Category: 38487-85-3

Roessler, Simon L.; Jelier, Benson J.; Tripet, Pascal F.; Shemet, Andrej; Jeschke, Gunnar; Togni, Antonio; Carreira, Erick M. published the artcile< Pyridyl Radical Cation for C-H Amination of Arenes>, Recommanded Product: 2-Amino-4-methoxybenzonitrile, the main research area is amination arene pyridinium triflate visible light photocatalysis mechanism; amination; late-stage functionalization; photoredox catalysis; pyridyl radical cation; radical mechanism.

Electron-transfer photocatalysis provides access to the elusive and unprecedented N-pyridyl radical cation from selected N-substituted pyridinium reagents. The resulting C(sp2)-H functionalization of (hetero)arenes furnishes versatile intermediates for the development of valuable aminated aryl scaffolds. Mechanistic studies that include the first spectroscopic evidence of a spin-trapped N-pyridyl radical adduct implicate SET-triggered, pseudo-mesolytic cleavage of the N-X pyridinium reagents mediated by visible light.

Angewandte Chemie, International Edition published new progress about Amination (pyridination). 38487-85-3 belongs to class nitriles-buliding-blocks, and the molecular formula is C8H8N2O, Recommanded Product: 2-Amino-4-methoxybenzonitrile.

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

Sun, Huan; Jiang, Yue; Lu, Ming-Kun; Li, Yun-Yun; Li, Li; Liu, Ji-Kai published the artcile< Iron-Catalyzed Tandem Radical Addition/Cyclization: Highly Efficient Access to Methylated Quinoline-2,4-diones>, Application In Synthesis of 38487-85-3, the main research area is methyl quinoline dione preparation; cyanoaryl acrylamide dimethyl sulfoxide photochem methylation iron catalyst.

A visible-light-induced and iron-catalyzed oxidative radical addition/cyclization cascade reaction of N-(o-cyanoaryl)acrylamides I [R1 = 4-Cl, 5-CF3, 3-Br, etc.; R2 = Me, Bn; R3 = Me, [(2,2-dimethylpropanoyl)oxy]methyl, Bn, Ph, (acetyloxy)methyl, (1,3-dioxo-2,3-dihydro-1H-isoindol-2-yl)methyl] with DMSO has been developed. The method exhibits a wide substrate scope and an excellent functional-group tolerance, thus providing an efficient and convenient access to a variety of methylated quinoline-2,4-diones II (R4 = 6-Cl, 6-CF3, 5-Br, etc.).

Synlett published new progress about Acrylamides Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 38487-85-3 belongs to class nitriles-buliding-blocks, and the molecular formula is C8H8N2O, Application In Synthesis of 38487-85-3.

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

Chen, Peng; Zhuang, Yu-Xin; Diao, Peng-Cheng; Yang, Fang; Wu, Shao-Yu; Lv, Lin; You, Wen-Wei; Zhao, Pei-Liang published the artcile< Synthesis, biological evaluation, and molecular docking investigation of 3-amidoindoles as potent tubulin polymerization inhibitors>, Synthetic Route of 38487-85-3, the main research area is amidoindole preparation antiproliferative mol docking tubulin inhibitor human; 3-Amidoindoles; Antiproliferative activity; Microtubules; Tubulin polymerization.

A series of novel 3-amidoindole derivatives possessing 3,4,5-trimethoxylphenyl groups I [R1 = H, Me, Cl, OMe; R2 = 2-thienyl, Ph, 4-FC6H4, etc.] was synthesized and evaluated for their antiproliferative and tubulin polymerization inhibitory activities. Some of them demonstrated moderate to potent activities in vitro against six cancer cell lines including MCF-7, MDA-MB-231, BT549, T47D, MDA-MB-468, and HS578T. The most active compound I [R1 = Cl; R2 = 4-ClC6H4] inhibited the growth of T47D, BT549, and MDA-MB-231 cell lines with IC50 values at 0.04, 3.17, and 6.43 μM, resp. Moreover, the flow cytometric anal. clearly revealed that compound I [R1 = Cl; R2 = 4-ClC6H4] significantly inhibited growth of breast cancer cells through arresting cell cycle in G2/M phase via a concentration-dependent manner. In addition, the compound I [R1 = Cl; R2 = 4-ClC6H4] also exhibited the most potent anti-tubulin activity with IC50 values of 9.5 μM, which was remarkable, compared to CA-4. Furthermore, mol. docking anal. demonstrated the interaction of the compound I [R1 = Cl; R2 = 4-ClC6H4] at the colchicine-binding site of tubulin.

European Journal of Medicinal Chemistry published new progress about Antiproliferative agents. 38487-85-3 belongs to class nitriles-buliding-blocks, and the molecular formula is C8H8N2O, Synthetic Route of 38487-85-3.

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

Kalogirou, Andreas S.; Kourtellaris, Andreas; Koutentis, Panayiotis A. published the artcile< Synthesis and Reactivity of 3',5'-Dichloro-1H-spiro(quinazoline-2,4'-[1,2,6]thiadiazin)-4(3H)-ones>, Quality Control of 38487-85-3, the main research area is chloro spiro quinazoline thiadiazine derivative synthesis reactivity.

A three-step synthesis of 3′,5′-dichloro-1H-spiro(quinazoline-2,4′-[1,2,6]thiadiazin)-4(3H)-ones starting from 3,4,4,5-tetra-chloro-4H-1,2,6-thiadiazine (I) is presented. The latter reacts with 2-aminobenzonitriles to give 2-[(3,5-dichloro-4H-1,2,6-thiadiazin-4-ylidene)amino]benzonitriles [e.g., I + 2-aminobenzonitrile → II (86%)] , which affords, after hydration, the resp. benzamides [II → III (84%)]. Upon heating at reflux in EtOH or HFIP, the benzamides intramolecularly cyclize onto the thiadiazine C4 position to give 3′,5′-dichloro-1H-spiro(quinazoline-2,4′-[1,2,6]thiadiazin)-4(3H)-ones [III → IV (95% in EtOH, 97% in HFIP)]. Single crystal X-ray crystallog. supports the structure of two analogs. The chloride displacement of these new spiroquinazolinones was demonstrated by Stille coupling, and by reaction with methoxide to afford both the mono and bis-methoxy derivatives

European Journal of Organic Chemistry published new progress about Aromatic nitriles Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation) (anthranilonitriles → [(dichlorothiadiazinylidene)amino]benzonitriles). 38487-85-3 belongs to class nitriles-buliding-blocks, and the molecular formula is C8H8N2O, Quality Control of 38487-85-3.

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

Abel-Snape, Xavier; Wycich, Gina; Lautens, Mark published the artcile< Synthesis of Indenes and Benzofulvenes via a Palladium-Catalyzed Three-Component Reaction>, Category: nitriles-buliding-blocks, the main research area is indene benzofulvene preparation palladium catalyst three component reaction.

A palladium-catalyzed three-component domino reaction to access indene derivatives is reported. This reaction proceeds via the sequential formation of three bonds: the first two resulting from inter- and intramol. carbopalladation and the final bond arising from an attack by a terminating nucleophilic reagent. Modifying the starting tether on the iodoarene led to either indenes or benzofulvenes. Three termination variations were compatible with this sequence, which furnished products in moderate to good yields. The oxabicycle used in this work acts as an acetylene surrogate, which is revealed in a postcatalytic retro-Diels-Alder step. A diastereomerically enriched mixture of oxabicyclic derivatives allowed for preliminary results for the enantioselective synthesis of indenes.

ACS Catalysis published new progress about Alkenynes Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 38487-85-3 belongs to class nitriles-buliding-blocks, and the molecular formula is C8H8N2O, Category: nitriles-buliding-blocks.

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

Jiang, Shuai; Cao, Wen-Bin; Xu, Xiao-Ping; Ji, Shun-Jun published the artcile< Cobalt-Catalyzed Isocyanide-Based Three-Component Cascade for the Synthesis of Quinazolines>, Related Products of 38487-85-3, the main research area is quinazoline preparation; arylisocyanide arylamine azide three component tandem heterocyclization cobalt catalyst.

A Co-catalyzed cyclization reaction of isocyanides 1-NC-4-R-5-R1C6H2CN (R = H, Me, F, OMe, etc.; R1 = H, OMe, Br), azides R2S(O)ON3 (R2 = n-Pr, Ph, cyclohexyl, thiophen-2-yl, etc.), and amines R3NH2 (R3 = n- Bu, Ph, 1-methyl-1H-indol-5-yl, etc.) to access quinazoline derivatives I and II (R4 = H, n-Bu, t-Bu, 4-methylphenyl) was described. This protocol features a high atom economy, mild reaction conditions, excellent yields, and a broad substrate scope. This cascade reaction involved three or four C-N bonds and the formation of one or two rings. The quinazolin-4(H)-imines I and II obtained are proven to be versatile intermediates for further valuable transformations. It was also found that the cobalt catalyst could be isolated from the reaction mixture and reused.

Organic Letters published new progress about Amines Role: RCT (Reactant), RACT (Reactant or Reagent). 38487-85-3 belongs to class nitriles-buliding-blocks, and the molecular formula is C8H8N2O, Related Products of 38487-85-3.

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

Sheng, Hui-Yang; Chen, Hui; Liao, Meng; Peng, Na; Yang, Mian; Cai, Qun; Liu, Yi published the artcile< Copper-catalyzed Tandem Cyclization to Access 4-Aminoquinoline Derivatives>, SDS of cas: 38487-85-3, the main research area is nitroethenylaryl aminobenzonitrile copper catalyst tandem Michael heterocyclization oxidation; nitro arylquinolinamine preparation.

An efficient and practical method for the synthesis of 4-aminoquinoline derivativeswas developed via copper-catalyzed cascade cyclization of 2-aminobenzonitrile and nitroolefins. This reaction proceeded through a consecutive Michael addition/cyclization/oxidization protocol, providing 4-aminoquinolines with moderate to excellent yields under mild conditions. This method features readily available materials, one-pot one-step operation, and proceeded without bases.

Chemistry Letters published new progress about Alkenes, nitro Role: RCT (Reactant), RACT (Reactant or Reagent). 38487-85-3 belongs to class nitriles-buliding-blocks, and the molecular formula is C8H8N2O, SDS of cas: 38487-85-3.

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

Cai, Yue-Ming; Zhang, Xin; An, Cui; Yang, Ye-Fei; Liu, Wei; Gao, Wen-Xia; Huang, Xiao-Bo; Zhou, Yun-Bing; Liu, Miao-Chang; Wu, Hua-Yue published the artcile< Catalyst-free oxidative N-N coupling for the synthesis of 1,2,3-triazole compounds with tBuONO>, Reference of 38487-85-3, the main research area is benzotriazinone preparation; aminobenzamide coupling; benzothiadiazole preparation; aminothiol N S coupling; triazolopyridine preparation; pyridinyl methanamine coupling.

A catalyst-free method was developed to synthesize 1,2,3-benzotriazinones I [R = H, 6-Cl, 6-Br, etc.] and 1,2,3-benzothiadiazoles II [R1 = H, 6-Cl, 6-Br, etc.] from 2-amino-benzamides and 2-amino thiols. Of particular note was that the one-step synthesis route to access [1,2,3]triazolo[1,5-a]pyridines III [R2 = H, Ph, 4-ClC6H4; R3 = H, 7-Me, 7-Br] from pyridin-2-ylmethanamine was reported for the first time. This approach featured no use of catalyst, extremely mild conditions and excellent efficiency.

Organic Chemistry Frontiers published new progress about Amino thiols Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 38487-85-3 belongs to class nitriles-buliding-blocks, and the molecular formula is C8H8N2O, Reference of 38487-85-3.

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

Melin, Lea; Gesner, Emily; Attwell, Sarah; Kharenko, Olesya A.; van der Horst, Edward H.; Hansen, Henrik C.; Gagnon, Alexandre published the artcile< Design and Synthesis of LM146, a Potent Inhibitor of PB1 with an Improved Selectivity Profile over SMARCA2>, COA of Formula: C8H8N2O, the main research area is LM146 quinazolin synthesis anticancer SAR PB1 bromodomain.

PB1 is a bromodomain-containing protein hypothesized to act as the nucleosome-recognition subunit of the PBAF complex. Although PB1 is a key component of the PBAF chromatin remodeling complex, its exact role has not been elucidated due to the lack of potent and selective inhibitors. Chem. probes that target specific bromodomains within the complex would constitute highly valuable tools to characterize the function and therapeutic pertinence of PB1 and of each of its bromodomains. Here, we report the design and synthesis of lead compound LM146, which displays strong stabilization of the second and fifth bromodomains of PB1 as shown by DSF. LM146 does not interact with bromodomains outside of sub-family VIII and binds to PB1(2), PB1(5), and SMARCA2B with KD values of 110, 61, and 2100 nM, resp., providing a ~34-fold selectivity profile for PB1(5) over SMARCA2.

ACS Omega published new progress about Antitumor agents. 38487-85-3 belongs to class nitriles-buliding-blocks, and the molecular formula is C8H8N2O, COA of Formula: C8H8N2O.

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

Hartz, Richard A.; Ahuja, Vijay T.; Nara, Susheel J.; Kumar, C. M. Vijaya; Manepalli, Raju K. V. L. P.; Sarvasiddhi, Sarat Kumar; Honkhambe, Swarnamba; Patankar, Vidya; Dasgupta, Bireshwar; Rajamani, Ramkumar; Muckelbauer, Jodi K.; Camac, Daniel M.; Ghosh, Kaushik; Pokross, Matthew; Kiefer, Susan E.; Brown, Jeffrey M.; Hunihan, Lisa; Gulianello, Michael; Lewis, Martin; Lippy, Jonathan S.; Surti, Neha; Hamman, Brian D.; Allen, Jason; Kostich, Walter A.; Bronson, Joanne J.; Macor, John E.; Dzierba, Carolyn D. published the artcile< Bicyclic Heterocyclic Replacement of an Aryl Amide Leading to Potent and Kinase-Selective Adaptor Protein 2-Associated Kinase 1 Inhibitors>, SDS of cas: 38487-85-3, the main research area is quinazoline quinoline preparation analgesic AAK1 inhibitor.

Investigation of the structure-activity relationships (SARs) of substituents on the resultant quinazoline and quinoline ring systems led to the identification of (S)- I =[R1 = CN, R2 = H], a brain-penetrant, AAK1-selective inhibitor with improved enzyme and cellular potency. The synthesis, SAR, and in vivo evaluation of a series of quinazoline and quinoline-based AAK1 inhibitors were described herein.

Journal of Medicinal Chemistry published new progress about Analgesics. 38487-85-3 belongs to class nitriles-buliding-blocks, and the molecular formula is C8H8N2O, SDS of cas: 38487-85-3.

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts