Day: February 23, 2023

Bulky Yet Flexible Pd-PEPPSI-IPent^An for the Synthesis of Sterically Hindered Biaryls in Air was written by Lu, Dong-Dong;He, Xu-Xian;Liu, Feng-Shou. And the article was included in Journal of Organic Chemistry in 2017.Recommanded Product: 615-20-3 This article mentions the following:

In this report, a type of moisture and air stable Pd-PEPPSI-IPent^An complex with the combination of acenaphthyl on the backbone and isopentyl groups on N-aryl moieties, I, was described and applied in the Suzuki-Miyaura cross-coupling reaction in air. The reaction conditions were optimized, and the structure-reactivity relationships between I and other classical efficient Pd-PEPPSI complexes were investigated intensively. Our study demonstrated that both the backbone and N-aryl moieties gave rise to a significant effect on this transformation when exposed to air. A wide range of sterically hindered (hetero)aryl chlorides with (hetero)arylboronic acids were compatible, giving good to excellent isolated yields of sterically hindered bi(hetero)aryls. In the experiment, the researchers used many compounds, for example, 2-Chlorobenzothiazole (cas: 615-20-3Recommanded Product: 615-20-3).

2-Chlorobenzothiazole (cas: 615-20-3) belongs to thiazole derivatives. Thiazoles in peptides or their ability to bind proteins, DNA and RNA has led to many synthetic studies and new applications. Various laboratory methods exist for the organic synthesis of thiazoles. Prominent is the Hantzsch thiazole synthesis is a reaction between haloketones and thioamides.Recommanded Product: 615-20-3

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

Ruthenium silicate (RS-1) zeolite: novel heterogeneous efficient catalyst for synthesis of 2-arylbenzothiazole derivatives was written by Gadekar, Sachin P.;Lande, Machhindra K.. And the article was included in Research on Chemical Intermediates in 2021.Recommanded Product: 2-(4-Methylphenyl)benzothiazole This article mentions the following:

Mesoporous silicate and transition metal (Ru⁺³) containing mesoporous silicate materials or ruthenium silicate Ru⁺³/Si⁺⁴ where synthesis by using hydrothermal process. Mesoporous ruthenium silicate (RS-1) and zeolite catalyst have been successfully synthesized with variable molar ratio such as (a) Ru:Si 1:100, (b) Ru:Si 1:150, (c) Ru:Si 1:200. The elemental composition, structural morphol., crystal phase and properties and various parameters of the catalyst were examined by Fourier transform IR spectroscopy, SEM, powder X-ray diffraction. Energy dispersive X-ray pattern/spectroscopy anal. EDX/EDS, where as the activity of obtained catalysts was tested in the Willgerodt-Kindler synthesis between 2-aminothiophenol and substituted aryl aldehyde (1:1 mol) to form a 2-arylbenzothiazole. The novelty of the presented work was the ruthenium (Ru⁺³) metal impregnations in silicate framework for the synthesis of novel ruthenium silicate (RS-1) zeolite as a catalyst and the investigation of the various parameters, role, its stability and catalytic activity in the Willgerodt-Kindler (combined both Knovenagel and Maichel addition reaction) synthesis. The developed protocol has several benefits such as short reaction time, mild reaction condition, and good reusability of catalyst. Graphic abstract: [graphic not available: see fulltext]. In the experiment, the researchers used many compounds, for example, 2-(4-Methylphenyl)benzothiazole (cas: 16112-21-3Recommanded Product: 2-(4-Methylphenyl)benzothiazole).

2-(4-Methylphenyl)benzothiazole (cas: 16112-21-3) belongs to thiazole derivatives. Thiazole is a five-membered, unsaturated, planar, π-excessive heteroaromatic containing one sulfur atom and one pyridine-type nitrogen atom at position 3 of the cyclic ring system. Electrophilic attack at nitrogen depends on the presence of electron density at nitrogen as well as the position and nature of substituent linked to the thiazole ring.Recommanded Product: 2-(4-Methylphenyl)benzothiazole

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

Pharmacokinetics and mechanism of renal excretion of short acting sulfonamides and N₄-acetylsulfonamide derivatives in man. Structural requirements of sulfonamides for active tubular secretion was written by Vree, T. B.;Hekster, Y. A.;Damsma, J. E.;Tijhuis, M.;Friesen, W. T.. And the article was included in European Journal of Clinical Pharmacology in 1981.Computed Properties of C11H11N3O3S2 This article mentions the following:

The pharmacokinetics of short acting sulfonamides and a series of N₄-acetylsulfonamides was investigated. Sulfonamides with a S atom 2 at. bond distances from the N¹-atom are excreted by active tubular secretion, e.g. sulfamethizole  [144-82-1], sulfaethidole  [94-19-9], and sulfathiazole  [72-14-0]. When the S atom is replaced by an O or N, active renal excretion no longer occurs. N⁴-Acetylsulfonamides are excreted by active tubular secretion. The renal clearance value of the N⁴-acetylsulfonamides are not influenced by the substituent at the N¹ position. Two groups of N⁴-acetylsulfonamides can be distinguished. One has a T_1/2 of 4-6 h and a renal clearance value of 20-60 mL/min and the second has a T_1/2 of 10-20 h and a renal clearance of <10 mL/min. N⁴-Acetylsulfonamides are deacetylated ∼5%. In the experiment, the researchers used many compounds, for example, N-(4-(N-(Thiazol-2-yl)sulfamoyl)phenyl)acetamide (cas: 127-76-4Computed Properties of C11H11N3O3S2).

N-(4-(N-(Thiazol-2-yl)sulfamoyl)phenyl)acetamide (cas: 127-76-4) belongs to thiazole derivatives. Thiazoles in peptides or their ability to bind proteins, DNA and RNA has led to many synthetic studies and new applications. Electrophilic attack at nitrogen depends on the presence of electron density at nitrogen as well as the position and nature of substituent linked to the thiazole ring.Computed Properties of C11H11N3O3S2

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

1-Piperazinylphthalazines as potential VEGFR-2 inhibitors and anticancer agents: Synthesis and in vitro biological evaluation was written by Abou-Seri, Sahar M.;Eldehna, Wagdy M.;Ali, Mamdouh M.;Abou El Ella, Dalal A.. And the article was included in European Journal of Medicinal Chemistry in 2016.Recommanded Product: 2103-99-3 This article mentions the following:

In our endeavor towards the development of effective VEGFR-2 inhibitors, three novel series of phthalazine derivatives based on 1-piperazinyl-4-arylphthalazine scaffold were synthesized. All the newly prepared phthalazines were evaluated in vitro for their inhibitory activity against VEGFR-2. In particular, compounds I and II potently inhibited VEGFR-2 at sub-micromolar IC₅₀ values 0.35 ± 0.03 and 0.40 ± 0.04 μM, resp. Moreover, seventeen selected compounds were evaluated for their in vitro anticancer activity according to US-NCI protocol, where compounds I and II proved to be the most potent anticancer agents. While, compound I exhibited potent broad spectrum anticancer activity with full panel GI₅₀ (MG-MID) value of 3.62 μM, compound II showed high selectivity toward leukemia and prostate cancer subpanels [subpanel GI₅₀ (MG-MID) 3.51 and 5.15 μM, resp.]. Mol. docking of compounds I and II into VEGFR-2 active site was performed to explore their potential binding mode. In the experiment, the researchers used many compounds, for example, 4-(4-Chlorophenyl)thiazol-2-amine (cas: 2103-99-3Recommanded Product: 2103-99-3).

4-(4-Chlorophenyl)thiazol-2-amine (cas: 2103-99-3) belongs to thiazole derivatives. The thiazole ring is notable as a component of the vitamin thiamine (B1). There are numerous natural products that possess a thiazole ring with broad pharmacological activities. Thiamine, also known as vitamin B1, possesses a thiazole ring linked with 2-methylpyrimidine-4-amine as hydrochloride salt.Recommanded Product: 2103-99-3

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