Category: 1885-29-6

Li, Quanzhe published the artcileOne-Pot Synthesis of Spirocyclopenta[a]indene Derivatives via a Cascade Ring Expansion and Intramolecular Friedel-Crafts-Type Cyclization, COA of Formula: C7H6N2, the main research area is spirocyclopentaindene derivative preparation; propargyl alc tethered alkylidenecyclobutane preparation cascade ring expansion cyclization.

A one-pot efficient synthetic approach for the rapid construction of spirocyclopenta[a]indene derivatives has been developed via an iodine-initiated cascade ring expansion and intramol. Friedel-Crafts-type cyclization from propargyl alc.-tethered alkylidenecyclobutanes under mild conditions with broad substrate scope. This cascade process can be elegantly conducted on a gram scale. A plausible reaction mechanism has been proposed on the basis of a series of deuterium labeling and control experiments

Journal of Organic Chemistry published new progress about Cyclization. 1885-29-6 belongs to class nitriles-buliding-blocks, name is 2-Aminobenzonitrile(Flakes or Chunks), and the molecular formula is C7H6N2, COA of Formula: C7H6N2.

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

Tian, Jun-Jie published the artcileIntramolecular Cyclizations of Vinyl-Substituted N,N-Dialkyl Arylamines Enabled by Borane-Assisted Hydride Transfer, Quality Control of 1885-29-6, the main research area is arylamine dialkyl vinyl borane hydride transfer cyclization catalyst; tetrahydrobenzoquinoline preparation.

Catalytic amounts of B(C6F5)3 have been found to be able to promote the intramol. cyclization of vinyl-substituted N,N-dialkyl arylamines to afford nitrogen-containing heterocycles I (R = Me, Bn, n-pentyl; R1 = H, Ph, n-Bu; R2 = Ph, 4-EtC6H4, 3-MeC6H4, Me, n-Pr, etc.). Our mechanistic studies indicate the reaction is initiated by abstraction of an α-hydride from an N-alkyl substituent by B(C6F5)3, which is followed by cyclization, and is concluded by delivery of the hydride to the cyclic cationic intermediate. The dual roles of B(C6F5)3, first as an oxidant and then as a hydride-carrying reductant, have enabled a rare redox-neutral cyclization process between a sp3 carbon and an electron-rich olefin without using a transition metal or an external oxidant.

ACS Catalysis published new progress about Boranes Role: CAT (Catalyst Use), USES (Uses). 1885-29-6 belongs to class nitriles-buliding-blocks, name is 2-Aminobenzonitrile(Flakes or Chunks), and the molecular formula is C7H6N2, Quality Control of 1885-29-6.

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

Hu, Xiaoping published the artcileNickel-Catalyzed β-Regioselective Amination/Cyclization of Ynamide-Nitriles with Amines: Synthesis of Functionalized 3-Aminoindoles and 4-Aminoisoquinolines, Application In Synthesis of 1885-29-6, the main research area is indole amino aryliminobenzyl preparation; ynamide nitrile regioselective amination cyclization aromatic amine nickel catalyst.

A highly regioselective nickel/Lewis acid catalyzed amination/cyclization of ynamide-nitriles I (R1 = Ph, 4-MeOC6H4, 2-FC6H4, 2-thienyl, etc.; R2 = Me, 4-FC6H4, 4-MeC6H4, 4-MeOC6H4) with amines R3NH2 (R3 = Ph, 4-FC6H4, 3,5-Me2C6H3, 1-naphthyl, 2-thiazolyl, etc.) involving β-addition has been developed. The reaction offers an attractive and efficient route for the synthesis of 3-aminoindoles II. A 4-aminoisoquinoline was also obtained via this approach. The R2SO2-group on the ynamide acts as a directing group to produce the alkenyl nickel species with high regioselectivity.

Organic Letters published new progress about Amination catalysts. 1885-29-6 belongs to class nitriles-buliding-blocks, name is 2-Aminobenzonitrile(Flakes or Chunks), and the molecular formula is C7H6N2, Application In Synthesis of 1885-29-6.

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

Yang, Fanpeng published the artcilePalladium-Catalyzed Coupling Reaction of o-Alkenyl Chloroformylanilines with o-Alkynylanilines: An Approach to Indolylmethyl Oxindole, Application In Synthesis of 1885-29-6, the main research area is indolylmethyl oxindole preparation; ortho alkenyl chloroformylaniline alkynylaniline cascade coupling palladium catalyst.

A palladium-catalyzed cascade Heck cyclization/3-(2-oxindolyl)methylation on intramol. amination of o-alkynylanilines for the synthesis of indolylmethyl oxindoles is developed. This protocol exhibits high efficiency, good functional group tolerance and scalability from easily accessible starting materials. In this transformation, chloroformylaniline was used as an oxidative reagent and o-alkynylaniline was used as a 3-indolyl precursor.

Asian Journal of Organic Chemistry published new progress about Amines, alkynyl Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 1885-29-6 belongs to class nitriles-buliding-blocks, name is 2-Aminobenzonitrile(Flakes or Chunks), and the molecular formula is C7H6N2, Application In Synthesis of 1885-29-6.

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

Roy, Bivas Chandra published the artcileTandem synthesis of quinazolinone scaffolds from 2-aminobenzonitriles using aliphatic alcohol-water system, Category: nitriles-buliding-blocks, the main research area is aminobenzonitrile aliphatic alc water tandem hydration dehydrogenative coupling; quinazolinone preparation green chem.

Ru(II) complex catalyzed tandem synthesis of quinazolinone derivatives is reported here. In this sustainable protocol, 2-aminobenzonitriles were directly transformed to quinazolinones using alc.-water system. A variety of quinazolinones was successfully synthesized in good to excellent yields by utilizing challenging methanol and aliphatic alcs. The practical applicability of the protocol was extended by preparative scale synthesis of various heterocycles as well as natural products. To understand the mechanism of this protocol, several control experiments and DFT studies were carried out. Based on the DFT calculations, a metal-ligand cooperative mechanism was proposed for this system.

Catalysis Science & Technology published new progress about Aromatic nitriles Role: RCT (Reactant), RACT (Reactant or Reagent) (2-aminoaryl). 1885-29-6 belongs to class nitriles-buliding-blocks, name is 2-Aminobenzonitrile(Flakes or Chunks), and the molecular formula is C7H6N2, Category: nitriles-buliding-blocks.

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

Wan, Yin-Bo published the artcileHighly Enantioselective Iridium-Catalyzed Hydrogenation of o-Amidophenyl Ketones Enabled by 1,2-Diphenylethylenediamine-Derived P,N,N-Ligands with Tertiary Amine Terminus, HPLC of Formula: 1885-29-6, the main research area is arylcarbonylaryl acetamide iridium catalyst enantioselective hydrogenation; hydroxymethylaryl acetamide preparation.

A readily available and highly modular class of chiral P,N,N-ligands based on a structurally flexible nonchiral phosphine-amine framework with an optically active 1,2-diphenylethylenediamine unit bearing a tertiary amine terminus as the chiral source were developed and successfully applied in the Ir-catalyzed asym. hydrogenation of o-amidophenyl ketones. These tridentate P,N,N-ligands exhibited excellent activity, enantioselectivity, and substrate tolerance, thus furnishing various optically active o-amidobenzhydrols in up to 99% yields and with >99% ee. The utility of this protocol was proven by synthetically diverse product transformation and highly enantioselective production of a rice plant growth regulator, (S)-inabenfide.

Organic Letters published new progress about Aralkyl alcohols Role: PRP (Properties), RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 1885-29-6 belongs to class nitriles-buliding-blocks, name is 2-Aminobenzonitrile(Flakes or Chunks), and the molecular formula is C7H6N2, HPLC of Formula: 1885-29-6.

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

Zeng, Fanxin published the artcileDesign, Synthesis and Bioactivity Evaluation of Coumarin-BMT Hybrids as New Acetylcholinesterase Inhibitors, Name: 2-Aminobenzonitrile(Flakes or Chunks), the main research area is tetrahydromethanoacridinyl aminoalkylcarboxamido coumarin preparation acetylcholinesterase inhibition kinetics SAR docking; acetylcholinesterase inhibitors; bioactivity evaluation; coumarin–BMT hybrids; molecular docking.

The compound bridge methylene tacrine (BMT) was synthesized, which has the classical pharmacophore structure of Tacrine (THA). Based on the principle of active substructure splicing, BMT was used as a lead compound and synthesized coumarin-BMT hybrids I [n = 5, 6, 7; R1 = H, Me, MeO, F3CO, Br; R2 = H, MeO] by introducing coumarin to BMT. In this work, 21 novel hybrids of BMT and coumarin I were synthesized and evaluated for their inhibitory activity on AChE. All obtained compounds I presented preferable inhibition. Compound I [n = 6, R1 = Me, R2 = H] was the most active compound, with the value of Ki as 49.2 nM, which was higher than Galantamine (GAL) and lower than THA. The result of mol. docking showed that the highest binding free energy was -40.43 kcal/mol for compound I [n = 6, R1 = Me, R2 = H] which was an identical trend with the calculated Ki.

Molecules published new progress about Aminoacridines Role: PAC (Pharmacological Activity), PRP (Properties), RCT (Reactant), SPN (Synthetic Preparation), THU (Therapeutic Use), BIOL (Biological Study), RACT (Reactant or Reagent), PREP (Preparation), USES (Uses). 1885-29-6 belongs to class nitriles-buliding-blocks, name is 2-Aminobenzonitrile(Flakes or Chunks), and the molecular formula is C7H6N2, Name: 2-Aminobenzonitrile(Flakes or Chunks).

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

Waltemate, Jana published the artcile10-(4-Phenylpiperazine-1-carbonyl)acridin-9(10H)-ones and related compounds: Synthesis, antiproliferative activity and inhibition of tubulin polymerization, Name: 2-Aminobenzonitrile(Flakes or Chunks), the main research area is piperazinecarbonyl acridinone synthesis anticancer tubulin polymerization inhibitor; 10-(4-Phenylpiperazine-1-carbonyl)acridin-9(10H)-ones; 10-Benzoylacridin-9(10H)-ones; Antimitotic; Apoptosis; Colchicin binding site; Inhibition of Tubulin Polymerization.

As part of our continuing search for potent inhibitors of tubulin polymerization, two novel series of 42 10-(4-phenylpiperazine-1-carbonyl)acridin-9(10H)-ones and N-benzoylated acridones were synthesized on the basis of a retrosynthetic approach. All newly synthesized compounds were tested for antiproliferative activity and interaction with tubulin. Several analogs potently inhibited tumor cell growth. Among the compounds tested, 10-(4-(3-methoxyphenyl)piperazine-1-carbonyl)acridin-9(10H)-one (17c, I) exhibited excellent growth inhibitory effects on 93 tumor cell lines, with an average GI50 value of 5.4 nM. We were able to show that the strong cytotoxic effects are caused by disruption of tubulin polymerization, as supported by the EBI (N,N’-Ethylenebis(iodoacetamide)) assay and the fact that the most potent inhibitors of cancer cell growth turned out to be the most efficacious tubulin polymerization inhibitors. Potencies were nearly comparable or superior to those of the antimitotic reference compounds Closely related to this, the most active analogs inhibited cell cycling at the G2/M phase at concentrations down to 30 nM and induced apoptosis in K562 leukemia cells. We believe that our work not only proves the excellent suitability of the acridone scaffold for the design of potent tubulin polymerization inhibitors but also enables synthetic access to further potentially interesting N-acylated acridones.

Bioorganic & Medicinal Chemistry Letters published new progress about Acylation. 1885-29-6 belongs to class nitriles-buliding-blocks, name is 2-Aminobenzonitrile(Flakes or Chunks), and the molecular formula is C7H6N2, Name: 2-Aminobenzonitrile(Flakes or Chunks).

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

Li, Shuai published the artcileDesign, synthesis and biological evaluation of homoerythrina alkaloid derivatives bearing a triazole moiety as PARP-1 inhibitors and as potential antitumor drugs, HPLC of Formula: 1885-29-6, the main research area is homoerythrina alkaloid triazole preparation antitumor PARP 1 inhibitor; 1,2,3-Triazole; Antitumor; Apoptosis; Drug discovery; Homoerythrina alkaloid; PARP-1 inhibitor.

A series of homoerythrina alkaloid derivatives containing a 1,2,3-triazole moiety as PARP-1 inhibitors were designed and synthesized. And their anti-proliferative activity was further evaluated. Compound I had excellent activity to inhibit proliferation of A549 cells (IC50 = 1.89μM), which was higher than harringtonine (IC50 = 10.55μM), pemetrexed (IC50 = 3.39μM), and rucaparib (IC50 = 4.91μM). Furthermore, the selectivity index of compound I was higher than rucaparib and pemetrexed for lung cancer cells. Flow cytometry anal. showed that compound I significantly arrested the cell cycle in the S phase, then induced apoptosis of A549 cells (apoptosis rate is 46%), which effectively inhibited cell proliferation. Simultaneously, western blot anal. revealed that compound I could prevent the biosynthesis of PAR. Further anal. results revealed that compound I could inhibit the expression of cyclin A, down-regulate the expression of bcl-2/bax, activate caspase-3, and ultimately induce apoptosis of A549 cells. All the results indicated that compound I had potential research value as a novel PARP-1 inhibitor in antitumor, and it provided a new reference for further development of PARP-1 inhibitors.

Bioorganic Chemistry published new progress about Antitumor agents. 1885-29-6 belongs to class nitriles-buliding-blocks, name is 2-Aminobenzonitrile(Flakes or Chunks), and the molecular formula is C7H6N2, HPLC of Formula: 1885-29-6.

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

Rodriguez, Jose F. published the artcileSynthesis of 1-Amino-2,2,2-trifluoroalkylphosphonates from Alkene-Tethered Trifluoroacetimidoyl Chlorides, Category: nitriles-buliding-blocks, the main research area is alkene tethered trifluoroacetimidoyl chloride preparation cyclization alkyl phosphite; aminotrifluoroalkyl phosphonate preparation crystal structure; mol structure aminotrifluoroalkyl phosphonate.

The reaction of alkene-tethered trifluoroacetimidoyl chlorides with trialkyl phosphites furnishes 1-amino-2,2,2-trifluoroalkylphosphonates. The products were generated in moderate to good yields, and the scalability of this process was showcased. Partial hydrolysis of the phosphonate moiety was achieved. The cyclization probably occurs via formation of an imidoyl phosphonate intermediate that becomes susceptible to nucleophilic attack at N through the strong electron-withdrawing groups at the imidoyl C.

Organic Letters published new progress about Crystal structure. 1885-29-6 belongs to class nitriles-buliding-blocks, name is 2-Aminobenzonitrile(Flakes or Chunks), and the molecular formula is C7H6N2, Category: nitriles-buliding-blocks.

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts