Day: October 14, 2022

Pels, Kevin; Dickson, Paige; An, Hongchan; Kodadek, Thomas published the artcile< DNA-Compatible Solid-Phase Combinatorial Synthesis of β-Cyanoacrylamides and Related Electrophiles>, Application of C10H7NOS, the main research area is DNA solid phase combinatorial beta cyanoacrylamide electrophile; DNA; DNA-encoded library; Knoevenagel condensation; combinatorial chemistry; covalent; cyanoacrylamide; one bead one compound library; reversible.

The Knoevenagel condensation can be exploited in combinatorial synthesis on the solid phase. Condensation products from such reactions were structurally characterized, and their Michael reactivity with thiol and phosphine nucleophiles is described. Cyanoacrylamides were previously reported to react reversibly with thiols, and notably, dilution into low pH buffer can trap covalent adducts, which are isolable via chromatog. Finally, the authors synthesized both traditional and DNA-encoded one-bead, one-compound libraries containing cyanoacrylamides as a source of cysteine-reactive reversibly covalent protein ligands.

ACS Combinatorial Science published new progress about Combinatorial library (DNA-encoded). 198904-53-9 belongs to class thiazole, and the molecular formula is C10H7NOS, Application of C10H7NOS.

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

Morales-Nava, Rosmarbel; Fernandez-Zertuche, Mario; Ordonez, Mario published the artcile< Microwave-assisted improved synthesis of oxazolidin-2-ones, oxazolidine-2-thiones and thiazolidine-2-thione chiral auxiliaries>, Product Details of C10H11NS2, the main research area is amino alc carbonate cyclization carbonylation microwave; carbon sulfide amino alc cyclization carbonylation microwave; oxazolidinone chiral auxiliary preparation; oxazolidinethione chiral auxiliary preparation; thiazolidinethione chiral auxiliary preparation.

The synthesis of the target compounds was achieved by a microwave-assisted method and typical 4-substituted oxazolidinone chiral auxiliaries were obtained. Under these conditions, treatment of (S)-phenylalaninol, (S)-phenylglycinol, (S)-valinol, and (1S,2R)-norephedrine with (EtO)2CO or CS2 under the appropriate and specific microwave reaction conditions, led to an efficient synthesis of oxazolidin-2-ones, oxazolidine-2-thiones, and thiazolidine-2-thiones. The methodol. provides these chiral auxiliaries with improved yields and a remarkable reduction in reaction times, particularly in the case of 2-thiazolidinethione derivatives, as compared with the conventional methods.

Molecules published new progress about Amino alcohols, chiral Role: RCT (Reactant), RACT (Reactant or Reagent). 171877-39-7 belongs to class thiazole, and the molecular formula is C10H11NS2, Product Details of C10H11NS2.

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

Kikelj, D.; Urleb, U. published the artcile< Product class 17: thiazoles>, Formula: C7H9NO2S, the main research area is review thiazole preparation.

A review of synthetic methods to prepare thiazoles as well as reactive modifications of thiazole moieties.

Science of Synthesis published new progress about Cyclization. 20582-55-2 belongs to class thiazole, and the molecular formula is C7H9NO2S, Formula: C7H9NO2S.

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

Lohans, Christopher T.; van Belkum, Marco J.; Cochrane, Stephen A.; Huang, Zedu; Sit, Clarissa S.; McMullen, Lynn M.; Vederas, John C. published the artcile< Biochemical, Structural, and Genetic Characterization of Tridecaptin A1, an Antagonist of Campylobacter jejuni>, Recommanded Product: (S)-4-Benzylthiazolidine-2-thione, the main research area is sequence tridecaptin A1 paenicidin B Paenibacillus gene cluster; antimicrobial agents; bacteriocins; lipopeptides; peptides; structure elucidation.

Bacillus circulans NRRL B-30644 (now Paenibacillus terrae) was previously reported to produce SRCAM 1580, a bacteriocin active against the food pathogen Campylobacter jejuni. We have been unable to isolate SRCAM 1580, and did not find any genetic determinants in the genome of this strain. We now report the reassignment of this activity to the lipopeptide tridecaptin A1. Structural characterization of tridecaptin A1 was achieved through NMR, MS/MS and GC-MS studies. The structure was confirmed through the first chem. synthesis of tridecaptin A1, which also revealed the stereochem. of the lipid chain. The impact of this stereochem. on antimicrobial activity was examined The biosynthetic machinery responsible for tridecaptin production was identified through bioinformatic analyses. P. terrae NRRL B-30644 also produces paenicidin B, a novel lantibiotic active against Gram-pos. bacteria. MS/MS analyses indicate that this lantibiotic is structurally similar to paenicidin A.

ChemBioChem published new progress about 16S rRNA Role: BSU (Biological Study, Unclassified), PRP (Properties), BIOL (Biological Study). 171877-39-7 belongs to class thiazole, and the molecular formula is C10H11NS2, Recommanded Product: (S)-4-Benzylthiazolidine-2-thione.

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

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