurrently highlighting the cellular proteins and lipids without further labeling, we find that the TPP uptake causes little cytotoxicity to the host cells. The bioorthogonal hyperspectral SRS microscopy imaging reveals that TPP can maintain stable affinity to mitochondria during the restructuring of mitochondrial networking, demonstrating its great potential for real-time monitoring of pharmacokinetics of small mols. associated with live biol. hosts, thereby promoting the development of mitochondria-targeting imaging probes and therapies in the near future.

Analytical Chemistry (Washington, DC, United States) published new progress about Bioorthogonal reaction (bioorthogonal hyperspectral SRS microscopy). 10602-04-7 belongs to class alcohols-buliding-blocks, and the molecular formula is C9H8O, HPLC of Formula: 10602-04-7.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

You, Peiye; Wei, Rongjia; Ning, Guohong; Li, Dan published the artcile< An Eosin Y Encapsulated Cu(I) Covalent Metal Organic Framework For Efficient Photocatalytic Sonogashira Cross-Coupling Reaction>, HPLC of Formula: 10602-04-7, the main research area is Eosin Y encapsulated copper covalent metal organic framework preparation; internal alkyne selective preparation; iodobenzene alkyne Sonogashira cross coupling copper photocatalyst.

Herein, the encapsulation of an organic dye(i.e., Eosin Y, EY) into a Cu(I) cyclic trinuclear unit(CTU) based covalent-metal organic framework(CMOF), namely EY@JNM-1, as photocatalyst for the Sonogashira cross-coupling reaction of iodobenzene with alkynes to afford internal alkynes I [R = Ph, 4-MeC6H4, 4-ClC6H4, etc.] was reported. The EY@JNM-1 not only exhibited high catalytic activity for the alkynes(>99% conversion) and excellent selectivity for the cross-coupling product(>99%) under mild conditions, but also displayed excellent stability and recyclability.

Chemical Research in Chinese Universities published new progress about Alkynes Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 10602-04-7 belongs to class alcohols-buliding-blocks, and the molecular formula is C9H8O, HPLC of Formula: 10602-04-7.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Wang, Huamin; Shi, Wenyan; Li, Yongli; Yu, Mingming; Gao, Yuan; Lei, Aiwen published the artcile< Photoinduced radical relay way toward α-CF3 ketones with low-cost trifluoromethylation reagents>, Quality Control of 10602-04-7, the main research area is alpha trifluoromethyl ketone preparation; alkyne trifluoromethanesulfonic anhydride trifluoromethylation photoinduction; triethylsilyl trifluoromethanesulfonate alkyne trifluoromethylation photoinduction.

A cost-efficient and practical approach of photoinduction of a radical relay process was disclosed for the synthesis of α-CF3 ketones ArC(O)CH2CF3 [Ar = Ph, 4-ClC6H4, 4-PhC6H4, etc.] using alkynes and low-cost trifluoromethylation reagents. It was showed that trifluoromethylation reagents such as TES-OTf, Tf2O, TMS-OTf, TBS-OTf, H-OTf, and others could be used successfully as inexpensive CF3 precursors under metal-free and redox-neutral conditions. The potential application of this protocol was highlighted and gram-scale synthesis. Mechanistic studies revealed that this transformation might involve a radical process, and acetic acid not only promoted the formation of enol triflates, but also accelerated the in situ conversion from enol triflates to α-CF3 ketones.

CCS Chemistry published new progress about Alkynes Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 10602-04-7 belongs to class alcohols-buliding-blocks, and the molecular formula is C9H8O, Quality Control of 10602-04-7.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Tironi, Matteo; Dix, Stefan; Hopkinson, Matthew N. published the artcile< Deoxygenative nucleophilic difluoromethylselenylation of carboxylic acids and alcohols with BT-SeCF2H>, Category: alcohols-buliding-blocks, the main research area is carboxylic acid alc difluoromethylselenylation deoxygenative nucleophilic.

The benzothiazolium salt BT-SeCF2H is introduced as an efficient nucleophilic reagent for transferring difluoromethylselenyl groups onto organic mols. SeCF2H-Containing selenoesters could be prepared upon deoxygenative substitution of readily available carboxylic acids, while silver catalysis allowed for efficient formation of (difluoromethyl)selenoethers, including the established electrophilic reagent BnSeCF2H, directly from simple alcs. To the best of knowledge, these deoxygenative reactions represent the first reported nucleophilic difluoromethylselenylation processes and thus open up new approaches to prepare valuable fluorinated compounds

Organic Chemistry Frontiers published new progress about Alcohols Role: RCT (Reactant), RACT (Reactant or Reagent). 10602-04-7 belongs to class alcohols-buliding-blocks, and the molecular formula is C9H8O, Category: alcohols-buliding-blocks.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Mandler, Michael D.; Degnan, Andrew P.; Zhang, Shasha; Aulakh, Darpandeep; Georges, Ketleine; Sandhu, Bhupinder; Sarjeant, Amy; Zhu, Yeheng; Traeger, Sarah C.; Cheng, Peter T.; Ellsworth, Bruce A.; Regueiro-Ren, Alicia published the artcile< Structural and Thermal Characterization of Halogenated Azidopyridines: Under-Reported Synthons for Medicinal Chemistry>, COA of Formula: C9H8O, the main research area is halogenated azidopyridine preparation structure thermal property click reaction; safety shock sensitivity energetic material.

Owing to their participation in Click reactions, bifunctional azides are valuable intermediates in the preparation of medicines and biochem. tool compounds Despite the privileged nature of pyridines among pharmaceutical scaffolds, reports of the synthesis and characterization of azidopyridines bearing a halogen substituent for further elaboration are almost completely unknown in the literature. As azidopyridines carry nearly equal numbers of nitrogen and carbon atoms, we hypothesized that safety concerns limited the application of these useful bifunctional building blocks in medicinal and biol. chem. To address this concern, we prepared and characterized nine azidopyridines bearing a single fluorine, chlorine, or bromine atom. All were examined by differential scanning calorimetry (DSC), in which they demonstrated exotherms of 228-326 kJ/mol and onset temperatures between 119 and 135°C. Selected azidopyridines were advanced to mech. stress testing, in which impact sensitivity was noted for one regioisomer of C5H3FN4. The utility of these versatile intermediates was demonstrated through their use in a variety of Click reactions and the diversification of the halogen handles.

Organic Letters published new progress about Alkynes Role: RCT (Reactant), RACT (Reactant or Reagent). 10602-04-7 belongs to class alcohols-buliding-blocks, and the molecular formula is C9H8O, COA of Formula: C9H8O.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Tironi, Matteo; Hopkinson, Matthew N. published the artcile< Silver-Catalyzed Nucleophilic Deoxydifluoromethylthiolation of Activated Aliphatic Alcohols with BT-SCF2H>, Related Products of 10602-04-7, the main research area is difluoromethylthioether preparation; aliphatic alc difluoromethyl thio methylbenzothiazolium triflate nucleophilic deoxydifluoromethylthiolation silver.

Deoxygenative conversion of alcs. into difluoromethylthioethers is reported using 2-((difluoromethyl)thio)-3-methylbenzo[d]thiazol-3-ium triflate (BT-SCF2H) as a source of -SCF2H anions. The presence of silver(I) triflate as a catalyst was found to be crucial for stabilizing the in situ-generated anion, while the concomitant formation of a reactive 2-(alkoxy)benzothiazolium electrophile likely ensures a fast onward substitution reaction, avoiding the build-up of -SCF2H. To the best of authors’ knowledge, this process represents the first report of a direct nucleophilic substitution reaction with -SCF2H and delivers products containing the medicinally relevant difluoromethylthio motif in a single step from widely available alcs.

European Journal of Organic Chemistry published new progress about Aralkyl alcohols Role: RCT (Reactant), RACT (Reactant or Reagent). 10602-04-7 belongs to class alcohols-buliding-blocks, and the molecular formula is C9H8O, Related Products of 10602-04-7.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Yang, Shao-Qian; Wang, Yi-Fan; Zhao, Wei-Cheng; Lin, Guo-Qiang; He, Zhi-Tao published the artcile< Stereodivergent Synthesis of Tertiary Fluoride-Tethered Allenes via Copper and Palladium Dual Catalysis>, COA of Formula: C9H8O, the main research area is fluoroester conjugated enyne copper palladium hydrocarbonation catalyst; allene stereoselective preparation gold cyclization; fluorinated hydrofuran stereoselective preparation.

Herein we describe a protocol for the unprecedented stereodivergent synthesis of tertiary fluoride-tethered allenes bearing a stereogenic center and stereogenic axis via Cu/Pd synergistic catalysis. A broad scope of conjugated enynes are coupled with various α-fluoroesters in high yields with high diastereoselectivities and generally >99% ee. In addition, the four stereoisomers of the allene products ensure precise access to the corresponding four stereoisomers of the fluorinated hydrofurans via a novel stereodivergent axial-to-central chirality transfer process.

Journal of the American Chemical Society published new progress about Alkenynes Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation) (conjugated). 10602-04-7 belongs to class alcohols-buliding-blocks, and the molecular formula is C9H8O, COA of Formula: C9H8O.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts