Tag: 100-200

On June 15, 1983, Kamiya, Takashi published a patent.Synthetic Route of 64987-16-2 The title of the patent was Thiazole derivatives. And the patent contained the following:

The title compds I and II (R = COCO2H; R1 = protected amino, alkylamino; R2 = H, halo) were prepared Thus, 14 g I (R = 4-EtO2CCH2, R1 = 2-NH2, R2 = H) was acylated with EtCMe2O2CCl to give 12 g III (R3 = CH2CO2Et). This (0.3 g) was oxidized with SeO2 to give 0.22 g III (R3 = COCO2Et), which (2.8 g) was saponified to give 1.75 g III (R3 = COCO2H). I and II are intermediates in preparation of antibiotic 3-cephem-4-carboxylic acid derivatives The experimental process involved the reaction of Methyl 2-(2-aminothiazol-4-yl)acetate(cas: 64987-16-2).Synthetic Route of 64987-16-2

The Article related to aminothiazoleglycolate, thiazoleglycolate amino, thiazoleacetate amino oxo, cephalosporin intermediate aminothiazoleglycolate, Biomolecules and Their Synthetic Analogs: Beta-Lactam Fungal Metabolites and other aspects.Synthetic Route of 64987-16-2

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

On February 7, 2013, Baloglu, Erkan; Ghosh, Shomir; Lobera, Mercedes; Schmidt, Darby R. published a patent.Quality Control of Methyl 2-(2-aminothiazol-4-yl)acetate The title of the patent was Preparation of substituted phenylacetamides as novel retinoid-related orphan receptor gamma (RORγ) modulators. And the patent contained the following:

The title compounds I [m = 0-2; n = 1-3; X1-X5 = N, N(O), CH, CR5; one of Y1 and Y2 = O or NR8 and the other is bond; or X1 = CR5, Y1 = NR8, Y2 = a bond, and R5 and R8, taken together with the atoms to which they are attached, form (un)substituted 5-7 membered ring, optionally containing an addnl. heteroatom selected from O, N and S; Cy = (un)substituted cycloalkyl, hetreocycloalkyl, Ph or 5-6 membered heteroaryl; Z = O, S, SO2, C(O), NR6, a bond; A1-A5 = N, N(O), CH, CR10; R1 = alkyl, haloalkyl, cycloalkyl, etc.; R2 = H, alkyl, haloalkyl; or R1 and R2 taken together with the carbon atom to which they are attached form (un)substituted 3-8 membered ring, optionally containing a heteroatom selected from O, N, and S; R3 and R31 = H, OH, alkyl, etc.; R4 = H, halo, alkyl, etc.; R41 = H, halo, OH, NH2, alkyl; or R4 and R41 taken together with the carbon atom to which they are attached form (un)substituted 3-8 membered ring, optionally containing a heteroatom selected from O, N, and S; R5 = alkyl, haloalkyl, cycloalkyl, etc.; R6 = H, alkyl, haloalkyl, etc.; R8 = H, alkyl, haloalkyl; R10 = alkyl, haloalkyl, cycloalkyl, etc.; with the provisos], useful as novel retinoid-related orphan receptor gamma (RORγ) modulators in the treatment of diseases mediated by RORγ, were prepared E.g., a multi-step synthesis of II, starting from 2-chloro-4-methylbenzonitrile and phenylmagnesium bromide, was described. Exemplified compounds I were tested in the dual FRET assay and were found to have a pIC50 between 5 and 9. Pharmaceutical composition comprising the compound I was disclosed. The experimental process involved the reaction of Methyl 2-(2-aminothiazol-4-yl)acetate(cas: 64987-16-2).Quality Control of Methyl 2-(2-aminothiazol-4-yl)acetate

The Article related to phenylacetamide preparation retinoid related orphan receptor gamma rorgamma modulator, Heterocyclic Compounds (More Than One Hetero Atom): Oxazoles, Isoxazoles and other aspects.Quality Control of Methyl 2-(2-aminothiazol-4-yl)acetate

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

On August 24, 1999, Hirota, Yoshihiro; Matsunaga, Tomonori published a patent.Name: Methyl 2-(2-aminothiazol-4-yl)acetate The title of the patent was Preparation of chloroacetylamino thiazoleacetic acid ester derivatives. And the patent contained the following:

The title cephalosporin intermediates of formula I [X = alkyl, aralkyl; Y = H2, O, alkoxyimino, carbalkoxy-alkoxyimino] are prepared Thus, chloroacetyl chloride was added slowly to Et 2-(2-aminothiazol-4-yl)-2(Z)-methoxyiminoacetate and propylene oxide acid capture agent in THF to give II in 84% yield. The experimental process involved the reaction of Methyl 2-(2-aminothiazol-4-yl)acetate(cas: 64987-16-2).Name: Methyl 2-(2-aminothiazol-4-yl)acetate

The Article related to thiazoleacetic acid ester chloroacetylamino preparation cephalosporin intermediate, Biomolecules and Their Synthetic Analogs: Beta-Lactam Fungal Metabolites and other aspects.Name: Methyl 2-(2-aminothiazol-4-yl)acetate

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

On May 26, 1983, Kinast, Guenther published a patent.Safety of Methyl 2-(2-aminothiazol-4-yl)acetate The title of the patent was Intermediates useful in the preparation of cephalosporins. And the patent contained the following:

Thiazolines I [R = protective group; R1, R2 = (un)substituted alkyl, cycloalkyl, aryl, heterocyclic], useful as intermediates for cephalosporins II [R3 = (un)substituted alkyl, cycloalkyl, aryl, heterocyclic; R4 = appropriate substituent], were prepared Thus Et 2-amino-4-thiazolylacetate was treated with (Me3CO2C)2O to give I (R = Me3CO2C, R1 = CMe3, R2 = Et) which was treated with MeCHO to give III. Saponification of III to the acid, successive reaction with MeSO2Cl and 7-aminocephalosporanic acid, and deblocking gave II (R3 = Me, R4 = CH2OAc). The experimental process involved the reaction of Methyl 2-(2-aminothiazol-4-yl)acetate(cas: 64987-16-2).Safety of Methyl 2-(2-aminothiazol-4-yl)acetate

The Article related to aminothiazolylalkenamidocephem, cephem aminothiazolylalkenamido, Biomolecules and Their Synthetic Analogs: Beta-Lactam Fungal Metabolites and other aspects.Safety of Methyl 2-(2-aminothiazol-4-yl)acetate

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

On May 5, 2021, Chen, Jin-Ping; Battini, Narsaiah; Ansari, Mohammad Fawad; Zhou, Cheng-He published an article.Application of 24295-03-2 The title of the article was Membrane active 7-thiazoxime quinolones as novel DNA binding agents to decrease the genes expression and exert potent anti-methicillin-resistant Staphylococcus aureus activity. And the article contained the following:

A novel class of 7-thiazoxime quinolones was developed as potential antimicrobial agents for the sake of bypassing resistance of quinolones. Biol. assays revealed that some constructed 7-thiazoxime quinolones possessed effective antibacterial efficiency. Me acetate oxime derivative I exhibited 32-fold more active than ciprofloxacin against MRSA, which also possessed rapidly bactericidal ability and low toxicity towards mammalian cells. The combination use of 7-thiazoxime quinolone I and ciprofloxacin was able to improve antibacterial potency and effectively alleviate bacterial resistance. The preliminarily mechanism exploration revealed that compound I could destroy the cell membrane and insert into MRSA DNA to bind with DNA gyrase, then decrease the expression of gyrB and femB genes. The above results strongly suggested that Me acetate oxime derivative I held a promise for combating MRSA infection. The experimental process involved the reaction of 2-Acetylthiazole(cas: 24295-03-2).Application of 24295-03-2

The Article related to membrane active thiazoxime quinolone preparation mrsa antibacterial dna binding, cell membrane, drug-resistance, gene, mrsa dna, quinolone, Heterocyclic Compounds (One Hetero Atom): Quinolines and Isoquinolines and other aspects.Application of 24295-03-2

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

On May 31, 2020, Hussein, Essam M.; Al-Rooqi, Munirah M.; Elkhawaga, Amal A.; Ahmed, Saleh A. published an article.Reference of 4-Phenylthiazol-2-amine The title of the article was Tailoring of novel biologically active molecules based on N4-substituted sulfonamides bearing thiazole moiety exhibiting unique multi-addressable biological potentials. And the article contained the following:

In the present study, a new series of 2-(4-substituted-thiazol-2-ylamino)acetamides and N-(4-substituted-thiazol-2-yl)acetamides incorporating sulfonamide moieties I (R = H, 4-bromophenyl, pyren-1-yl, etc.; R1 = CH2C(O), C(O)CH2; X = CH2, O) was designed, synthesized, well-characterized and successfully evaluated for their antimicrobial activity against multidrug resistant strains and screened for cytotoxic activity against normal lung fibroblast (WI-38), human lung carcinoma (A549), and human breast carcinoma (MDA-MB-231) cell lines. Fluorescence-activated cell sorting (FACS) anal. and mol. modeling study were performed to identify the mode of action of the novel synthesized compounds and their binding interactions with the active sites of dihydrofolate reductase enzyme (DHFR). The experimental process involved the reaction of 4-Phenylthiazol-2-amine(cas: 2010-06-2).Reference of 4-Phenylthiazol-2-amine

The Article related to acetamide aminothiazolyl sulfonyl preparation docking antibacterial antifungal antitumor activity, Heterocyclic Compounds (More Than One Hetero Atom): Thiazoles, Isothiazoles and other aspects.Reference of 4-Phenylthiazol-2-amine

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

On January 31, 2021, Zhang, Qian; Wu, Jiefei; Pan, Zexi; Zhang, Wen; Zhou, Wei published an article.Quality Control of 4-Phenylthiazol-2-amine The title of the article was A one-pot synthesis of 2-aminothiazoles via the coupling of ketones and thiourea using I2/dimethyl sulfoxide as a catalytic oxidative system. And the article contained the following:

A series of 2-aminothiazoles was prepared in moderate-to-good yields by the direct coupling of ketones and thiourea using I2/dimethyl sulfoxide as a catalytic oxidative system. This method avoids the preparation of lachrymatory and toxic α-haloketones and the use of an acid-binding agent, thus provided a more convenient approach to 2-aminothiazoles compared to the Hantzsch reaction. The experimental process involved the reaction of 4-Phenylthiazol-2-amine(cas: 2010-06-2).Quality Control of 4-Phenylthiazol-2-amine

The Article related to ketone thiourea iodine catalyst dimethyl sulfoxide oxidative coupling, aminothiazole preparation, Heterocyclic Compounds (More Than One Hetero Atom): Thiazoles, Isothiazoles and other aspects.Quality Control of 4-Phenylthiazol-2-amine

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

On February 15, 2007, Srinivas, Akella Satya Surya Visweswara; Mathiyazhagan, Kasinathan; Sharada, Duddu Savaraiah; Ponpandian, Thanasekaran; Revathy, Kulasekharan; Reddy, Gaddam Om; Kamaraj, Mani; Rajagopal, Sriram published a patent.Name: Methyl 2-(2-aminothiazol-4-yl)acetate The title of the patent was Preparation of heterocyclic compounds as inhibitors of histone deacetylase for treatment of cancer. And the patent contained the following:

The title heterocyclic compounds with general formula of A-(CH2)m-O-C(=X)-NH-(CH2)n-E-(CH2)p-C(=Y)-N(R1)R2 [wherein A and E = independently (hetero)aryl, arylalkyl, or benzo-fused heteroaryl, etc.; X and Y = independently O, S, or (un)substituted NH; R1 and R2 = independently H, OH, alkoxy, arylalkyl, etc.; or R1 and R2 form a ring; m, n, and p = independently 0-2], or derivatives, analogs, stereoisomers, and pharmaceutically acceptable salts thereof were prepared as inhibitors of histone deacetylase (HDAC) for treatment of cancer. For example, I was prepared in a multi-step synthesis. I showed inhibitory activity with IC50 of 0.021 μM against HDAC. The experimental process involved the reaction of Methyl 2-(2-aminothiazol-4-yl)acetate(cas: 64987-16-2).Name: Methyl 2-(2-aminothiazol-4-yl)acetate

The Article related to preparation heterocyclic compound thiazole inhibitor histone deacetylase treatment cancer, Heterocyclic Compounds (More Than One Hetero Atom): Thiazoles, Isothiazoles and other aspects.Name: Methyl 2-(2-aminothiazol-4-yl)acetate

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

On June 5, 2019, Zarnegar, Zohre; Shokrani, Zahra; Safari, Javad published an article.HPLC of Formula: 2010-06-2 The title of the article was Asparagine functionalized Al2O3 nanoparticle as a superior heterogeneous organocatalyst in the synthesis of 2-aminothiazoles. And the article contained the following:

Asparagine functionalized aluminum oxide nanoparticles (Asp-Al2O3) have been prepared by a two-step procedure involving the grafting of Al2O3 with 3-chloropropyltrimethoxysilane (CPTMS) and subsequent organofunctionalization using asparagine amino acid. It is shown that Asp-Al2O3 exhibits as an active nanocatalyst for the preparation of 2-aminothiazoles is achieved by one-pot reaction of methylcarbonyls, thiourea and iodine. The structure of Asp-Al2O3 was characterized by fourier transform IR radiation (FT-TR), thermal gravimetric anal. (TGA), X-ray diffraction (XRD), scanning electron microscopic (SEM), and energy-dispersive anal. of X-ray (EDAX) analyses. Advantages of this modified methodol. include higher purity and excellent yield of products, greener and cleaner conditions, easy isolation of products and convenient manipulation. Moreover, immobilization of organocatalysts on the Al2O3 surface are stable under the catalytic reaction conditions resulting their efficient reuse. The experimental process involved the reaction of 4-Phenylthiazol-2-amine(cas: 2010-06-2).HPLC of Formula: 2010-06-2

The Article related to asparagine aluminum oxide nanoparticle preparation, aminothiazole preparation green chem, Heterocyclic Compounds (More Than One Hetero Atom): Thiazoles, Isothiazoles and other aspects.HPLC of Formula: 2010-06-2

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

On December 31, 2012, Zhang, Lei; Chen, Xiaojie; Liu, Jun; Zhu, Qingzhang; Leng, Ying; Luo, Xiaomin; Jiang, Hualiang; Liu, Hong published an article.SDS of cas: 64987-16-2 The title of the article was Discovery of novel dual-action antidiabetic agents that inhibit glycogen phosphorylase and activate glucokinase. And the article contained the following:

Dual-target-directed agents simultaneously inhibiting glycogen phosphorylase (GP) and activating glucokinase (GK) could decelerate the inflow of glucose from glycogenolysis and accelerate the outflow of glucose in the liver, and therefore allow for better control over hyperglycemia in a synergetic manner. A series of hybrid compounds were designed by structure-assisted and ligand-based strategies. In vitro bioassays found two novel compounds I and II worthy of further optimization on balance of dual action to GP and GK. In addition, for single-target activity, two compounds exhibited more potent GP inhibitory activity and four compounds showed better GK activation than their corresponding references The experimental process involved the reaction of Methyl 2-(2-aminothiazol-4-yl)acetate(cas: 64987-16-2).SDS of cas: 64987-16-2

The Article related to heteroaryl amide preparation glycogen phosphorylase inhibition glucokinase activation, Heterocyclic Compounds (More Than One Hetero Atom): Thiazoles, Isothiazoles and other aspects.SDS of cas: 64987-16-2

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