Month: October 2022

Drobnica, L.; Knoppova, V.; Komanova, E. published the artcile< Isothiocyanates. XXXII. Microsynthesis of 3-substituted rhodanines>, Related Products of 10574-69-3, the main research area is rhodanine isothiocyanate thioglycolate.

Eleven 3-substituted rhodanines (I, R = Me, allyl, Ph, p-MeOC6H4, PhCH2, etc.) were prepared by addition of RNCS to HSCH2CO2R1(R1 = H, Et) and acid cyclization of the resultant thiocarbamoylmercaptoacetates RNHCS2CH2CO2R1. I were purified by thinlayer chromatog. Kinetic and uv data were given.

Chemicke Zvesti published new progress about 10574-69-3. 10574-69-3 belongs to class thiazole, and the molecular formula is C10H9NOS2, Related Products of 10574-69-3.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Sun, Shuang; Oliveira, Bruno L.; Jimenez-Oses, Gonzalo; Bernardes, Goncalo J. L. published the artcile< Radical-Mediated Thiol-Ene Strategy: Photoactivation of Thiol-Containing Drugs in Cancer Cells>, Name: Ethyl 2-(((tert-butoxycarbonyl)amino)methyl)thiazole-4-carboxylate, the main research area is photoactivation thiol containing drug cancer; cage compounds; cancer; photochemistry; radicals; thiol-ene.

Photoactivated drugs provide an opportunity to improve efficacy alongside reducing side-effects in the treatment of severe diseases such as cancer. Described herein is a photoactivation decaging method of isobutylene-caged thiols through a UV-initiated thiol-ene reaction. The method was demonstrated with an isobutylene-caged cysteine, cyclic disulfide-peptide, and thiol-containing drug, all of which were rapidly and efficiently released under mild UV irradiation in the presence of thiol sources and a photoinitiator. Importantly, it is shown that the activity of histone deacetylase inhibitor largazole can be switched off when stapled, but selectively switched on within cancer cells when irradiated with non-phototoxic light.

Angewandte Chemie, International Edition published new progress about Antitumor agents. 96929-05-4 belongs to class thiazole, and the molecular formula is C12H18N2O4S, Name: Ethyl 2-(((tert-butoxycarbonyl)amino)methyl)thiazole-4-carboxylate.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Liu, Shihui; Pan, Peng; Fan, Huaqiang; Li, Hao; Wang, Wei; Zhang, Yongqiang published the artcile< Photocatalytic C-H silylation of heteroarenes by using trialkylhydrosilanes>, Formula: C7H9NO2S, the main research area is photocatalytic silylation heteroarene hydrosilane green chem.

The efficient and selective C-H silylation of heteroarenes, especially the pharmaceutically relevant electron-deficient heteroarenes, represents a great challenge in organic synthesis. Herein we wish to report a distinctive visible light-promoted photocatalytic C-H silylation approach that enables the direct coupling of trialkylhydrosilanes with both electron-deficient and -rich heteroarenes as well as with cyano-substituted arenes in moderate to high yields and with good regioselectivity. The protocol features operational simplicity, mild reaction conditions, and the use of safe and readily available Na2S2O8, bis(trimethylsilyl) peroxide (BTMSPO) or iPr3SiSH as the radical initiators. Notably, the challenging bulky and inert trialkylhydrosilanes, such as (t-butyldimethyl)silane (tBuMe2SiH) and (triisopropyl)silane (iPr3SiH), work smoothly with the protocol. Moreover, despite the higher stability of tBuMe2Si silylation products, our studies revealed their great reactivity and versatility in diverse C-Si-based chem. transformations, providing an operationally simple, low-cost, and environmentally benign synthetic technol. for mol. construction and elaboration.

Chemical Science published new progress about Green chemistry. 20582-55-2 belongs to class thiazole, and the molecular formula is C7H9NO2S, Formula: C7H9NO2S.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Ostrovskii, Vladimir S.; Beletskaya, Irina P.; Titanyuk, Igor D. published the artcile< Trifluoroacetaldehyde N-Tosylhydrazone as a Precursor of Trifluorodiazoethane in Reactions of Insertion into the Heteroatom-Hydrogen Bond>, Synthetic Route of 96-53-7, the main research area is trifluoroacetaldehyde tosylhydrazone trifluorodiazoethane insertion reaction copper catalyst.

Trifluorodiazoethane is a widely explored trifluoroethylating reagent, which is suitable for the preparation of a large number of fluorine-containing organic mols. Nevertheless, CF3CHN2 has some disadvantages, such as volatility, storage instability, toxicity, and explosiveness. Herein, the application of trifluoroacetaldehyde N-tosylhydrazone as a CF3CHN2 precursor capable of generating in situ trifluorodiazoethane under mild basic conditions is reported. Copper-catalyzed P-H, O-H, S-H, and C-H insertion reactions of trifluoroacetaldehyde N-tosylhydrazone revealed its wide applicability in the synthesis of trifluoroethyl-containing substances.

Organic Letters published new progress about Carboxylic acids Role: RCT (Reactant), RACT (Reactant or Reagent). 96-53-7 belongs to class thiazole, and the molecular formula is C3H5NS2, Synthetic Route of 96-53-7.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Vulpetti, Anna; Casale, Elena; Roletto, Fulvia; Amici, Raffaella; Villa, Manuela; Pevarello, Paolo published the artcile< Structure-based drug design to the discovery of new 2-aminothiazole CDK2 inhibitors>, Application of C6H10N2S, the main research area is CDK2 inhibitor aminothiazole drug design crystal structure.

N-(5-Bromo-1,3-thiazol-2-yl)butanamide (compound 1) was found active (IC50 = 808 nM) in a high throughput screening (HTS) for CDK2 inhibitors. By exploiting crystal structures of several complexes between CDK2 and inhibitors and applying structure-based drug design (SBDD), we rapidly discovered a very potent and selective CDK2 inhibitor 4-[(5-isopropyl-1,3-thiazol-2-yl)amino] benzenesulfonamide (compound 4, IC50 = 20 nM). The syntheses, structure-based analog design, kinases inhibition data and x-ray crystallog. structures of CDK2/inhibitor complexes are reported.

Journal of Molecular Graphics & Modelling published new progress about Crystal structure. 101080-15-3 belongs to class thiazole, and the molecular formula is C6H10N2S, Application of C6H10N2S.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Miyamoto, Hidetoshi; Sakumoto, Chihiro; Takekoshi, Eriko; Maeda, Yukiko; Hiramoto, Narumi; Itoh, Takahiro; Kato, Yoshiaki published the artcile< Effective Method To Remove Metal Elements from Pharmaceutical Intermediates with Polychelated Resin Scavenger>, Recommanded Product: Ethyl 4-methylthiazole-5-carboxylate, the main research area is metal palladium catalyst removal pharmaceutical resin.

A catalytic reaction is an important methodol. for the production of pharmaceuticals from the viewpoint of green and sustainable chem. Since elemental impurity levels should be controlled within acceptable limits in API, the development of removal of element is also important as well. The technol. for removal of elements was developed using cost-effective polychelated resin scavenger. The precious elements were removed efficiently by passing through the packed cartridge filled with appropriate scavenger. The feasibility of the scavenger was evaluated, and the application for actual manufacturing process is described. In contrast to another type of immobilized scavengers, polychelated resin scavenger provides an inexpensive method to scavenge several elements.

Organic Process Research & Development published new progress about Activated charcoal Role: NUU (Other Use, Unclassified), USES (Uses). 20582-55-2 belongs to class thiazole, and the molecular formula is C7H9NO2S, Recommanded Product: Ethyl 4-methylthiazole-5-carboxylate.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Xiao, Qiong; Wang, Li-Ping; Jiao, Xiao-Zhen; Liu, Xiao-Yu; Wu, Qian; Xie, Ping published the artcile< Concise total synthesis of largazole>, Recommanded Product: Ethyl 2-(((tert-butoxycarbonyl)amino)methyl)thiazole-4-carboxylate, the main research area is largazole cyclic peptide enantioselective synthesis stereoselective aldol addition; thiazolidinethione chiral auxiliary stereoselective aldol addition largazole enantioselective synthesis; macrolactamization largazole cyclic peptide enantioselective synthesis.

The concise total synthesis of largazole (I) was accomplished. The key step included the use of the Nagao thiazolidinethione auxiliary for a diastereoselective acetate aldol reaction, and it acts as an acylating agent for peptide formation.

Journal of Asian Natural Products Research published new progress about Aldol addition, stereoselective. 96929-05-4 belongs to class thiazole, and the molecular formula is C12H18N2O4S, Recommanded Product: Ethyl 2-(((tert-butoxycarbonyl)amino)methyl)thiazole-4-carboxylate.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Sun, Wencheng; Teng, Qiaoling; Cheng, Dongping; Li, Xiaonian; Xu, Xiaoliang published the artcile< The hydrodebromination of 1,1-dibromoalkenes via visible light catalysis>, Computed Properties of 1003-32-3, the main research area is dibromoalkene preparation iridium photocatalyst diastereoselective hydrodebromination green chem; bromoalkene preparation.

A hydrodebromination reaction of 1,1-dibromoalkenes was established via visible light catalysis. A variety of structurally different vinyl bromides were obtained in moderate to excellent yields.

Tetrahedron Letters published new progress about Aldehydes Role: RCT (Reactant), RACT (Reactant or Reagent). 1003-32-3 belongs to class thiazole, and the molecular formula is C4H3NOS, Computed Properties of 1003-32-3.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Yang, Xingye; Qin, Xiaojun; Ji, Huimin; Du, Lupei; Li, Minyong published the artcile< Constructing firefly luciferin bioluminescence probes for in vivo imaging>, Application of C11H8N2O3S2, the main research area is .

Bioluminescence imaging (BLI) is a widely applied visual approach for real-time detecting many physiol. and pathol. processes in a variety of biol. systems. Based on the caging strategy, lots of bioluminescent probes have been well developed. While the targets react with recognizable groups, caged luciferins liberate luciferase substrates, which react with luciferase generating a bioluminescent response. Among the various bioluminescent systems, the most widely utilized bioluminescent system is the firefly luciferin system. The H and carboxylic acid of luciferin are critically caged sites. The introduced self-immolative linker extends the applications of probes. Firefly luciferin system probes have been successfully applied for analyzing physiol. processes, monitoring the environment, diagnosing diseases, screening candidate drugs, and evaluating the therapeutic effect. Here, we systematically review the general design strategies of firefly luciferin bioluminescence probes and their applications. Bioluminescence probes provide a new approach for facilitating investigation in a diverse range of fields. It inspires us to explore more robust light emission luciferin and novel design strategies to develop bioluminescent probes.

Organic & Biomolecular Chemistry published new progress about 2591-17-5. 2591-17-5 belongs to class thiazole, and the molecular formula is C11H8N2O3S2, Application of C11H8N2O3S2.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Bazhin, Arkadiy A.; Sinisi, Riccardo; De Marchi, Umberto; Hermant, Aurelie; Sambiagio, Nicolas; Maric, Tamara; Budin, Ghyslain; Goun, Elena A. published the artcile< A bioluminescent probe for longitudinal monitoring of mitochondrial membrane potential>, Reference of 2591-17-5, the main research area is bioluminescent probe mitochondria membrane potential.

Mitochondrial membrane potential (ΔΨm) is a universal selective indicator of mitochondrial function and is known to play a central role in many human pathologies, such as diabetes mellitus, cancer and Alzheimer′s and Parkinson′s diseases. Here, the authors report the design, synthesis and several applications of mitochondria-activatable luciferin (MAL), a bioluminescent probe sensitive to ΔΨm, and partially to plasma membrane potential (ΔΨp), for non-invasive, longitudinal monitoring of ΔΨm in vitro and in vivo. The authors applied this new technol. to evaluate the aging-related change of ΔΨm in mice and showed that nicotinamide riboside (NR) reverts aging-related mitochondrial depolarization, revealing another important aspect of the mechanism of action of this potent biomol. In addition, the authors demonstrated application of the MAL probe for studies of brown adipose tissue (BAT) activation and non-invasive in vivo assessment of ΔΨm in animal cancer models, opening exciting opportunities for understanding the underlying mechanisms and for discovery of effective treatments for many human pathologies.

Nature Chemical Biology published new progress about Aging, animal. 2591-17-5 belongs to class thiazole, and the molecular formula is C11H8N2O3S2, Reference of 2591-17-5.

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica