Day: November 3, 2022

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 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 June 28, 2011, Biedermann, Frank; Appel, Eric A.; del Barrio, Jesus; Gruendling, Till; Barner-Kowollik, Christopher; Scherman, Oren A. published an article.Product Details of 92-36-4 The title of the article was Postpolymerization Modification of Hydroxyl-Functionalized Polymers with Isocyanates. And the article contained the following:

The postpolymn. functionalization of hydroxyl-group terminated polymers (Mn in the range of 1000-6000 g mol-1) such as poly(ethylene glycol) (PEG), poly(N-isopropylacrylamide) (PNIPAM), poly(N,N-dimethylacrylamide) (PDMAM), and poly(tert-Bu acrylate) (PtBA) with a wide range of functional isocyanate derivatives such as azobenzene, viologen, and anthracene was studied. It was shown by 1H and 13C NMR, GPC, Fourier transform IR spectroscopy (FTIR), and electrospray ionization mass spectrometry (ESI-MS) that a high degree of end-group conversion, typically >98%, with little or no formation of side products can be achieved at ambient temperature PNIPAM, PDMAM, PtBA, and PHEAM polymers were obtained by reversible addition-fragmentation chain transfer (RAFT) radical polymerization from a hydroxyl-group containing chain transfer agent (CTA). The formation of the carbamate was compatible with the trithiocarbonate end-group of the RAFT polymers. Addnl., this approach allows for the direct functionalization of RAFT polymers without the need of addnl. steps such as deprotection or aminolysis of the CTA. This route was subsequently used for the preparation of a variety of side-chain functional polymers from poly(N-hydroxyethyl acrylamide) (PHEAM). Three different high yielding methods were employed to prepare the isocyanates (R-NCO). Either amino or carboxylic acid precursors were converted into the desired R-NCO or hydroxyl group moieties were reacted with an excess of 1,6-hexamethylene diisocyanate (HDI) to statistically form the monofunctional product. The experimental process involved the reaction of 2-(4-Aminophenyl)-6-methylbenzothiazole(cas: 92-36-4).Product Details of 92-36-4

The Article related to postpolymn modification hydroxyl functionalized polymer isocyanate carbamate, Chemistry of Synthetic High Polymers: Chemical Transformation Of Polymers and other aspects.Product Details of 92-36-4

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

On February 28, 2022, Kalhor, Mehdi; Zarnegar, Zohre published an article.Quality Control of 4-Phenylthiazol-2-amine The title of the article was 1-Methylimidazolium ionic liquid supported on Ni@zeolite-Y: fabrication and performance as a novel multi-functional nanocatalyst for one-pot synthesis of 2-aminothiazoles and 2-aryl benzimidazoles. And the article contained the following:

In the present study, 1-methyl-3-(3-trimethoxysilylpropyl)-1H-imidazol-3-ium chloride-supported Ni@zeolite-Y-based nanoporous materials (Ni@zeolite-Im-IL) were synthesized and their structures were confirmed using different characterization techniques such as FT-IR, FE-SEM, EDX, XRD, BET and TGA-DTG analyses. In order to synthesize this multi-functional nano-system, zeolite-NaY was modified first, with exchanged Ni2+ ions and 3-chloropropyltriethoxysilane (CPTES) as a coupling reagent and then functionalized to imidazolium chloride ionic liquid by N-methylimidazole. New multi-functional nano-material of Ni@zeolite-Im-IL demonstrated high activity in the catalytic synthesis of 2-aminothiazoles 3a-l by one-pot reaction of methylcarbonyls, thiourea and iodine at 80°C in DMSO with good to excellent yields (85-98%). Also, the catalytic synthesis of 2-aryl benzimidazoles, 6a-m was performed by the condensational reaction of o-arylendiamine and aromatic aldehydes in EtOH at room temperature with excellent yields (90-98%). Advantages of this efficient synthetic strategy include higher purity and shorter reaction time, excellent yield, easy isolation of products, the good stability, activity and feasible reusability of the metallic ionic liquid nanocatalyst. These benefits have made this method more compatible with the principles of green chem. 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 methylimidazolium ionic liquid supported nickel zeolitey nanocatalyst synthesis fabrication, Catalysis, Reaction Kinetics, and Inorganic Reaction Mechanisms: Catalysts and other aspects.Quality Control of 4-Phenylthiazol-2-amine

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

On January 9, 2020, Franch, Luigi; Ghosh, Shomir; Glick, Gary; Katz, Jason; Opipari, Anthony William, Jr.; Roush, William R.; Seidel, Hans Martin; Shen, Dong-Ming; Venkatraman, Shankar; Winkler, David Guenther published a patent.Related Products of 64987-16-2 The title of the patent was Heteroaryl compounds as NLRP modulators and their preparation. And the patent contained the following:

The invention relates to heteroaryl compounds of formula I, or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable salt thereof, and are useful to treat connected to the modulation of NLRP3. Compounds of formula I wherein n is 0 and 1; o is 0, 1, 2 and 3; q is 1 and 2; A and E are independently 5- to 10-membered heteroaryl and C6-10 aryl; R1a is (un)substituted C1-6 alkyl and SONH2 and derivatives; R1b is substituted C1-6 alkyl, SO2NH2 and derivatives, OH and derivatives, etc.; R2 is C1-6 alkyl, C1-6 haloalkyl, C1-6 alkoxy, etc.; R6 and R7 are independently C1-6 alkyl, C1-6 alkoxy, halo, CN, NO2, etc.; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by amidation of 2,2,2-trichloroethyl N-[2-azatricyclo[7.3.0.0[3,7]]dodeca-1,3(7),8-trien-8-yl]carbamate with 3-(hydroxymethyl)-N1-methylbenzene-1,4-disulfonamide. The invention compounds were evaluated for their NLRP3 modulatory activity. From the assay, it was determined that compound II exhibited IC50 value in the range of ≥ 0.2μM to < 1μM. The experimental process involved the reaction of Methyl 2-(2-aminothiazol-4-yl)acetate(cas: 64987-16-2).Related Products of 64987-16-2

The Article related to heteroaryl preparation nlrp3 modulator, Heterocyclic Compounds (More Than One Hetero Atom): Thiazoles, Isothiazoles and other aspects.Related Products of 64987-16-2

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

On January 9, 2020, Glick, Gary; Roush, William; Venkatraman, Shankar; Shen, Dong-Ming; Ghosh, Shomir; Seidel, Hans Martin; Franchi, Luigi; Winkler, David Guenther; Opipari, Anthony William, Jr.; Katz, Jason published a patent.Safety of Methyl 2-(2-aminothiazol-4-yl)acetate The title of the patent was Aryl and heteroaryl compounds as NLRP modulators and their preparation. And the patent contained the following:

The invention relates to heteroaryl compounds of formula I, or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable salt thereof, and are useful to treat connected to the modulation of NLRP3. Compounds of formula I wherein n is 0 and 1; o is 0, 1, 2 and 3; q is 1 and 2; A and E are independently 5- to 10-membered heteroaryl and C6-10 aryl; R1a is (un)substituted C1-6 alkyl, SONR11R12 and CR11R12NR11R12; R1b is substituted C1-6 alkyl, SO2NH2 and derivatives, OH and derivatives, etc.; R2 is C1-6 alkyl, C1-6 haloalkyl, C1-6 alkoxy, etc.; R6 and R7 are independently C1-6 alkyl, C1-6 alkoxy, halo, CN, NO2, etc.; R11 and R12 are independently H and (un)substituted C1-6 alkyl; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by chlorination of 2-[4-[(cyclopentyloxy)methyl]-2,6-bis(propan-2-yl)phenyl]acetic acid; the resulting 2-[4-[(cyclopentyloxy)methyl]-2,6-bis(propan-2-yl)phenyl]acetyl chloride underwent amidation with 3-(hydroxymethyl)-N1-methylbenzene-1,4-disulfonamide to give compound II. The invention compounds were evaluated for their NLRP3 modulatory activity. From the assay, it was determined that compound II exhibited IC50 value in the range of ≥ 0.04μM to < 0.2μM. 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 heteroaryl preparation nlrp3 modulator, Heterocyclic Compounds (More Than One Hetero Atom): Thiazoles, Isothiazoles and other aspects.Safety of Methyl 2-(2-aminothiazol-4-yl)acetate

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

Koppireddi, Satish; Komsani, Jayaram Reddy; Tiwari, Ashok K.; Ali, Amtul Z.; Yadla, Rambabu published an article in 2014, the title of the article was Synthesis and biological evaluation of new derivatives of tertiary thiazolamines.Quality Control of 2-Amino-4-(4-iodophenyl)thiazole And the article contains the following content:

A series of new 4-(substituted phenyl)-N,N-bis(4-(trifluoromethyl)benzyl)thiazol-2-amines I (R = C6H5, 4-ClC6H4, 4-BrC6H4, 4-IC6H4, etc.) and 4-(4-chlorophenyl)-N,N-bis(4-methoxybenzyl)thiazol-2-amines II have been synthesized. Compound I (R = 2-FC6H4) has shown promising α-glucosidase inhibitory activity, while compound I (R = H) and II (R = 4-MeOC6H4) have displayed significant anticancer potential against neuroblastoma cells. Some of the targets have shown promising α-glucosidase inhibitory and anticancer activity. The experimental process involved the reaction of 2-Amino-4-(4-iodophenyl)thiazole(cas: 31699-14-6).Quality Control of 2-Amino-4-(4-iodophenyl)thiazole

The Article related to tertiary thiazolamine preparation anticancer, Heterocyclic Compounds (More Than One Hetero Atom): Thiazoles, Isothiazoles and other aspects.Quality Control of 2-Amino-4-(4-iodophenyl)thiazole

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

On January 24, 1985, there was a patent about blood platelet.Application of 64987-16-2 The title of the patent was Alkyl 2-substituted amino-4-thiazolylacetates. And the patent contained the following:

The title esters I [R, R1 = 5-(1-imidazolyl)pentyl, Me; cyclohexylamino, Me; EtNH, Et] were prepared by reaction of II with the corresponding carboxylic acids or isocyanates. I had platelet aggregation inhibitory activity at 5-25 mg/kg-day. Thus, a mixture of 6-(1-imidazolyl)hexanoic acid 0.9, 1-hydroxybenzotriazole 0.7, and DCC 1 g in DMF was stirred 30 min at 40-50°, 0.9 g II (R1 = Me) in DMF added, and the whole stirred 1 h at 40-50% to give I [R = 5-(1-imidazolyl)pentyl, R1 = Me]. The experimental process involved the reaction of Methyl 2-(2-aminothiazol-4-yl)acetate(cas: 64987-16-2).Application of 64987-16-2

The Article related to aminothiazolylacetate blood platelet aggregation, Heterocyclic Compounds (More Than One Hetero Atom): Thiazoles, Isothiazoles and other aspects.Application of 64987-16-2

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

On July 21, 2005, Murray, Anthony; Lau, Jesper; Jeppesen, Lone; Vedso, Per; Ankersen, Michael; Lundbeck, Jane Marie; Kristiansen, Marit; Valcarce-Lopez, Maria Carmen; Polisetti, Dharma Rao; Subramanian, Govindan; Andrews, Robert Carl; Christen, Daniel P.; Cooper, Jeremy T.; Santhosh, Kalpathy Chidambareswaran published a patent.Safety of Ethyl 2-((2-aminothiazol-5-yl)thio)acetate The title of the patent was Preparation of heteroaryl ureas and their use as glucokinase activators. And the patent contained the following:

Title compounds I [wherein R1, R2 = (un)substituted cycloalk(en)yl, heterocyclyl or heterocycloalkenyl; A = (un)substituted heteroaryl, or pharmaceutically acceptable salts, stereoisomers and tautomers thereof] were prepared For example, treatment of 2-aminothiazole with carbonyldiimidazole followed by condensation with dicyclohexylamine gave urea II. The invented compounds are activators of glucokinase, and thus may be useful for the management, treatment, control, or adjunct treatment of diseases, where increasing glucokinase activity is beneficial (no data). The experimental process involved the reaction of Ethyl 2-((2-aminothiazol-5-yl)thio)acetate(cas: 859522-19-3).Safety of Ethyl 2-((2-aminothiazol-5-yl)thio)acetate

The Article related to urea heteroaryl preparation glucokinase activator, Heterocyclic Compounds (More Than One Hetero Atom): Thiazoles, Isothiazoles and other aspects.Safety of Ethyl 2-((2-aminothiazol-5-yl)thio)acetate

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

On May 21, 2008, Zhao, Hongfu; Liu, Gang; Zheng, Gengxiu; Sun, Bin; Guo, Fangshui; Wang, Guangzheng published a patent.Electric Literature of 64987-16-2 The title of the patent was Method for preparing 2-(2-butoxycarbonylaminothiazol-4-yl)-2-pentenoate. And the patent contained the following:

The title method comprises: (1) carrying out reaction of alkyl 2-(2-aminothiazol-4-yl)acetate 1.0 mol and di-tert-Bu dicarbonate 1.0-1.5 mol in the presence of 4-N,N-dimethylaminopyridine as catalyst at 0-80°C to obtain alkyl 2-(2-butoxycarbonylaminothiazol-4-yl)acetate, and (2) cooling alkyl 2-(2-butoxycarbonylaminothiazol-4-yl)acetate to -60-0°C, adding alkali, adding propionaldehyde, heating to room temperature, and carrying out reaction to obtain the final product. The method has the advantages of shortening reaction time, reducing usage of di-tert-Bu dicarbonate, and enhancing yield. The experimental process involved the reaction of Methyl 2-(2-aminothiazol-4-yl)acetate(cas: 64987-16-2).Electric Literature of 64987-16-2

The Article related to aminothiazolylpentenoate butoxycarbonyl preparation, Heterocyclic Compounds (More Than One Hetero Atom): Thiazoles, Isothiazoles and other aspects.Electric Literature of 64987-16-2

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