Author: tianli

Sharma, G. M.; Parshad, Baldev; Narang, K. S. published the artcile< Thiazole derivatives. VI. Synthesis of 2-chloro-5-bromothiazoles>, Safety of 5-Bromo-2-chlorothiazole, the main research area is chloro bromo thiazoles; bromo chloro thiazoles; thiazoles chloro bromo.

The title compounds (I) were prepared as follows: ω – thiocyano ketones, NCSCH2C:OR were dissolved in CCl4 or C6H6, depending upon their solubilities, equivalent amounts C5H5N added, and an equivalent amount Br in the same solvent added dropwise at 40-50°. The solvent was distilled in vacuo, the residue treated with H2O to remove C5H5N.HBr, the ω-bromo-ω-thiocyano ketones RCOCH2SCN (II) were collected, washed, and crystallized from EtOH, solutions of II in dry ether saturated with dry HCl gas at 0°, the mixtures kept 12 hrs. at room temperature, the ether was decanted, and the residue purified either by distillation or crystallization to afford 2-chloro-5-bromothiazoles (III). The following II and III were prepared [R, m.p. II, % yield II, m.p. (or b.p./mm.) III, and % yield given]: Ph, 74°, 55.5, (155°/7), 67.6; p-MeC6H4, 94°, 54.5, 64°, 66.03; p-MeOC6H4, 81°, 86.2, 96°, 69.8; p-ClC6H4, 136°, 67.8, 85°, 70.9; p-BrC6H4, 120°, 71.6, 108°, 66.7.

Indian Journal of Chemistry published new progress about Cyclization. 3034-56-8 belongs to class thiazole, and the molecular formula is C3HBrClNS, Safety of 5-Bromo-2-chlorothiazole.

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

Hafez, Ebtissam Abdel Aziz; Abed, Nosrat Mustafa; Elsakka, Ibrahim Ahmed; Elnagdi, Mohamed Hilmy published the artcile< Reactions with heterocyclic diazonium salts. Synthesis of several new azolylhydrazones>, Reference of 72054-60-5, the main research area is azolylhydrazone preparation cyclization; fused azole; thiazolylhydrazone; triazolylhydrazone; thiazolotriazine; pyrazolotriazine.

Several new stable azolylhydrazones, e.g. I and II, were synthesized via coupling of diazotized cyclic amidines with active methylene reagents. The obtained compounds were utilized for synthesis of several, otherwise not readily accessible fused azoles, e.g. III and IV.

Journal of Heterocyclic Chemistry published new progress about Cyclocondensation reaction. 72054-60-5 belongs to class thiazole, and the molecular formula is C7H10N2O2S, Reference of 72054-60-5.

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

Sieng, Bora; Maldonado, Matias Funes; Romagnoli, Carlo; Amedjkouh, Mohamed published the artcile< One-Pot Alkynylation of Azaaryl Aldehydes and Spontaneous Base-Free Rearrangement into Enone Esters: an Autoinductive Mechanism>, Formula: C4H3NOS, the main research area is unsaturated ketoester diastereoselective preparation; butyllithium methylzinc catalyst addition propiolate heteroaryl aldehyde stereoselective rearrangement; isotope labeling allenoate trapping mechanism addition rearrangement propargylic alc.

When heteroaromatic aldehydes are reacted with Et propiolate in the presence of Me2Zn or BuLi, γ-oxo-α,β-unsaturated esters were generated by spontaneous rearrangements of the intermediate propargylic alcs.; in some cases, the propargyl alcs. were formed without rearrangement. The mechanism of the rearrangement was studied using isotope labeling and trapping of a proposed allenoate intermediate; an autocatalytic mechanism is proposed.

European Journal of Organic Chemistry published new progress about Addition reaction. 1003-32-3 belongs to class thiazole, and the molecular formula is C4H3NOS, Formula: C4H3NOS.

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

Kharidia, S. P.; Trivedi, J. J. published the artcile< Synthesis of 3-(substituted benzyl)-5-alkylrhodanines>, Related Products of 10574-69-3, the main research area is .

Preparation of benzylamines and benzylammonium dithiocarbamates (not isolated) and their condensation with α-halo fatty acids were carried out according to Raval and T. (CA 57, 12465h) to give the tabulated I (m.ps. shown). I showed no antifungal, antibacterial, or antiprotozoal activity.

Journal of the Indian Chemical Society 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

Ribeiro, Gabriel H.; Guedes, Adriana P. M.; de Oliveira, Tamires D.; de Correia, Camila R. S. T. b.; Colina-Vegas, Legna; Lima, Mauro A.; Nobrega, Joaquim A.; Cominetti, Marcia R.; Rocha, Fillipe V.; Ferreira, Antonio G.; Castellano, Eduardo E.; Teixeira, Felipe R.; Batista, Alzir A. published the artcile< Ruthenium(II) Phosphine/Mercapto Complexes: Their in Vitro Cytotoxicity Evaluation and Actions as Inhibitors of Topoisomerase and Proteasome Acting as Possible Triggers of Cell Death Induction>, Application In Synthesis of 96-53-7, the main research area is preparation ruthenium diphenylphosphinobutane phosphine diphenylpyridylphosphine thiazolinethiol complex; crystal structure ruthenium diphenylphosphinobutane phosphine diphenylpyridylphosphine thiazolinethiol complex; HSA interaction ruthenium diphenylphosphinobutane phosphine diphenylpyridylphosphine thiazolinethiol complex; cyclic voltammetry ruthenium diphenylphosphinobutane phosphine diphenylpyridylphosphine thiazolinethiol complex; DNA interaction ruthenium diphenylphosphinobutane phosphine diphenylpyridylphosphine thiazolinethiol complex; anticancer activity ruthenium diphenylphosphinobutane phosphine diphenylpyridylphosphine thiazolinethiol complex.

A series of new ruthenium complexes of the general formula [Ru(NS)(dpphpy)(dppb)]PF6 (Ru1-Ru3), where dpphpy = diphenyl-2-pyridylphosphine, NS ligands = 2-thiazoline-2-thiol (tzdt, Ru1, 1), 2-mercaptopyrimidine (pySm, Ru2, 2), and 4,6-diamino-2-mercaptopyrimidine (damp, Ru3, 3), and dppb = 1,4-bis(diphenylphosphino)butane, were synthesized and characterized by elemental anal., spectroscopic techniques (IR, UV/visible, and 1D and 2D NMR), and x-ray diffraction. In the characterization, the correlation between the phosphorus atoms and their resp. aromatic hydrogen atoms of the compounds in the assignment stands outs, by 1H-31P HMBC experiments The compounds show anticancer activities against A549 (lung) and MDA-MB-231 (breast) cancer cell lines, higher than the clin. drug cisplatin. All of the complexes are more cytotoxic against the cancer cell lines than against the MRC-5 (lung) and MCF-10 Å (breast) nontumorigenic human cell lines. For A549 tumor cells, cell cycle anal. upon treatment with Ru2 showed that it inhibits the mitotic phase because arrest was observed in the Sub-G1 phase. Addnl., the compound induces cell death by an apoptotic pathway in a dose-dependent manner, according to annexin V-PE assay. The multitargeted character of the compounds was studied, and the biomols. were DNA, topoisomerase IB, and proteasome, as well as the fundamental biomol. in the pharmacokinetics of drugs, human serum albumin. The complexes do not target DNA in the cells. At low concentrations, the compounds showed the ability to partially inhibit the catalytic activity of topoisomerase IB in the process of relaxation of the DNA plasmid. Among the complexes assayed in cultured cells, complex Ru3 was able to diminish the proteasomal chymotrypsin-like activity to a greater extent. New ruthenium phosphine complexes show anticancer activities against A549 (lung) and MDA-MB-231 (breast) cancer cell lines, higher than the clin. drug cisplatin. For A549 tumor cells, cell cycle anal. upon treatment with Ru2 showed that it inhibits the mitotic phase because arrest was observed in the Sub-G1 phase and induces cell death by an apoptotic pathway. The multitargeted character of the compounds was studied with the biomols. DNA, topoisomerase IB, and proteasome.

Inorganic Chemistry published new progress about Antitumor agents. 96-53-7 belongs to class thiazole, and the molecular formula is C3H5NS2, Application In Synthesis of 96-53-7.

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

Martinez, Ana; Alonso, Mercedes; Castro, Ana; Dorronsoro, Isabel; Gelpi, J. Luis; Luque, F. Javier; Perez, Concepcion; Moreno, Francisco J. published the artcile< SAR and 3D-QSAR Studies on Thiadiazolidinone Derivatives: Exploration of Structural Requirements for Glycogen Synthase Kinase 3 Inhibitors>, Safety of 3-Benzyl-2-thioxothiazolidin-4-one, the main research area is thiadiazolidinone derivative preparation QSAR glycogen synthase kinase 3 inhibitor.

The 2,4-disubstituted thiadiazolidinones (TDZD) are described as the first ATP-noncompetitive GSK-3 inhibitors. Following an SAR study about TDZD, different structural modifications in the heterocyclic ring aimed to test the influence of each heteroatom on the biol. study are here reported here. Various compounds such as hydantoins, dithiazolidindiones, rhodanines, maleimides, and triazoles were synthesized and screened as GSK-3 inhibitors. After an extensive SAR study among these different heterocyclic families, TDZDs have been revealed as a privileged scaffold for the selective inhibition of GSK-3. A Co-MFA anal. was also performed highlighting the mol. electrostatic field interaction in the interaction of TDZDs with GSK-3. Moreover, first mapping studies indicate two binding modes which in turn might imply relevant differences in the mechanism that underly the inhibitory activity of TDZDs.

Journal of Medicinal Chemistry published new progress about Conformation. 10574-69-3 belongs to class thiazole, and the molecular formula is C10H9NOS2, Safety of 3-Benzyl-2-thioxothiazolidin-4-one.

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

Hughes, Rachael A.; Thompson, Stewart P.; Alcaraz, Lilian; Moody, Christopher J. published the artcile< Total Synthesis of the Thiopeptide Antibiotic Amythiamicin D>, SDS of cas: 31825-95-3, the main research area is amythiamicin antibiotic thiopeptide total synthesis; pyridine trisubstituted preparation hetero Diels Alder reaction acetylenamine ethoxyazadiene.

The thiopeptide (or thiostrepton) antibiotics are a class of sulfur containing highly modified cyclic peptides with interesting biol. properties, including reported activity against MRSA and malaria. This work describes the total synthesis of the thiopeptide natural product amythiamicin D (I), and the key step is a biosynthesis-inspired hetero-Diels-Alder route to the pyridine core of the thiopeptide. Preliminary studies using a range of serine-derived 1-ethoxy-2-azadienes established that hetero-Diels-Alder reaction with N-acetylenamines proceeded efficiently under microwave irradiation to give 2,3,6-trisubstituted pyridines. The thiazole building blocks of the antibiotic were obtained by either classical Hantzsch reactions or by dirhodium(II)-catalyzed chemoselective carbene N-H insertion followed by thionation, and were combined to give the bis-thiazole that forms the left-hand fragment of the antibiotic. The key Diels-Alder reaction of a tris-thiazolylazadiene II with benzyl 2-(1-acetylaminoethenyl)thiazole-4-carboxylate gave the core tetrathiazolyl pyridine III, which was elaborated into the natural product by successive incorporation of glycine and bis-thiazole fragments followed by macrocyclization.

Journal of the American Chemical Society published new progress about Cyclic peptides Role: SPN (Synthetic Preparation), PREP (Preparation) (thiopeptides). 31825-95-3 belongs to class thiazole, and the molecular formula is C5H6N2OS, SDS of cas: 31825-95-3.

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

Kim, Jun Hyeok; Bell, Laura J.; Wang, Xiao; Wimalasekera, Rinuckshi; Bastos, Hugo P.; Kelly, Krystyna A.; Hannah, Matthew A.; Webb, Alex A. R. published the artcile< Arabidopsis sirtuins and poly(ADP-ribose) polymerases regulate gene expression in the day but do not affect circadian rhythms>, SDS of cas: 2591-17-5, the main research area is Arabidopsis sirtuin PARP gene expression circadian oscillaton; Arabidopsis thaliana; Nicotinamide-adenine dinucleotide; circadian clock; poly(ADP-ribose) glycohydrolase; poly(ADP-ribose) polymerases; sirtuins.

Nicotinamide-adenine dinucleotide (NAD) is involved in redox homeostasis and acts as a substrate for NADases, including poly(ADP-ribose) polymerases (PARPs) that add poly(ADP-ribose) polymers to proteins and DNA, and sirtuins that deacetylate proteins. Nicotinamide, a byproduct of NADases increases circadian period in both plants and animals. In mammals, the effect of nicotinamide on circadian period might be mediated by the PARPs and sirtuins because they directly bind to core circadian oscillator genes. We have investigated whether PARPs and sirtuins contribute to the regulation of the circadian oscillator in Arabidopsis. We found no evidence that PARPs and sirtuins regulate the circadian oscillator of Arabidopsis or are involved in the response to nicotinamide. RNA-seq anal. indicated that PARPs regulate the expression of only a few genes, including FLOWERING LOCUS C. However, we found profound effects of reduced sirtuin 1 expression on gene expression during the day but not at night, and an embryo lethal phenotype in knockouts. Our results demonstrate that PARPs and sirtuins are not associated with NAD regulation of the circadian oscillator and that sirtuin 1 is associated with daytime regulation of gene expression.

Plant, Cell & Environment published new progress about Arabidopsis. 2591-17-5 belongs to class thiazole, and the molecular formula is C11H8N2O3S2, SDS of cas: 2591-17-5.

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

Masuda, Naoyuki; Yamamoto, Osamu; Fujii, Masahiro; Ohgami, Tetsuro; Moritomo, Ayako; Kontani, Toru; Kageyama, Shunji; Ohta, Mitsuaki published the artcile< Regioselective Alkylation of Thiazolylsulfonamides: Direct and Efficient Synthesis of 3-Alkylthiazolidene Derivatives>, Recommanded Product: 5-Isopropylthiazol-2-amine, the main research area is thiazolylsulfonamide alkyl halide regioselective alkylation; thiazolidene sulfonamide preparation; alkylthiazolidene sulfonamide preparation; sulfonyliminothiazole preparation.

Various N(3)-alkylated thiazolidene sulfonamide derivatives were efficiently prepared by the direct endo-selective alkylation of thiazolyl sulfonamides. The effects of different bases and solvents were investigated, and the NaH-THF combination was found to be the most effective at conferring high yields and endo-selectivity.

Synthetic Communications published new progress about Alkylation, regioselective. 101080-15-3 belongs to class thiazole, and the molecular formula is C6H10N2S, Recommanded Product: 5-Isopropylthiazol-2-amine.

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

Liang, Xiao-Ping; Luo, Min; Kang, Li; Tang, Long-Xing; Liang, Qing; Liu, Yuan-Lin; Yang, Zi; Zhang, Chun-Tao; Peng, Cai-Yun; Fu, Rong-Geng published the artcile< Facile one-pot three-component strategy for the synthesis of 2-amino-4-arylthiazoles via elemental sulfur source>, Application of C9H7N3O2S, the main research area is amino arylthiazole preparation green chem; aryl methyl ketone sulfur cyanamide three component cascade.

A novel and facile metal-free method for the green synthesis of 2-amino-4-arylthiazole derivatives I (Ar = 3-nitrophenyl, 2-naphthyl, pyridin-4-yl, etc.) through the three-component cascade reaction of aromatic Me ketones ArC(O)Me, elemental sulfur and cyanamide is reported. One C-N bond and two C-S bonds were formed in one-pot protocol without using catalysts.

Tetrahedron Letters published new progress about Alkyl aryl ketones Role: RCT (Reactant), RACT (Reactant or Reagent). 57493-24-0 belongs to class thiazole, and the molecular formula is C9H7N3O2S, Application of C9H7N3O2S.

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