Tag: M.W=200-250

Li, Lin published the artcileDiscovery of novel dual inhibitors of VEGFR and PI3K kinases containing 2-ureidothiazole scaffold, Product Details of C9H11N3O3, the main research area is phenylureidothiazolformamide preparation VEGFR PI3K kinase inhibitory anticancer SAR activity.

A series of compounds possessing 2-(3-phenyl)ureidothiazol-4-formamide derivatives with a 2-ureidothiazole scaffold were designed and synthesized. Some compounds demonstrated inhibition of cell proliferation against both MDA-MB-231 and HepG2 cell lines using Sorafenib as the pos. control. Compounds I showed a good to moderate inhibition on VEGFR-2 and PI3Kα which was proved by further mol. docking study. This study suggests that compound I is a potential dual inhibitor of VEGFR-2 and PI3Kα and is applicable for further investigation.

Chinese Chemical Letters published new progress about Antitumor agents. 26820-62-2 belongs to class pyridine-derivatives, name is 4-(5-Nitropyridin-2-yl)morpholine, and the molecular formula is C9H11N3O3, Product Details of C9H11N3O3.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Wang, Chao-Yu published the artcilePalladium(II) complexes containing a bulky pyridinyl N-heterocyclic carbene ligand: Preparation and reactivity, HPLC of Formula: 89076-64-2, the publication is Journal of Organometallic Chemistry (2007), 692(18), 3976-3983, database is CAplus.

Coordination chem. of a pyridine imidazole-2-ylidene ligand (pyN-C) with sterically hindered substituents toward Pd(II) metal ions was studied. The Pd carbene complex [(C-pyN-C)Pd(η³-allyl)Cl] (3) was prepared via transmetalation from the corresponding Ag carbene complexes with [ClPd(η³-allyl)]₂. Upon the abstraction of chloride, coordination of pyridinyl N becomes feasible to form [C,N-(pyN-C)Pd(η³-allyl)](BF₄) (4). Ligand substitution reaction of 4 with PPh₃ gave [(C-pyN-C)Pd(PPh₃)(η³-allyl)](BF₄), in which the pyridinyl N donor is substituted by the phosphine. This Pd complex appears to be base sensitive. Treatment of 4 with KOCMe₃ causes decomposition to yield metal nanoparticles. Also, decomplexation of 4 takes place under H atm. to generate the carbene precursor, 1-(6-mesityl-2-picolyl)-3-mesitylimidazolium salt. Nevertheless, the Pd complex 4 shows good catalytic activity on the Suzuki-Miyaura and Mizoroki-Heck reactions.

Journal of Organometallic Chemistry published new progress about 89076-64-2. 89076-64-2 belongs to pyridine-derivatives, auxiliary class Pyridine,Nitro Compound,Benzene, name is 5-Nitro-2-phenylpyridine, and the molecular formula is C7H4ClIO2, HPLC of Formula: 89076-64-2.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Tang, Luning published the artcileSelective single C-F bond arylation of trifluoromethylalkene derivatives, Application of (1-(tert-Butoxycarbonyl)-1,2,3,6-tetrahydropyridin-4-yl)boronic acid, the publication is Chemical Science (2019), 10(37), 8701-8705, database is CAplus and MEDLINE.

A strategically novel single C-F bond functionalization of CF₃-derived mols., which shows a prominent advantage for the expedient construction of difluoromethylene-bridged organic scaffolds, is disclosed. The reported protocol consists of S_N2′ amination, N-alkylation and palladium-catalyzed allylic substitution reactions, which enables straightforward arylation and alkenylation of vinyltrifluoromethane derivatives Furthermore, this strategy is characterized by its broad substrate scope with respect to both CF₃-alkene and arylboronic acid derivatives

Chemical Science published new progress about 844501-00-4. 844501-00-4 belongs to pyridine-derivatives, auxiliary class Pyridine,Boronic acid and ester,Amide,Boronic Acids,Boronic acid and ester, name is (1-(tert-Butoxycarbonyl)-1,2,3,6-tetrahydropyridin-4-yl)boronic acid, and the molecular formula is C12H9N3O4, Application of (1-(tert-Butoxycarbonyl)-1,2,3,6-tetrahydropyridin-4-yl)boronic acid.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Popov, V. I. published the artcileNovel syntheses of fluoroferrocene and pentafluoroanisole, Application of 1-Fluoropyridiniumtriflate, the publication is Ukrainskii Khimicheskii Zhurnal (Russian Edition) (1990), 56(10), 1115-16, database is CAplus.

Treating mercurated ferrocene (I; R = HgOAc) (II) or (CF₃CO₂Hg)₅C₆OMe with AcOF in CFCl₃/HOAc gave 42, 29% I (R = F) or C₆F₅OMe, resp. II was also fluorinated in 37% yield by using N-fluoropyridinium trifluoromethanesulfonate.

Ukrainskii Khimicheskii Zhurnal (Russian Edition) published new progress about 107263-95-6. 107263-95-6 belongs to pyridine-derivatives, auxiliary class Fluorination reagent, name is 1-Fluoropyridiniumtriflate, and the molecular formula is C6H5F4NO3S, Application of 1-Fluoropyridiniumtriflate.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Bao, Jiyin published the artcileDiscovery of benzo[d]oxazole derivatives as the potent type-I FLT3-ITD inhibitors, Application of (1-(tert-Butoxycarbonyl)-1,2,3,6-tetrahydropyridin-4-yl)boronic acid, the publication is Bioorganic Chemistry (2020), 103248, database is CAplus and MEDLINE.

A series of compounds I [R¹ = H, Me, F, MeO; R² = diethylamino, piperidinyl, piperazin-1-yl, etc.; R³ = Ph, pyridin-3-yl, pyridin-4-yl, etc.] were designed and synthesized based on benzo[d]oxazole-2-amine scaffold to discover new potent Fms-like tyrosine kinase 3 inhibitors. During the medicinal chem. works, flexible mol. docking was used to provide design rationale and study the binding modes of the target compounds Through the mixed SAR exploration based on the enzymic and cellular activities, compound I [R¹ = MeO; R² = piperazin-1-yl; R³ = 3-carbamoylphenyl] was identified with potent FLT3-ITD inhibitory (IC₅₀: 0.41 nM) and anti-proliferative (IC₅₀: 0.037μM against MV4-11 cells) activities. And the binding mode of I [R¹ = MeO; R² = piperazin-1-yl; R³ = 3-carbamoylphenyl] with ”DFG-in” FLT3 was simulated by a 20-ns mol. dynamics run, providing some insights into further medicinal chem. efforts toward novel FLT3 inhibitors in AML therapy.

Bioorganic Chemistry published new progress about 844501-00-4. 844501-00-4 belongs to pyridine-derivatives, auxiliary class Pyridine,Boronic acid and ester,Amide,Boronic Acids,Boronic acid and ester, name is (1-(tert-Butoxycarbonyl)-1,2,3,6-tetrahydropyridin-4-yl)boronic acid, and the molecular formula is C10H18BNO4, Application of (1-(tert-Butoxycarbonyl)-1,2,3,6-tetrahydropyridin-4-yl)boronic acid.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Ma, Junjie published the artcileNi-Catalyzed C-H Cyanation of (Hetero)arenes with 2-Cyanoisothiazolidine 1,1-Dioxide as a Cyanation Reagent, Name: 5-Nitro-2-phenylpyridine, the publication is Organic Letters (2021), 23(8), 2868-2872, database is CAplus and MEDLINE.

A nickel-catalyzed C-H cyanation reaction of arenes has been developed using 2-cyanoisothiazolidine 1,1-dioxide as an electrophilic cyanation reagent. Many different directing groups can be used in this cyanation to obtain a series of cyanation products with good yields. Adopting this strategy to introduce a cyano group, natural alkaloid menisporphine was successfully synthesized through cyano group conversion that further proved the practicality of this cyanation method.

Organic Letters published new progress about 89076-64-2. 89076-64-2 belongs to pyridine-derivatives, auxiliary class Pyridine,Nitro Compound,Benzene, name is 5-Nitro-2-phenylpyridine, and the molecular formula is C11H8N2O2, Name: 5-Nitro-2-phenylpyridine.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Wang, Xisheng published the artcilePd(II)-catalyzed para-selective C-H arylation of monosubstituted arenes, Formula: C6H5F4NO3S, the publication is Journal of the American Chemical Society (2011), 133(35), 13864-13867, database is CAplus and MEDLINE.

Pd-catalyzed highly para-selective C-H arylation of monosubstituted arenes (including toluene) is developed for the first time using an F⁺ reagent as a bystanding oxidant. This finding provides a new retrosynthetic disconnection for para-substituted biaryl synthesis e. g., I via C-H/C-H cross-coupling.

Journal of the American Chemical Society published new progress about 107263-95-6. 107263-95-6 belongs to pyridine-derivatives, auxiliary class Fluorination reagent, name is 1-Fluoropyridiniumtriflate, and the molecular formula is C3H5BN2O2, Formula: C6H5F4NO3S.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Mu, Bing published the artcilePd-Catalyzed Tandem Cyclization via C-H Arylation and Acylation for the Construction of Polycyclic Scaffolds, Computed Properties of 1174626-28-8, the publication is Organic Letters (2016), 18(20), 5260-5263, database is CAplus and MEDLINE.

The first Pd-catalyzed tandem cyclization of imidazo[1,2-a]pyridines with 2-chlorobenzaldehydes through C-H arylation and acylation is presented for the efficient synthesis of novel 6H-benzo[b]imidazo[5,1,2-de]quinolizin-6-ones. The direct acylation reaction proceeded smoothly without the aid of directing groups and in the presence of air as a clean and free terminal oxidant.

Organic Letters published new progress about 1174626-28-8. 1174626-28-8 belongs to pyridine-derivatives, auxiliary class Pyridine,Amine,Benzene,Ether, name is 2-Amino-6-benzyloxypyridine, and the molecular formula is C12H12N2O, Computed Properties of 1174626-28-8.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Motornov, Vladimir published the artcileCopper(I)-Catalyzed Regioselective Chan-Lam N2-Vinylation of 1,2,3-Triazoles and Tetrazoles, Name: (1-(tert-Butoxycarbonyl)-1,2,3,6-tetrahydropyridin-4-yl)boronic acid, the publication is Advanced Synthesis & Catalysis (2019), 361(14), 3306-3311, database is CAplus.

Copper-catalyzed coupling of π-deficient NH-azoles with vinylboronic acids or vinyltrifluoroborate salt provided a direct route to N2-vinyl-1,2,3-triazoles and N2-vinyltetrazoles. The coupling reaction was efficiently catalyzed by (phen)Cu(PPh₃)Br with low catalyst loading (5 mol%) under base-free conditions. The method was applicable for vinylation of unsubstituted, monosubstituted and disubstituted 1,2,3-triazoles with various functionalities with high N2-selectivity.

Advanced Synthesis & Catalysis published new progress about 844501-00-4. 844501-00-4 belongs to pyridine-derivatives, auxiliary class Pyridine,Boronic acid and ester,Amide,Boronic Acids,Boronic acid and ester, name is (1-(tert-Butoxycarbonyl)-1,2,3,6-tetrahydropyridin-4-yl)boronic acid, and the molecular formula is C10H18BNO4, Name: (1-(tert-Butoxycarbonyl)-1,2,3,6-tetrahydropyridin-4-yl)boronic acid.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Fenger, Isabelle published the artcileReusable polymer-supported palladium catalysts: an alternative to tetrakis(triphenylphosphine)palladium in the Suzuki cross-coupling reaction, Recommanded Product: 5-Nitro-2-phenylpyridine, the publication is Tetrahedron Letters (1998), 39(24), 4287-4290, database is CAplus.

The Suzuki cross-coupling reaction of a boronic acid and a bromoarom. compound requires palladium catalysis. Almost identical yields were obtained under the usual conditions, with 30 mequivalent of Pd(PPh₃)₄, and with 2 mequiv of a polymer-supported catalyst, which was easily prepared in two steps from Merrifield polymer. Recovery and reuse of the catalyst is easy, and only 0.60% of the initial amount of palladium is lost during a reaction.

Tetrahedron Letters published new progress about 89076-64-2. 89076-64-2 belongs to pyridine-derivatives, auxiliary class Pyridine,Nitro Compound,Benzene, name is 5-Nitro-2-phenylpyridine, and the molecular formula is C11H8N2O2, Recommanded Product: 5-Nitro-2-phenylpyridine.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem