thiazole归档 - Page 227 of 974 - Heterocyclic Building Blocks-Thiazole

de Oliveira Lima Filho, Edson’s team published research in ACS Omega in 2020 | CAS: 95-24-9

6-Chlorobenzothiazol-2-ylamine(cas: 95-24-9) belongs to thiazoles. Thiazoles are a class of five-membered rings containing nitrogen and sulfur with excellent antitumor, antiviral and antibiotic activities.Synthetic Route of C7H5ClN2SThe thiazole ring has been identified as a central feature of numerous natural products, perhaps the most famous example of which is epothilone.

de Oliveira Lima Filho, Edson; Malvestiti, Ivani published their research in ACS Omega on December 29 ,2020. The article was titled 《Mechanochemical Thiocyanation of Aryl Compounds via C-H Functionalization》.Synthetic Route of C7H5ClN2S The article contains the following contents:

Aryl thiocyanate compounds are important building blocks for the synthesis of bioactive compounds and intermediates for several functional groups. Reported thiocyanation reactions via C-H functionalization have limited substrate scope and low RME. The ball-milling method reported here uses ammonium persulfate and ammonium thiocyanate as reagents and silica as a grinding auxiliary. It afforded aryl thiocyanates with moderate to excellent yields for a wide variety of aryl compounds (36 examples, 8-96% yield), such as anilines, phenols, anisoles, thioanisole, and indole, thus tolerating substrates with sensitive functional groups. New products such as benzo[d][1,3]oxathiol-2-ones were obtained with C-4 substituted phenols. Thus, to our knowledge, we report, for the first time, aryl thiocyanation reaction by ball-milling at room temperature and solvent-free conditions, with short reaction times and no workup. Anal. of several mass-based green metrics indicates that it is an efficient greener method.6-Chlorobenzothiazol-2-ylamine(cas: 95-24-9Synthetic Route of C7H5ClN2S) was used in this study.

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

Liu, X. W.’s team published research in Asian Journal of Chemistry in 2014 | CAS: 3034-22-8

5-Bromothiazol-2-amine(cas: 3034-22-8) belongs to anime. Left-handed and right-handed forms (mirror-image configurations, known as optical isomers or enantiomers) are possible when all the substituents on the central nitrogen atom are different (i.e., the nitrogen is chiral). With amines, there is extremely rapid inversion in which the two configurations are interconverted.Reference of 5-Bromothiazol-2-amine

In 2014,Liu, X. W.; Zhang, H.; Yang, Y. J.; Li, J. Y.; Li, B.; Zhou, X. Z.; Zhang, J. Y. published 《Synthesis, antibacterial evaluation and molecular docking study of nitazoxanide analogues》.Asian Journal of Chemistry published the findings.Reference of 5-Bromothiazol-2-amine The information in the text is summarized as follows:

A series of nitazoxanide analogs I, II (R = 2,4-F2, 3,4-F2, 2-CF3, 4-CF3; X = NO2, Cl, Br) were synthesized. The antibacterial activities of synthesized compounds against Clostridium difficile were evaluated and I (R = 4-CF3) was the most promising compound The preliminary results showed that compounds containing nitro-substituted thiazole ring displayed notable activities. Compounds with thiazole moiety replaced by a pyrimidine ring exhibited moderate activities. Mol. docking study of nitazoxanide and I (R = 4-CF3) with pyruvate ferredoxin oxidoreductase suggested that the nitro group interacts with thiamine pyrophosphate and surrounding amino acids, which were almost same compared with pyruvate. The results revealed that nitazoxanide may be a competitive inhibitor of pyruvate and nitro-group is necessary for thiazolide’s activities against anaerobic organisms containing pyruvate ferredoxin oxidoreductase enzyme. In the experiment, the researchers used many compounds, for example, 5-Bromothiazol-2-amine(cas: 3034-22-8Reference of 5-Bromothiazol-2-amine)

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

Okumura, Kazuro’s team published research in Bulletin of the Chemical Society of Japan in 1996-08-31 | 96929-05-4

Bulletin of the Chemical Society of Japan published new progress about Peptide analogs Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 96929-05-4 belongs to class thiazole, and the molecular formula is C12H18N2O4S, Recommanded Product: Ethyl 2-(((tert-butoxycarbonyl)amino)methyl)thiazole-4-carboxylate.

Okumura, Kazuro; Ito, Akio; Saito, Hiroyuki; Nakamura, Yutaka; Shin, Chung-gi published the artcile< Dehydrooligopeptides. XIV. Syntheses of 2-[(Z)-1-aminoalken-1-yl]oxazole-4-carboxylic acid and the main common skeleton of thiostrepton peptide antibiotics A10255G and A10255J.>, Recommanded Product: Ethyl 2-(((tert-butoxycarbonyl)amino)methyl)thiazole-4-carboxylate, the main research area is dehydrooligopeptide preparation thiostrepton peptide antibiotic intermediate.

Precursor (I) to title cyclopeptide antibiotics (II; R = Q1, Q2) is constructed from novel 2-[(Z)-1-amino-1-propen-1-yl]oxazole-4-carboxylic acids (III; R1 = Me, Me2CH, Ph; R2 = H, Me) and 2-(1-aminomethyl)- and 2[(S)-1-aminoethyl]thiazole-4-carboxylic acid residues.

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

Crimmins, Michael T’s team published research in Synlett in 2012-06-18 | 171877-39-7

Synlett published new progress about Aldehydes Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 171877-39-7 belongs to class thiazole, and the molecular formula is C10H11NS2, Computed Properties of 171877-39-7.

Crimmins, Michael T.; Azman, Adam M. published the artcile< A modular, stereoselective approach to spiroketal synthesis>, Computed Properties of 171877-39-7, the main research area is modular stereoselective synthesis spiroketal milbemycin fragment.

A highly convergent and flexible synthetic approach to stereochem. defined spiroketals is reported. Substituents can be incorporated at various positions around the spiroketal framework without significant disruption to the synthetic scheme. The approach has been exploited to prepare the spiroketal fragment of milbemycin β14.

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

Nicolaou, K C’s team published research in Journal of the American Chemical Society in 2008-07-30 | 31825-95-3

Journal of the American Chemical Society published new progress about Antitumor agents. 31825-95-3 belongs to class thiazole, and the molecular formula is C5H6N2OS, Product Details of C5H6N2OS.

Nicolaou, K. C.; Leung, Gulice Y. C.; Dethe, Dattatraya H.; Guduru, Ramakrishna; Sun, Ya-Ping; Lim, Chek Shik; Chen, David Y.-K. published the artcile< Chemical Synthesis and Biological Evaluation of Palmerolide A Analogues>, Product Details of C5H6N2OS, the main research area is palmerolide A analog preparation antitumor.

Mol. design and chem. synthesis of several palmerolide A analogs allowed the first structure activity relationships (SARs) of this newly discovered marine antitumor agent. From several analogs synthesized and tested, compounds I (with a Ph substituent on the side chain) and II (lacking the C-7 hydroxyl group) were the most interesting, exhibiting approx. a 10-fold increase in potency and equipotency, resp., to the natural product. These findings point the way to more focused structure activity relationship studies.

Journal of the American Chemical Society published new progress about Antitumor agents. 31825-95-3 belongs to class thiazole, and the molecular formula is C5H6N2OS, Product Details of C5H6N2OS.

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

Pena, Stella’s team published research in Bioorganic & Medicinal Chemistry Letters in 2012-08-01 | 96929-05-4

Bioorganic & Medicinal Chemistry Letters published new progress about Antimalarials. 96929-05-4 belongs to class thiazole, and the molecular formula is C12H18N2O4S, Category: thiazole.

Pena, Stella; Scarone, Laura; Manta, Eduardo; Stewart, Lindsay; Yardley, Vanessa; Croft, Simon; Serra, Gloria published the artcile< Synthesis of a Microcystis aeruginosa predicted metabolite with antimalarial activity>, Category: thiazole, the main research area is peptidomimetic synthesis Microcystis aeruginosa metabolite antimalarial agent; peptide coupling oxazole thiazole macrocyclization.

The synthesis of a Microcystis aeruginosa predicted metabolite analog of aerucyclamide B was performed. This hexacyclopeptide was obtained from three heterocyclic building blocks by a convergent macrocycle-assembly methodol. The compound exhibited good in vitro antiplasmodial activity (IC50: 0.18μM, K1, chloroquine-resistant strain).

Bioorganic & Medicinal Chemistry Letters published new progress about Antimalarials. 96929-05-4 belongs to class thiazole, and the molecular formula is C12H18N2O4S, Category: thiazole.

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

Michaelis, Lars’s team published research in Synlett in 2014 | 171877-39-7

Synlett published new progress about Antibacterial agents. 171877-39-7 belongs to class thiazole, and the molecular formula is C10H11NS2, Application In Synthesis of 171877-39-7.

Michaelis, Lars; Schinzer, Dieter published the artcile< Studies toward the total synthesis of sorangicins: a shortened synthesis of the dioxabicyclo[3.2.1]octane core>, Application In Synthesis of 171877-39-7, the main research area is sorangicin preparation antibiotic antibacterial agent.

An access to the dioxabicyclo[3.2.1]octane core of 6-methyl-8-(3,3a,8,9,10,11,12,13,14,15,18,19,22,23,25,26,28,34a-octadecahydro-11,14,15-trihydroxy-10,38-dimethyl-28-oxo-9,13-epoxy-23,26-etheno-2,5-methano-2H,5H-furo[2,3-l][1,4,14]trioxacyclotritriacontin-25-yl)-7-nonenoic acid [i.e., (+)-sorangicin A] was developed, using a keto lactone formation, a Mukaiyama-Michael reaction and an epoxide opening as the key steps. The synthesis of the target compound was achieved using (4S)-4-(phenylmethyl)-2-thiazolidinethione as a chiral auxiliary. The title compound thus formed was (8E)-2,5:3,7-dianhydro-4,6,8,9-tetradeoxy-6-methyl-9-phenyl-L-glycero-L-gluco-non-8-enitol, (8E)-2,5:3,7-dianhydro-4,6,8,9-tetradeoxy-6-methyl-9-phenyl-L-glycero-L-gluco-non-8-enose.

Synlett published new progress about Antibacterial agents. 171877-39-7 belongs to class thiazole, and the molecular formula is C10H11NS2, Application In Synthesis of 171877-39-7.

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

Nagase, Hiroshi’s team published research in Chemical & Pharmaceutical Bulletin in 1973 | 10574-69-3

Chemical & Pharmaceutical Bulletin published new progress about 10574-69-3. 10574-69-3 belongs to class thiazole, and the molecular formula is C10H9NOS2, Safety of 3-Benzyl-2-thioxothiazolidin-4-one.

Nagase, Hiroshi published the artcile< Fungicides. XXII. Reaction of dimethyl acetylenedicarboxylate with dithiocarbamates, thiolcarbamates, thiosemicarbazides, and thiosemicarbazones>, Safety of 3-Benzyl-2-thioxothiazolidin-4-one, the main research area is acetylenedicarboxylate reaction; thiocarbamate reaction acetylenedicarboxylate; thiosemicarbazide reaction acetylenedicarboxylate; thiosemicarbazone reaction acetylenedicarboxylate; thiazolidone.

Dimethyl acetylenedicarboxylate reacted readily with dithiocarbamates, thiolcarbamates, thiosemicarbazides, and thiosemicarbazones to give 4-thiazolidones [I, R = H, alkyl, PhCH2, NH2; X = S (II), O NR1 (R1 = Me, Ph, substituted-methyleneamino)]. The exo double bond of 4-thiazolidones (II) was highly reactive to dithiocarbamates to give 2,2′-dithioxo-5,5′-bi-4-thiazolidones, which were autoxidized to 2,2′-dithioxo-Δ5,5′-bi-4-thiazolidones in the presence of catalytic amount of amines.

Chemical & Pharmaceutical Bulletin published new progress about 10574-69-3. 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

Rezania, Jafar’s team published research in Journal of Molecular Structure in 2018-06-05 | 57493-24-0

Journal of Molecular Structure published new progress about Alkyl aryl ketones Role: PRP (Properties), RCT (Reactant), RACT (Reactant or Reagent). 57493-24-0 belongs to class thiazole, and the molecular formula is C9H7N3O2S, Recommanded Product: 2-Amino-4-(3-nitrophenyl)thiazole.

Rezania, Jafar; Behzadi, Hadi; Shockravi, Abbas; Ehsani, Morteza; Akbarzadeh, Elahe published the artcile< Corrigendum to ""Synthesis and DFT calculations of some 2-aminothiazoles"" [J. Mol. Struct. 1157 (5) (April 2018) 300-305] [Erratum to document cited in CA168:135942]>, Recommanded Product: 2-Amino-4-(3-nitrophenyl)thiazole, the main research area is aminothiazole preparation green chem DFT calculation erratum; ketone aryl thiourea cyclization iodine catalyst erratum.

In the original publication, there are errors in the affiliations section; the correction is provided here.

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

Ormond, Alexandra B’s team published research in Dyes and Pigments in 2013-02-28 | 1003-32-3

Dyes and Pigments published new progress about Excited singlet state. 1003-32-3 belongs to class thiazole, and the molecular formula is C4H3NOS, Product Details of C4H3NOS.

Ormond, Alexandra B.; Freeman, Harold S. published the artcile< Effects of substituents on the photophysical properties of symmetrical porphyrins>, Product Details of C4H3NOS, the main research area is singlet oxygen generation sym porphyrin photosensitizer; substituent effect photophys sym porphyrin derivative.

Porphyrin compounds having groups that mimic the phenolic moiety of m- and p-isomers of 5,10,15,20-tetrakis(hydroxyphenyl) porphyrin (THPP) have been synthesized along with 5,10,15,20-tetrakis(heteroaryl) porphyrins bearing 2-thienyl and 5-thiazolyl groups. Absorption and fluorescence spectroscopy, including fluorescence lifetime (τf) and quantum yield (Φf) measurements, were employed to characterize the singlet excited state of all compounds, using 5,10,15,20-tetraphenylporphyrin (H2TPP) as a standard (Φf = 0.12 in DMF). The generation of singlet oxygen by each porphyrin photosensitizer was measured as the singlet oxygen quantum yield (ΦΔ), using H2TPP as a standard (ΦΔ = 0.64 in DMF). Partition coefficients were determined using 2-octanol as the organic phase and PBS solution as the aqueous phase. Fluorescence quantum yields ranged from 0.01 to 0.18 for all compounds, with heteroaryl porphyrins having the lowest values. Singlet oxygen quantum yields ranged from 0.40 to 0.65, with heteroaryl porphyrins having the highest values, showing them to be better sensitizers than m- and p-THPP. Log P values were all >1 showing higher solubility in the 2-octanol layer.

Dyes and Pigments published new progress about Excited singlet state. 1003-32-3 belongs to class thiazole, and the molecular formula is C4H3NOS, Product Details of C4H3NOS.

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