Category: 64987-16-2

On August 31, 1987, Yoshioka, Mitsuru published an article.Synthetic Route of 64987-16-2 The title of the article was Synthetic studies related to oral β-lactam antibiotics. And the article contained the following:

A review. Review with 10 references on the development of an industrial process for producing 7432-S (I), a new oral cephem in 36-42% overall yields from penicillin G. 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 review cephem 7432 s manufacture, Biomolecules and Their Synthetic Analogs: Reviews and other aspects.Synthetic Route of 64987-16-2

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

On February 18, 1993, Lind, Peter Thomas; Morin, John Michael, Jr.; Noreen, Rolf; Ternansky, Robert John published a patent.Recommanded Product: 64987-16-2 The title of the patent was Thiourea derivatives and methods for inhibition of HIV and related viruses. And the patent contained the following:

A method for the inhibition of the replication of HIV is claimed that comprises contacting HIV with thiourea derivatives Among the specifically claimed compounds is N-[2-(2-pyridyl)ethyl]-N’-(5-bromo-2-pyridyl)thiourea (I). The experimental process involved the reaction of Methyl 2-(2-aminothiazol-4-yl)acetate(cas: 64987-16-2).Recommanded Product: 64987-16-2

The Article related to virucide hiv thiourea preparation, pyridylethyl thiourea preparation virucide hiv, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.Recommanded Product: 64987-16-2

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

Hamashima, Y. published an article in 1989, the title of the article was Synthesis, biological properties, and pharmacokinetics of 7432-S, a new oral cephem.SDS of cas: 64987-16-2 And the article contains the following content:

A number of cephems with ω-carboxyalkenoylamino substituents were prepared and tested for antibacterial activity and oral absorbability. Of these derivatives, the cephem with 7β-(2-(2-amino-4-thiazolyl)-4-carboxy-2-butenoyl)amino] substituent were well absorbed in mice. 7432-S (I) was finally selected as the clin. candidate having antibacterial activity and excellent oral bioavailability. 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 cephem 7432s preparation bactericide pharmacokinetics, Pharmacology: Effects Of Antimicrobials and Parasiticides and other aspects.SDS of cas: 64987-16-2

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

On May 14, 2009, Elleder, Daniel; Young, John A. T.; Baiga, Thomas J.; Noel, Joseph P. published a patent.Related Products of 64987-16-2 The title of the patent was Non-nucleoside reverse transcriptase inhibitors. And the patent contained the following:

Disclosed herein are antiviral agents, in particular non-nucleoside reverse transcriptase inhibitors (NNRTIs). Also disclosed are methods of making the NNRTIs, as well as compositions that include such NNRTIs and methods of their use for treating viral infections, in particular retroviral infections, such as HIV infection. 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 nonnucleoside reverse transcriptase inhibitor viral infection treatment, hiv infection treatment nonnucleoside reverse transcriptase inhibitor, Pharmacology: Effects Of Antimicrobials and Parasiticides and other aspects.Related Products of 64987-16-2

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

On April 10, 2014, Margathe, Jean-Francois; Iturrioz, Xavier; Alvear-Perez, Rodrigo; Marsol, Claire; Riche, Stephanie; Chabane, Hadjila; Tounsi, Nassera; Kuhry, Maxime; Heissler, Denis; Hibert, Marcel; Llorens-Cortes, Catherine; Bonnet, Dominique published an article.Safety of Methyl 2-(2-aminothiazol-4-yl)acetate The title of the article was Structure-Activity Relationship Studies toward the Discovery of Selective Apelin Receptor Agonists. And the article contained the following:

Apelin is the endogenous ligand for the previously orphaned G protein-coupled receptor APJ. Apelin and its receptor are widely distributed in the brain, heart, and vasculature, and are emerging as an important regulator of body fluid homeostasis and cardiovascular functions. To further progress in the pharmacol. and the physiol. role of the apelin receptor, the development of small, bioavailable agonists and antagonists of the apelin receptor, is crucial. In this context, E339-3D6 was described as the first nonpeptidic apelin receptor agonist. The authors show here that 1 is actually a mixture of polymethylated species, and they describe an alternative and versatile solid-phase approach that allows access to highly pure 27, the major component of 1. This approach was also applied to prepare a series of derivatives in order to identify the crucial structural determinants required for the ligand to maintain its affinity for the apelin receptor as well as its capacity to promote apelin receptor signaling and internalization. The study of the structure-activity relationships led to the identification of ligands 19, 21, and 38, which display an increased affinity compared to that of 27. The latter and 19 behave as full agonists with regard to cAMP production and apelin receptor internalization, whereas 21 is a biased agonist toward cAMP production Interestingly, the three ligands display a much higher stability in mouse plasma (T1/2 > 10 h) than the endogenous apelin-17 peptide 2 (T1/2 < 4 min). 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 apelin receptor ligand fluorescent peptide solid phase preparation sar, Amino Acids, Peptides, and Proteins: Poly(Amino Acids) and Peptides and other aspects.Safety of Methyl 2-(2-aminothiazol-4-yl)acetate

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

On November 1, 2001, Lehmann, Thomas; Fischer, Ruediger; Albers, Markus; Roelle, Thomas; Mueller, Gerhard; Hessler, Gerhard; Tajimi, Masaomi; Ziegelbauer, Karl; Okigami, Hiromi; Bacon, Kevin; Hasegawa, Haruki published a patent.Product Details of 64987-16-2 The title of the patent was Preparation of cyclic carboxylic acid peptides as integrin antagonists. And the patent contained the following:

Peptides R6-X-A-N(R5)CR3R4-Y-DR1R2 [R1 represents a 4-9-membered (un)saturated aromatic cyclic residue which can contain 0-3 heteroatoms N, S or O and may be annulated and/or substituted; R2, R3, R4 and R5 represent H or (un)substituted C1-C10 alkyl, C2-C10 alkenyl or alkynyl, C6 or C10 aryl, C3-C7 cycloalkyl or a 4-9-membered (un)saturated heterocyclic residue containing up to 2 atoms O, N or S; R6 represents Ph or a 5- to 6-membered aromatic heterocyclic residue containing up to 3 atoms O, N and S and which may annulated or substituted; A represents CO, COCO, SO, SO2, PO, PO2, 2- or 4-pyrimidyl, 2-pyridyl, 2- or 4-imidazolyl, 2-benzimidazolyl or certain other rings which may be substituted; X represents CRX-1RX-2 (RX-1 and RX-2 are H, C1-C4 alkyl, C2-C4 alkenyl or alkynyl) or together with R6 forms a 4-7-membered ring, which can include up to 2 heteroatoms, up to two double bonds and be substituted; Y represents a bond, CO, SO, SO2, O, S, CRY-1RY-2 or NRY-3, where RY-1, RY-2 or RY-3 are a bond, H, (un)substituted C1-C4 alkyl, C2-C4 alkenyl or alkynyl] and their pharmaceutically acceptable salts were prepared for the treatment of inflammatory diseases. Thus, 2-MeC6H4NHCONH-p-C6H4CH2CO-L-Leu-NHC6H4CO2H-m was prepared and showed IC50 ≤ 0.5 μM in the Jurkat VCAM-1 assay. The experimental process involved the reaction of Methyl 2-(2-aminothiazol-4-yl)acetate(cas: 64987-16-2).Product Details of 64987-16-2

The Article related to cyclic carboxylic acid peptide preparation integrin antagonist inflammation inhibitor, Amino Acids, Peptides, and Proteins: Poly(Amino Acids) and Peptides and other aspects.Product Details of 64987-16-2

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 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 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