Category: 844501-00-4

Gutierrez-Bonet, Alvaro published the artcileAsymmetric Synthesis of Tertiary and Secondary Cyclopropyl Boronates via Cyclopropanation of Enantioenriched Alkenyl Boronic Esters, Computed Properties of 844501-00-4, the publication is Organic Letters (2022), 24(19), 3455-3460, database is CAplus and MEDLINE.

The cyclopropanation of alkenyl boronates and subsequent derivatization of the boronate handle are a convenient strategy to quickly build mol. complexity and access diverse compounds with a high sp³ fraction. Herein, the authors describe the asym. cyclopropanation of enantioenriched hydrobenzoin-derived alkenyl boronic esters toward the synthesis of tertiary and secondary cyclopropyl boronates.

Organic Letters 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, Computed Properties of 844501-00-4.

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

Brem, Jurgen published the artcileImitation of β-lactam binding enables broad-spectrum metallo-β-lactamase inhibitors, Computed Properties of 844501-00-4, the publication is Nature Chemistry (2022), 14(1), 15-24, database is CAplus and MEDLINE.

Carbapenems are vital antibiotics, but their efficacy is increasingly compromised by metallo-β-lactamases (MBLs). Here we report the discovery and optimization of potent broad-spectrum MBL inhibitors. A high-throughput screen for NDM-1 inhibitors identified indole-2-carboxylates (InCs) as potential β-lactamase stable β-lactam mimics. Subsequent structure-activity relationship studies revealed InCs as a new class of potent MBL inhibitor, active against all MBL classes of major clin. relevance. Crystallog. studies revealed a binding mode of the InCs to MBLs that, in some regards, mimics that predicted for intact carbapenems, including with respect to maintenance of the Zn(II)-bound hydroxyl, and in other regards mimics binding observed in MBL-carbapenem product complexes. InCs restore carbapenem activity against multiple drug-resistant Gram-neg. bacteria and have a low frequency of resistance. InCs also have a good in vivo safety profile, and when combined with meropenem show a strong in vivo efficacy in peritonitis and thigh mouse infection models. [graphic not available: see fulltext]

Nature 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, Computed Properties of 844501-00-4.

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

Hong, Junting published the artcileCarboxylation of Alkenyl Boronic Acids and Alkenyl Boronic Acid Pinacol Esters with CO₂ Catalyzed by Cuprous Halide, HPLC of Formula: 844501-00-4, the publication is European Journal of Organic Chemistry (2020), 2020(19), 2813-2818, database is CAplus.

A cuprous halide catalyzed carboxylation of alkenyl boronic acids and alkenyl boronic acid pinacol esters under CO₂, affording the corresponding α,β-unsaturated carboxylic acids in good yield, has been developed. The potassium (E)-trifluoro(styryl)borate is also compatible with this reaction. This simple and efficient copper(I) catalytic system showed good functional group tolerance.

European Journal of Organic 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, HPLC of Formula: 844501-00-4.

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

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

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

Matsuura, Rei published the artcilePalladium(II)-catalyzed γ-selective hydroarylation of alkenyl carbonyl compounds with arylboronic acids, Application of (1-(tert-Butoxycarbonyl)-1,2,3,6-tetrahydropyridin-4-yl)boronic acid, the publication is Chemical Science (2018), 9(44), 8363-8368, database is CAplus and MEDLINE.

A catalytic γ-selective syn-hydroarylation of alkenyl carbonyl compounds using arylboronic acids was developed using a substrate directivity approach with a palladium(II) catalyst. This method tolerated a wide range of functionalized (hetero)arylboronic acids and a variety of substitution patterns on the alkene. Preliminary mechanistic studies suggested that transmetalation is rate-limiting.

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 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

Law, Robert P. published the artcileDiscovery of Tetrahydroquinoxalines as Bromodomain and Extra-Terminal Domain (BET) Inhibitors with Selectivity for the Second Bromodomain, Quality Control of 844501-00-4, the publication is Journal of Medicinal Chemistry (2018), 61(10), 4317-4334, database is CAplus and MEDLINE.

The bromodomain and extra-terminal domain (BET) family of proteins bind acetylated lysine residues on histone proteins. The four BET bromodomains-BRD2, BRD3, BRD4, and BRDT-each contain two bromodomain modules. BET bromodomain inhibition is a potential therapy for various cancers and immunoinflammatory diseases, but few reported inhibitors show selectivity within the BET family. Inhibitors with selectivity for the first or second bromodomain are desired to aid investigation of the biol. function of these domains. Focused library screening identified a series of tetrahydroquinoxalines with selectivity for the second bromodomains of the BET family (BD2). Structure-guided optimization of the template improved potency, selectivity, and physicochem. properties, culminating in potent BET inhibitors with BD2 selectivity.

Journal of Medicinal 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, Quality Control of 844501-00-4.

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