Month: November 2022

Mancha, Gisela published the artcileEfficient synthesis of racemic and chiral alkenyl sulfoxides by palladium-catalyzed Suzuki coupling, Product Details of C11H16BNO3, the publication is Tetrahedron (2010), 66(34), 6901-6905, database is CAplus.

Alkenyl sulfoxide derivatives are obtained in high yields through a palladium-catalyzed Suzuki/Miyaura cross-coupling reaction of racemic and chiral 1-halo sulfoxides with aryl and alkenyl boronic acids. Chiral substrates react with no loss of optical purity and high optical yields. The reaction takes place with different palladium catalysts, such as Pd(PPh₃)₄ or Pd(OAc)₂/DABCO. Although nitrogen ligands like DABCO lead to an active palladium catalyst, they are less effective than the phosphine ones.

Tetrahedron published new progress about 146140-95-6. 146140-95-6 belongs to amides-buliding-blocks, auxiliary class Boronic acid and ester,Amine,Benzene,Amide,Boronic Acids,Boronic Acids,Boronic acid and ester,, name is (2-Pivalamidophenyl)boronic acid, and the molecular formula is C11H16BNO3, Product Details of C11H16BNO3.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Pudlo, Marc published the artcileFirst Suzuki-Miyaura type cross-coupling of ortho-azidobromobenzene with arylboronic acids and its application to the synthesis of fused aromatic indole-heterocycles, HPLC of Formula: 146140-95-6, the publication is Tetrahedron (2007), 63(41), 10320-10329, database is CAplus.

A short synthesis of some fused indole-heterocycles, e.g., I (R = H, CN or CHO), has been achieved via Pd-catalyzed cross-coupling reactions between azido-2-bromobenzene and arylboronic acids and subsequent thermally induced nitrene insertion. Addnl., 4-amino-α-carboline, a versatile intermediate toward grossularine analogs has also been prepared by Suzuki-Miyaura cross-coupling of 4-pivaloylaminopyridine-3-boronic acid with 2-bromoaniline, followed by simple functional group transformations.

Tetrahedron published new progress about 146140-95-6. 146140-95-6 belongs to amides-buliding-blocks, auxiliary class Boronic acid and ester,Amine,Benzene,Amide,Boronic Acids,Boronic Acids,Boronic acid and ester,, name is (2-Pivalamidophenyl)boronic acid, and the molecular formula is C11H16BNO3, HPLC of Formula: 146140-95-6.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Chisca, Diana published the artcileFour Cu(II) coordination polymers with biocompatible isonicotinamide and picolinate ligands in interplay with anionic and neutral linkers, Application of Isonicotinamide, the publication is Inorganic Chemistry Communications (2021), 108864, database is CAplus.

Four Cu(II)-based neutral coordination polymers, 1D {[Cu(isonia)₂(adi)(dmf)].0.5H₂adi}_n (1), 2D {[Cu(isonia)₂(adi)](H₂O.H₂adi)}_n (2), 1D {[Cu(pic)(CH₃COO)(bpe)].H₂O}_n (3), and 2D [Cu₂(pic)₂(CH₃COO)₂(bpy)]_n (4) with biocompatible mols.: isonicotinamide (isonia), pyridine-2-carboxylic (picolinic, Hpic) and adipic (H₂adi) acids and 1,2-bis(4-pyridyl)-ethane (bpe) and 4,4′-bipyridine (bpy) as neutral linkers are reported. The polymer extension in 1 and 2 is reached via bidentate bridging adi anions with isonia ligands as single 1 and double 2 pillars. 1D and 2D coordination arrays are associated in elegant 3D H-bonded networks via interplay of robust amide(isonia)…amide(isonia) homosynthon and NH…O(COO^–) side interactions. In 3 the pic residue coordinates in a chelate mode and forms the five-membered [Cu(pic)] corner fragment. The structure expansion occurs via bidentate-bridging bpe neutral linker registered in a coordination wire as different conformers thus providing long (Cu-bpe)₆ crystallog. unique chain fragment. Oppositely, in 4 the pic residue acts in a bidentate chelate bridging mode and gives rise to the 2D coordination array. The bpy trapping between each two Cu(II) atoms, does not participate in further structure extension. The decisive impact of amido-group of isonia ligand in structure rigidification and retention of protic H₂adi and water guest mols. is demonstrated. The gradual decrease of guest’s capacity correlates with an increased liphophilicity of 3 and 4 comparing with 1 and 2.

Inorganic Chemistry Communications published new progress about 1453-82-3. 1453-82-3 belongs to amides-buliding-blocks, auxiliary class Pyridine,Amine,Amide, name is Isonicotinamide, and the molecular formula is C6H6N2O, Application of Isonicotinamide.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Karp, Gary M. published the artcile3-(Heterocyclyl)phenyl cyanurates: synthesis and herbicidal activity, Synthetic Route of 2447-79-2, the publication is ACS Symposium Series (2002), 30-40, database is CAplus.

3-(Heterocyclyl)phenyl cyanurates such as I make up a novel class of protoporphyrinogen oxidase (protox) inhibitors which were prepared and evaluated for herbicidal activity. The compounds were primarily postemergence broadleaf compounds The effect of changes in the aryl moiety, the heteroaryl moiety, and in the pendant ester of the cyanurate moiety on the herbicidal activity of the heterocyclylaryl cyanurates was studied.

ACS Symposium Series published new progress about 2447-79-2. 2447-79-2 belongs to amides-buliding-blocks, auxiliary class Chloride,Amine,Benzene,Amide, name is 2,4-Dichlorobenzamide, and the molecular formula is C7H5Cl2NO, Synthetic Route of 2447-79-2.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Walters, Hannah E. published the artcileGeneration of a novel model of primary human cell senescence through Tenovin-6 mediated inhibition of sirtuins, Safety of 4-(tert-Butyl)-N-((4-(5-(dimethylamino)pentanamido)phenyl)carbamothioyl)benzamide, the publication is Biogerontology (2019), 20(3), 303-319, database is CAplus and MEDLINE.

Cell senescence, a state of cell cycle arrest and altered metabolism with enhanced pro-inflammatory secretion, underlies at least some aspects of organismal ageing. The sirtuin family of deacetylases has been implicated in preventing premature ageing; sirtuin overexpression or resveratrol-mediated activation of sirtuins increase longevity. Here we show that sirtuin inhibition by short-term, low-dose treatment with the exptl. anti-cancer agent Tenovin-6 (TnV6) induces cellular senescence in primary human fibroblasts. Treated cells cease proliferation and arrest in G1 of the cell cycle, with elevated p21 levels, DNA damage foci, high mitochondrial and lysosomal load and increased senescence-associated β galactosidase activity, together with actin stress fibers and secretion of IL-6 (indicative of SASP upregulation). Consistent with a histone deacetylation role of SIRT1, we find nuclear enlargement, possibly resulting from chromatin decompaction on sirtuin inhibition. These findings highlight TnV6 as a drug that may be useful in clin. settings where acute induction of cell senescence would be beneficial, but also provide the caveat that even supposedly non-genotoxic anticancer drugs can have unexpected and efficacy-limiting impacts on non-transformed cells.

Biogerontology published new progress about 1011557-82-6. 1011557-82-6 belongs to amides-buliding-blocks, auxiliary class Epigenetics,Sirtuin, name is 4-(tert-Butyl)-N-((4-(5-(dimethylamino)pentanamido)phenyl)carbamothioyl)benzamide, and the molecular formula is C8H6ClF3, Safety of 4-(tert-Butyl)-N-((4-(5-(dimethylamino)pentanamido)phenyl)carbamothioyl)benzamide.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Blencowe, Anton published the artcileSurface modification of nylon 6,6 using a carbene insertion approach, Name: N,N-Diethyl-2,2,2-trifluoroacetamide, the publication is New Journal of Chemistry (2006), 30(1), 53-58, database is CAplus.

The diazirine functionalized fluorenone, 3-[3-(trifluoromethyl)diazirin-3-yl]phenyl-9-oxo-9H-fluorene-2-carboxylate was synthesized to act as a model compound capable of modifying a wide variety of polymeric substrates. Photochem. activation of the diazirine moiety of the fluorenone derivative was utilized to afford highly reactive carbenes capable of insertion into or addition to a wide variety of functionalities. The photoinduced attachment of a fluorenone derivative to nylon 6,6 has been studied using UV-visible spectroscopic anal. Incorporation of the fluorenone chromophore onto the backbone of nylon at different loading levels and after different coating cycles has been investigated and is detailed.

New Journal of Chemistry published new progress about 360-92-9. 360-92-9 belongs to amides-buliding-blocks, auxiliary class Trifluoromethyl,Fluoride,Amine,Aliphatic hydrocarbon chain,Amide, name is N,N-Diethyl-2,2,2-trifluoroacetamide, and the molecular formula is C6H10F3NO, Name: N,N-Diethyl-2,2,2-trifluoroacetamide.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Charnley, Adam K. published the artcileCrystal structures of human RIP2 kinase catalytic domain complexed with ATP-competitive inhibitors: Foundations for understanding inhibitor selectivity, Name: Morpholine-4-carbothioamide, the publication is Bioorganic & Medicinal Chemistry (2015), 23(21), 7000-7006, database is CAplus and MEDLINE.

Receptor interacting protein 2 (RIP2) is an intracellular kinase and key signaling partner for the pattern recognition receptors NOD1 and NOD2 (nucleotide-binding oligomerization domain-containing proteins 1 and 2). As such, RIP2 represents an attractive target to probe the role of these pathways in disease. In an effort to design potent and selective inhibitors of RIP2 we established a crystallog. system and determined the structure of the RIP2 kinase domain in an apo form and also in complex with multiple inhibitors, including AMP-PCP (β,γ-methyleneadenosine 5′-triphosphate, a non-hydrolyzable ATP mimic) and structurally diverse ATP competitive chemotypes identified via a high-throughput screening campaign. These structures represent the first set of diverse RIP2-inhibitor co-crystal structures and demonstrate that the protein possesses the ability to adopt multiple DFG-in as well as DFG-out and C-helix out conformations. These structures reveal key protein-inhibitor structural insights and serve as the foundation for establishing a robust structure-based drug design effort to identify both potent and highly selective inhibitors of RIP2 kinase.

Bioorganic & Medicinal Chemistry published new progress about 14294-10-1. 14294-10-1 belongs to amides-buliding-blocks, auxiliary class Morpholine,Thiourea,Amine,Amide, name is Morpholine-4-carbothioamide, and the molecular formula is C5H10N2OS, Name: Morpholine-4-carbothioamide.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

O’Callaghan, C. N. published the artcileAnticancer agents XIII. Synthesis and antitumor activity of 2-iminochromene derivatives, SDS of cas: 15029-36-4, the publication is Proceedings of the Royal Irish Academy, Section B: Biological, Geological and Chemical Science (1979), 79B(6), 87-98, database is CAplus.

Iminochromenes I (R = H, 6-OMe, 7-OMe, 6-NO₂, 6,8-Br₂, 8-OEt, 8-OMe; R¹ = H, alkyl, hydroxyalkyl, NHCSNHMe, optionally substituted Ph, anilino, acylamino, morpholino) were prepared by condensing salicylaldehydes with NCCH₂CONHR¹. II (R² = OMe, OEt, OPr, R³ = H; R² = H, R³ = OMe, OEt, OPr) were obtained by condensing salicylaldehydes with 1-cyanoacetyl-3,5-dimethylpyrazole. I, II, and related compounds had antitumor activity. Thus, I (R = 6-OMe, R¹ = H) gave a mean survival time 131% of controls as 108 mg/kg in P 388 lymphocytic leukemia-infected mice.

Proceedings of the Royal Irish Academy, Section B: Biological, Geological and Chemical Science published new progress about 15029-36-4. 15029-36-4 belongs to amides-buliding-blocks, auxiliary class Nitrile,Amine,Aliphatic hydrocarbon chain,Amide, name is 2-Cyano-N-ethylacetamide, and the molecular formula is C5H8N2O, SDS of cas: 15029-36-4.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Czaplewski, Lloyd G. published the artcileAntibacterial alkoxybenzamide inhibitors of the essential bacterial cell division protein FtsZ, Synthetic Route of 64559-06-4, the publication is Bioorganic & Medicinal Chemistry Letters (2009), 19(2), 524-527, database is CAplus and MEDLINE.

3-Methoxybenzamide is a weak inhibitor of the essential bacterial cell division protein FtsZ. Exploration of the structure-activity relationships of 3-methoxybenzamide analogs led to the identification of potent anti-staphylococcal compounds

Bioorganic & Medicinal Chemistry Letters published new progress about 64559-06-4. 64559-06-4 belongs to amides-buliding-blocks, auxiliary class Amine,Benzene,Amide,Ether, name is 3-Methoxybenzothioamide, and the molecular formula is C8H9NOS, Synthetic Route of 64559-06-4.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Rocca, P. published the artcileFirst metalation of aryl iodides: directed ortho-lithiation of iodopyridines, halogen-dance, and application to synthesis, Computed Properties of 146140-95-6, the publication is Journal of Organic Chemistry (1993), 58(27), 7832-8, database is CAplus.

Metalation of iodopyridines was successfully achieved by LDA at low temperature In many cases, lithiation is ortho directed by the iodo group which subsequently ortho-migrates very fast to give stabilized iodolithiopyridines. This procedure was applied to 2-fluoro- and 2-chloro-3-iodopyridines, 3-fluoro-4-iodopyridine, and 2-chloro-3-fluoro-4-iodopyridine. The resulting lithio intermediates were obtained in high yields before being reacted with electrophiles leading to various polysubstituted pyridines. Some of these iodopyridines were used as key mols. for the preparation of fused polyaromatic alkaloids. Thus, perlolidine (I), δ-carbolines, and 2,10-diazaphenanthrenes were readily prepared in few steps taking advantage of the iodo reactivity for heteroring cross-coupling. Coupling of [2-(pivaloylamino)phenyl]boronic acid with 2-fluoro-4-iodo-3-pyridinecarboxaldehyde gave I.

Journal of Organic Chemistry published new progress about 146140-95-6. 146140-95-6 belongs to amides-buliding-blocks, auxiliary class Boronic acid and ester,Amine,Benzene,Amide,Boronic Acids,Boronic Acids,Boronic acid and ester,, name is (2-Pivalamidophenyl)boronic acid, and the molecular formula is C11H16BNO3, Computed Properties of 146140-95-6.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics