Category: 197958-29-5

Hao, Cheng Yi published the artcileCarbonylative coupling of aryl tosylates/triflates with arylboronic acids under CO atmosphere, Synthetic Route of 197958-29-5, the publication is RSC Advances (2016), 6(89), 86502-86509, database is CAplus.

The carbonylative Suzuki-Miyaura reaction between aryl tosylates/triflates with arylboronic acid was reported, using base-free conditions and a balloon pressure of carbon monoxide. Under these conditions, unsym. biaryl ketones were obtained in modest to excellent yields. This method was adapted to the synthesis of oxybenzone and ketoprofen in good yields under mild conditions.

RSC Advances published new progress about 197958-29-5. 197958-29-5 belongs to pyridine-derivatives, auxiliary class Pyridine,Boronic acid and ester, name is 2-Pyridinylboronic acid, and the molecular formula is C5H6BNO2, Synthetic Route of 197958-29-5.

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

Degnan, Andrew P. published the artcileBiaryls as potent, tunable dual neurokinin 1 receptor antagonists and serotonin transporter inhibitors, Safety of 2-Pyridinylboronic acid, the publication is Bioorganic & Medicinal Chemistry Letters (2015), 25(15), 3039-3043, database is CAplus and MEDLINE.

Depression is a serious illness that affects millions of patients. Current treatments are associated with a number of undesirable side effects. Neurokinin 1 receptor (NK₁R) antagonists have recently been shown to potentiate the antidepressant effects of serotonin-selective reuptake inhibitors (SSRIs) in a number of animal models. Herein we describe the optimization of a biaryl chemotype to provide a series of potent dual NK₁R antagonists/serotonin transporter (SERT) inhibitors. Through the choice of appropriate substituents, the SERT/NK₁R ratio could be tuned to afford a range of target selectivity profiles. This effort culminated in the identification of an analog that demonstrated oral bioavailability, favorable brain uptake, and efficacy in the gerbil foot tap model. Ex vivo occupancy studies with compound 58 demonstrated the ability to maintain NK₁ receptor saturation (>88% occupancy) while titrating the desired level of SERT occupancy (11-84%) via dose selection.

Bioorganic & Medicinal Chemistry Letters published new progress about 197958-29-5. 197958-29-5 belongs to pyridine-derivatives, auxiliary class Pyridine,Boronic acid and ester, name is 2-Pyridinylboronic acid, and the molecular formula is C5H6BNO2, Safety of 2-Pyridinylboronic acid.

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

Wang, Tao published the artcileDiscovery of the Human Immunodeficiency Virus Type 1 (HIV-1) Attachment Inhibitor Temsavir and Its Phosphonooxymethyl Prodrug Fostemsavir, Synthetic Route of 197958-29-5, the publication is Journal of Medicinal Chemistry (2018), 61(14), 6308-6327, database is CAplus and MEDLINE.

The optimization of the 4-methoxy-6-azaindole series of HIV-1 attachment inhibitors (AIs) that originated with 1 to deliver temsavir (3, BMS-626529) is described. The most beneficial increases in potency and pharmacokinetic (PK) properties were attained by incorporating N-linked, sp²-hybridized heteroaryl rings at the 7-position of the heterocyclic nucleus. Compounds that adhered to a coplanarity model afforded targeted antiviral potency, leading to the identification of 3 with characteristics that provided for targeted exposure and PK properties in three preclin. species. However, the phys. properties of 3 limited plasma exposure at higher doses, both in preclin. studies and in clin. trials as the result of dissolution- and/or solubility-limited absorption, a deficiency addressed by the preparation of the phosphonooxymethyl prodrug 4 (BMS-663068, fostemsavir). An extended-release formulation of 4 is currently in phase III clin. trials where it has shown promise as part of a drug combination therapy in highly treatment-experienced HIV-1 infected patients.

Journal of Medicinal Chemistry published new progress about 197958-29-5. 197958-29-5 belongs to pyridine-derivatives, auxiliary class Pyridine,Boronic acid and ester, name is 2-Pyridinylboronic acid, and the molecular formula is C11H15NO2, Synthetic Route of 197958-29-5.

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

Zhuang, Linghang published the artcileDiscovery of BI 135585, an in vivo efficacious oxazinanone-based 11β hydroxysteroid dehydrogenase type 1 inhibitor, Formula: C5H6BNO2, the publication is Bioorganic & Medicinal Chemistry (2017), 25(14), 3649-3657, database is CAplus and MEDLINE.

A potent, in vivo efficacious 11β hydroxysteroid dehydrogenase type 1 (11β HSD1) inhibitor (I) has been identified. Compound I inhibited 11β HSD1 activity in human adipocytes with an IC₅₀ of 4.3 nM and in primary human adipose tissue with an IC₈₀ of 53 nM. Oral administration of I to cynomolgus monkey inhibited 11β HSD1 activity in adipose tissue. Compound I exhibited >1000× selectivity over other hydroxysteroid dehydrogenases, displays desirable pharmacodynamic properties and entered human clin. trials in 2011.

Bioorganic & Medicinal Chemistry published new progress about 197958-29-5. 197958-29-5 belongs to pyridine-derivatives, auxiliary class Pyridine,Boronic acid and ester, name is 2-Pyridinylboronic acid, and the molecular formula is C12H16O3, Formula: C5H6BNO2.

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

Chang, Sheng published the artcilePd-Catalyzed desulfitative reaction of aryltrifluoroborates with sodium arenesulfinates in water, Application of 2-Pyridinylboronic acid, the publication is Applied Organometallic Chemistry (2018), 32(1), n/a, database is CAplus.

An efficient procedure for the synthesis of biaryls was catalyzed by Pd(CH₃CN)₄(BF₄)₂ is reported. This Pd-catalyzed cross-coupling reaction of aryltrifluoroborates with sodium arenesulfinates was developed under mild and environmentally benign conditions, in water without any ligand or additive. The reaction gave a range of structurally diverse unsym. bi-aryl mols. with excellent yields, in which the byproduct was sulfur dioxide. It is worth noting that this protocol is also applicable to many heterocyclic aromatics such as thiophene, furan, pyridine, quinoline, isoquinoline and indole.

Applied Organometallic Chemistry published new progress about 197958-29-5. 197958-29-5 belongs to pyridine-derivatives, auxiliary class Pyridine,Boronic acid and ester, name is 2-Pyridinylboronic acid, and the molecular formula is C5H6BNO2, Application of 2-Pyridinylboronic acid.

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

Devarajan, Nainamalai published the artcileCopper-catalyzed oxidative coupling of arylboronic acids with aryl carboxylic acids: Cu₃(BTC)₂ MOF as a sustainable catalyst to access aryl esters, Application In Synthesis of 197958-29-5, the publication is Organic Chemistry Frontiers (2018), 5(15), 2322-2331, database is CAplus.

A convenient and sustainable method was demonstrated for the oxidative coupling of arylboronic acids with aryl carboxylic acids via C-O cross-coupling reaction catalyzed by the unsaturated coordination sites of copper present in the Cu₃(BTC)₂ MOF. Cu₃(BTC)₂ was employed in a MOF-based catalysis reaction with high efficiency and high chemoselectivity without the use of any external oxidants, ligands or additives. The present methodol. avoided stoichiometric reagents and special reaction conditions and showed excellent functional group tolerance with decent to excellent yields of aryl esters R¹C(O)OR² [R¹ = Ph, 4-ClC₆H₄, 2-naphthyl, etc.; R² = Me, 3-MeOC₆H₄, 4-O₂NC₆H₄, etc.]. The catalyst was found to exhibit high stability and reusability, without loss in activity even after several cycles, which was evident from the FT-IR, PXRD and SEM characterizations of the reused catalyst.

Organic Chemistry Frontiers published new progress about 197958-29-5. 197958-29-5 belongs to pyridine-derivatives, auxiliary class Pyridine,Boronic acid and ester, name is 2-Pyridinylboronic acid, and the molecular formula is C5H6BNO2, Application In Synthesis of 197958-29-5.

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

Tsukada, Tomoharu published the artcileStructure-based drug design of tricyclic 8H-indeno[1,2-d][1,3]thiazoles as potent FBPase inhibitors, SDS of cas: 197958-29-5, the publication is Bioorganic & Medicinal Chemistry Letters (2010), 20(3), 1004-1007, database is CAplus and MEDLINE.

With the goal of improving metabolic stability and further enhancing FBPase inhibitory activity, a series of tricyclic 8H-indeno[1,2-d][1,3]thiazoles was designed and synthesized with the aid of structure-based drug design. Extensive SAR studies led to the discovery of 19a (I) with an IC₅₀ value of 1 nM against human FBPase. X-ray crystallog. studies revealed that high affinity of 19a was due to the hydrophobic interaction arising from better shape complementarity and to the hydrogen bonding network involving the side chain on the tricyclic scaffold.

Bioorganic & Medicinal Chemistry Letters published new progress about 197958-29-5. 197958-29-5 belongs to pyridine-derivatives, auxiliary class Pyridine,Boronic acid and ester, name is 2-Pyridinylboronic acid, and the molecular formula is C2H8Cl2N4S2, SDS of cas: 197958-29-5.

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

Eisenmann, Michael published the artcileStructure-based optimization of aldose reductase inhibitors originating from virtual screening, Recommanded Product: 2-Pyridinylboronic acid, the publication is ChemMedChem (2009), 4(5), 809-819, database is CAplus and MEDLINE.

Virtual screening discovered two prospective hits as potential leads for aldose reductase inhibition. Based on their crystal structures with the enzyme, a systematic optimization has been performed to reveal a first structure-activity relationship. A central thiophen moiety and a terminal nitro group exhibit the best binding properties. Diabetes mellitus is a universal health problem. The World Health Organization (WHO) estimates that 150 million people suffer from diabetes mellitus worldwide in 2005. Long-term complications are a serious problem in the treatment of diabetes, manifesting in macrovascular and microvascular complications. Sorbitol accumulation has been proposed to be an important factor in the development of microvascular complications such as nephropathy, neuropathy, retinopathy or cataract. Catalyzing the NADPH-dependent reduction of glucose to sorbitol, aldose reductase (ALR2) is an important target in the prevention of these complications. The development of novel aldose reductase inhibitors is expected to benefit strongly from a structure-based design approach. A virtual screening based on the ultrahigh-resolution crystal structure of the inhibitor IDD 594 in complex with human ALR2 identified two compounds with IC₅₀ values in the low micro- to submicromolar range. Based on the known interactions between the ligands and their binding pocket, we simplified the lead structures to give the minimal structural requirements and developed synthetic pathways from com. available compounds The newly synthesized compounds were assayed for their inhibition of ALR2, showing inhibitory activities down to the nanomolar range. Crystal structure anal. of the most potent derivative of our series revealed insights into the binding mode of the inhibitors.

ChemMedChem published new progress about 197958-29-5. 197958-29-5 belongs to pyridine-derivatives, auxiliary class Pyridine,Boronic acid and ester, name is 2-Pyridinylboronic acid, and the molecular formula is C5H6BNO2, Recommanded Product: 2-Pyridinylboronic acid.

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

Xu, Yuqin published the artcileThe Chan-Evans-Lam N-arylation of phosphonic/phosphinic amides, Synthetic Route of 197958-29-5, the publication is Tetrahedron (2017), 73(31), 4602-4609, database is CAplus.

A stoichiometric copper(II)-mediated arylation protocol of phosphinamides and phosphonamides was herein demonstrated. Various unreported N-aryl phosphinamides and phosphonamides were successfully prepared through Chan-Evans-Lam reaction with high efficiency (up to 88% yields) and good functional groups tolerance (30 examples) in the absence of any ligands or co-catalysts.

Tetrahedron published new progress about 197958-29-5. 197958-29-5 belongs to pyridine-derivatives, auxiliary class Pyridine,Boronic acid and ester, name is 2-Pyridinylboronic acid, and the molecular formula is C13H26N2, Synthetic Route of 197958-29-5.

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

Battula, S. R. K. published the artcileA mild and efficient copper-catalyzed N-arylation of unprotected sulfonimidamides using boronic acids, Formula: C5H6BNO2, the publication is Tetrahedron Letters (2014), 55(2), 517-520, database is CAplus.

An efficient and low cost copper catalyzed system for N-arylation of sulfonimidamides was developed. The reaction proceeds at room temperature under base free conditions. Various N-aryl, N-heteroaryl, and N-cyclopropyl sulfonimidamides were obtained in good to excellent yields.

Tetrahedron Letters published new progress about 197958-29-5. 197958-29-5 belongs to pyridine-derivatives, auxiliary class Pyridine,Boronic acid and ester, name is 2-Pyridinylboronic acid, and the molecular formula is C5H6BNO2, Formula: C5H6BNO2.

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