Month: October 2022

Bhattacharyya, Bhaswati; Dhara, Kaliprasanna published the artcile< Highly efficient, mild, one pot synthesis of 2-substituted benzimidazoles, benzothiazoles and pyridoimidazoles promoted by N-iodosuccinimide>, Related Products of 197638-83-8, the main research area is benzimidazole benzothiazole imidazopyridine preparation.

A common and highly efficient metal-free route for the synthesis of 2-substituted benzimidazoles, benzothiazoles and pyridoimidazoles from suitable 1,2- functionalized aromatic compounds and various aromatic and aliphatic aldehydes and ferrocenecarboxaldehyde was developed using 1-iodo-2,5-pyrrolidinedione, (N-iodosuccinimide) as the oxidizing agent. The methodol. involved very short reaction time, mild reaction procedure and easy work-up as well as excellent yields of the products. The synthesis of the target compounds was achieved by a reaction of 1,2-benzenediamine, 2-aminobenzenethiol, 2,3-pyridinediamine with aldehydes, such as benzaldehyde derivatives, 4-formylbenzonitrile, 1,3-benzodioxole-5-carboxaldehyde, citronellal, (formyl)ferrocene. The title compounds thus formed included 2-phenyl-1H-benzimidazole, 2-phenylbenzothiazole, (4-methyl-1H-benzimidazol-2-yl)ferrocene, 2-phenyl-3H-imidazo[4,5-b]pyridine derivatives

Journal of the Indian Chemical Society published new progress about Aliphatic aldehydes Role: RCT (Reactant), RACT (Reactant or Reagent). 197638-83-8 belongs to class piperazines, and the molecular formula is C16H22N2O3, Related Products of 197638-83-8.

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Eddie, Sharon L.; Gregson, Aaron; Graham, Emma; Burton, Stephanie; Harrison, Timothy; Burden, Roberta; Scott, Christopher J.; Mullan, Paul B.; Williams, Rich published the artcile< Identification and SAR exploration of a novel series of Legumain inhibitors>, Name: 4-(4-Methyl-1-piperazinyl)phenylboronic Acid, the main research area is Legumain mall mol inhibitor SAR dipeptide; Legumain; SAR; Small molecule inhibitor.

This letter describes the development of a series of potent and selective small mol. Legumain inhibitors suitable as chem. probes for in vitro experiments Our previous research had identified a dipeptide inhibitor utilizing a semi-reversible cyano warhead that generated 2, a cell active inhibitor. This work explores an alternative P2-P3 linker and further SAR exploration of the P3 group which led to the identification of 16i, a highly potent inhibitor with excellent physiochem. properties.

Bioorganic & Medicinal Chemistry Letters published new progress about Dipeptides Role: BSU (Biological Study, Unclassified), BIOL (Biological Study) (dipeptide Legumain inhibitors). 229009-40-9 belongs to class piperazines, and the molecular formula is C11H17BN2O2, Name: 4-(4-Methyl-1-piperazinyl)phenylboronic Acid.

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Nishiguchi, Gisele A.; Atallah, Gordana; Bellamacina, Cornelia; Burger, Matthew T.; Ding, Yu; Feucht, Paul H.; Garcia, Pablo D.; Han, Woo-Seok; Klivansky, Liana; Lindvall, Mika published the artcile< Discovery of novel 3,5-disubstituted indole derivatives as potent inhibitors of Pim-1, Pim-2, and Pim-3 protein kinases>, Recommanded Product: 1-Boc-4-(4-Formylphenyl)piperazine, the main research area is indole pyrazolopyridine derivative preparation SAR Pim kinase inhibitory.

A series of novel 3,5-disubstituted indole e. g., I and pyrazolopyridine e. g., II derivatives as potent and selective inhibitors of all three members of the Pim kinase family is described. High throughput screen identified a pan-Pim kinase inhibitor with a promiscuous scaffold. Guided by structure-based drug design, SAR of the series afforded a highly selective indole chemotype that was further developed into a potent set of compounds against Pim-1, 2, and 3 (Pim-1 and Pim-3: IC50 ≤ 2 nM and Pim-2: IC50 ≤ 100 nM).

Bioorganic & Medicinal Chemistry Letters published new progress about Alcohols Role: RCT (Reactant), RACT (Reactant or Reagent). 197638-83-8 belongs to class piperazines, and the molecular formula is C16H22N2O3, Recommanded Product: 1-Boc-4-(4-Formylphenyl)piperazine.

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Scott, James S.; Birch, Alan M.; Brocklehurst, Katy J.; Broo, Anders; Brown, Hayley S.; Butlin, Roger J.; Clarke, David S.; Davidsson, Ojvind; Ertan, Anne; Goldberg, Kristin; Groombridge, Sam D.; Hudson, Julian A.; Laber, David; Leach, Andrew G.; MacFaul, Philip A.; McKerrecher, Darren; Pickup, Adrian; Schofield, Paul; Svensson, Per H.; Sorme, Pernilla; Teague, Joanne published the artcile< Use of Small-Molecule Crystal Structures To Address Solubility in a Novel Series of G Protein Coupled Receptor 119 Agonists: Optimization of a Lead and in Vivo Evaluation>, Recommanded Product: tert-Butyl 4-(5-bromopyrimidin-2-yl)piperazine-1-carboxylate, the main research area is antidiabetic GPCR119 agonist preparation structure activity crystal structure.

G protein coupled receptor 119 (GPR119) is viewed as an attractive target for the treatment of type 2 diabetes and other elements of the metabolic syndrome. During a program toward discovering agonists of GPR119, we herein describe optimization of an initial lead compound, 2, into a development candidate, 42. A key challenge in this program of work was the insolubility of the lead compound Small-mol. crystallog. was utilized to understand the intermol. interactions in the solid state and resulted in a switch from an aryl sulfone to a 3-cyanopyridyl motif. The compound was shown to be effective in wild-type but not knockout animals, confirming that the biol. effects were due to GPR119 agonism.

Journal of Medicinal Chemistry published new progress about 5-HT2B receptors Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 374930-88-8 belongs to class piperazines, and the molecular formula is C13H19BrN4O2, Recommanded Product: tert-Butyl 4-(5-bromopyrimidin-2-yl)piperazine-1-carboxylate.

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Dong, Zhe; MacMillan, David W. C. published the artcile< Metallaphotoredox-enabled deoxygenative arylation of alcohols>, Quality Control of 374930-88-8, the main research area is alc aryl halide deoxygenative arylation metallaphotoredox.

Metal-catalyzed cross-couplings are a mainstay of organic synthesis and are widely used for the formation of C-C bonds, particularly in the production of unsaturated scaffolds1. However, alkyl cross-couplings using native sp3-hybridized functional groups such as alcs. remain relatively underdeveloped2. In particular, a robust and general method for the direct deoxygenative coupling of alcs. would have major implications for the field of organic synthesis. A general method for the direct deoxygenative cross-coupling of free alcs. must overcome several challenges, most notably the in situ cleavage of strong C-O bonds3, but would allow access to the vast collection of com. available, structurally diverse alcs. as coupling partners4. Authors report herein a metallaphotoredox-based cross-coupling platform in which free alcs. are activated in situ by N-heterocyclic carbene salts for carbon-carbon bond formation with aryl halide coupling partners. This method is mild, robust, selective and most importantly, capable of accommodating a wide range of primary, secondary and tertiary alcs. as well as pharmaceutically relevant aryl and heteroaryl bromides and chlorides. The power of the transformation has been demonstrated in a number of complex settings, including the late-stage functionalization of Taxol and a modular synthesis of Januvia, an antidiabetic medication. This technol. represents a general strategy for the merger of in situ alc. activation with transition metal catalysis.

Nature (London, United Kingdom) published new progress about Alcohols Role: RCT (Reactant), RACT (Reactant or Reagent). 374930-88-8 belongs to class piperazines, and the molecular formula is C13H19BrN4O2, Quality Control of 374930-88-8.

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Knippel, James Levi; Ye, Yuxuan; Buchwald, Stephen L. published the artcile< Enantioselective C2-Allylation of Benzimidazoles Using 1,3-Diene Pronucleophiles>, Product Details of C16H22N2O3, the main research area is benzimidazole aryl alkadiene copper catalyst enantioselective regioselective allylation; aryl alkenylbenzimidazole preparation.

Previously, several enantioselective allylation reactions of benzimidazoles were reported that functionalize the nucleophilic nitrogen atom. To the reversal of this inherent selectivity, N-allylation by using electrophilic N-OPiv benzimidazoles with readily available 1,3-dienes as nucleophile precursors were described. CuH-catalyzed approach utilized mild reaction conditions, exhibited broad functional-group compatibility and exclusively formed the C2-allylated product with excellent stereoselectivity.

Organic Letters published new progress about 1,3-Alkadienes Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 197638-83-8 belongs to class piperazines, and the molecular formula is C16H22N2O3, Product Details of C16H22N2O3.

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Robke, Lucas; Rodrigues, Tiago; Schroeder, Peter; Foley, Daniel J.; Bernardes, Goncalo J. L.; Laraia, Luca; Waldmann, Herbert published the artcile< Discovery of 2,4-dimethoxypyridines as novel autophagy inhibitors>, Recommanded Product: 1-Boc-4-(4-Formylphenyl)piperazine, the main research area is dimethoxy pyridine derivative preparation autophagy inhibitor structure.

Autophagy is a catabolic process, which mediates degradation of cellular components and has important roles in health and disease. Therefore, small mol. modulators of autophagy are in great demand. Herein, we describe a phenotypic high-content screen for autophagy inhibitors, which led to the discovery of a dimethoxypyridine-based class of autophagy inhibitors, which derive from previously reported, natural product-inspired MAP4K4 inhibitors. Comprehensive structure-activity relationship studies led to a potent compound, and biol. validation experiments indicated that the mode of action was upstream or independent of mTOR.

Tetrahedron published new progress about Apoptosis. 197638-83-8 belongs to class piperazines, and the molecular formula is C16H22N2O3, Recommanded Product: 1-Boc-4-(4-Formylphenyl)piperazine.

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Yang, Yang; Mustard, Thomas J. L.; Cheong, Paul Ha-Yeon; Buchwald, Stephen L. published the artcile< Palladium-Catalyzed Completely Linear-Selective Negishi Cross-Coupling of Allylzinc Halides with Aryl and Vinyl Electrophiles>, Application In Synthesis of 374930-88-8, the main research area is Negishi coupling allyl zinc aryl vinyl halide prenyl group; cross-coupling; heterocycles; organozinc reagents; palladium; prenylation.

A linear-selective Negishi coupling reaction was developed and the synthesis of the target compounds was achieved by a reaction of (allyl)zinc reagents [i.e., (prenyl)zinc bromide, (farnesyl)zinc, etc.] with aryl halides, heteroaryl halides, vinyl halides. The reaction features mild reaction conditions and a broad reactant scope with respect to aryl halides and vinyl halides and (allyl)zinc coupling components. Under optimized reaction conditions [2′-(amino-κN)[1,1′-biphenyl]-2-yl-κC][2′-(dicyclohexylphosphino-κP)-N2,N2,N6,N6-tetramethyl[1,1′-biphenyl]-2,6-diamine](methanesulfonate-κO)palladium was used as a catalyst. This synthetic approach was applied to the preparation of 6-methyl-3-(3-methyl-2-buten-1-yl)-9H-carbazol-2-ol (siamenol).

Angewandte Chemie, International Edition published new progress about Allylic compounds Role: RCT (Reactant), RACT (Reactant or Reagent) ((alkenyl)zinc compounds). 374930-88-8 belongs to class piperazines, and the molecular formula is C13H19BrN4O2, Application In Synthesis of 374930-88-8.

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Rindhe, S. S.; Karale, B. K.; Gupta, R. C.; Rode, M. A. published the artcile< Synthesis, antimicrobial and antioxidant activity of some oxindoles>, Name: 1-Boc-4-(4-Formylphenyl)piperazine, the main research area is oxindole preparation antibacterial antifungal antioxidant agent; Antibacterial; antifungal and antioxidant activity; oxindole.

The present work describes the synthesis and spectral anal. of several (3Z)-[4-[4-(arylsulfonyl)-1-piperazinyl]benzylidene]-1,3-dihydro-2H-indol-2-one derivatives The title compounds were screened in-vitro against six species of microorganisms, Staphylococcus aureus, Streptococcus pyogenes, Escherichia coli, Pseudomonas aeruginosa, Aspergillus niger and Aspergillus clavatus. Most of the compounds exhibited significant antimicrobial activity. All compounds were also screened in-vitro for the antioxidant activity using DPPH assay. Most of them have shown very significant antioxidant activity. The synthesis of the target compounds was achieved by an amidation (sulfonamidation) of 4-[4-[(2-oxo-3-indolylidene)methylene]phenyl]-1-piperazinecarboxylic acid 1,1-dimethylethyl ester with sulfonyl halides. The title compounds thus formed included 1,3-dihydro-3-[(3Z)-[4-[4-[[4-(1-methylethyl)phenyl]sulfonyl]-1-piperazinyl]phenyl]methylene]-2H-indol-2-one (I).

Indian Journal of Pharmaceutical Sciences published new progress about Antibacterial agents. 197638-83-8 belongs to class piperazines, and the molecular formula is C16H22N2O3, Name: 1-Boc-4-(4-Formylphenyl)piperazine.

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Kim, Juhyeon; Kim, Yoon Jung; Londhe, Ashwini M.; Pae, Ae Nim; Choo, Hyunah; Kim, Hak Joong; Min, Sun-Joon published the artcile< Synthesis and biological evaluation of disubstituted pyrimidines as selective 5-HT2C agonists>, Application In Synthesis of 374930-88-8, the main research area is pyrimidine preparation antagonist HT receptor; 5-HT2C receptor; binding affinity; cell-based assay; disubstituted pyrimidine; selectivity.

The synthesis of disubstituted pyrimidine derivatives I [R1 = 3-F, 4-F; n = 0, 1, 2; R2 = piperazin-1-yl, (2R)-2-methylpiperazin-1-yl, 1,4-diazepan-1-yl], II [R3 = (2R)-2-(3-fluorophenyl)propyl, (2R)-2-(4-fluorophenyl)propyl, 3-fluorophenyl, 4-fluorophenyl; R4 = 1,4-diazepan-1-yl, [(3R)-pyrrolidin-3-yl]aminyl, 2,7-diazaspiro[4.4]nonan-2-yl, etc.] and their biol. evaluation as selective 5-HT2C agonists were described. To improve selectivity for 5-HT2C over other subtypes, two series of disubstituted pyrimidines with fluorophenylalkoxy groups at either the 5-position or 4-position and varying cyclic amines at the 2-position were synthesized. The in vitro cell-based assay and binding assay identified compounds II [R3 = (2R)-2-(3-fluorophenyl)propyl, R4 = 1,4-diazepan-1-yl (I); R3 = (2R)-2-(4-fluorophenyl)propyl, R4 = 1,4-diazepan-1-yl] as potent 5-HT2C agonists. Further studies on selectivity to 5-HT subtypes and drug-like properties indicated that 2,4-disubstituted pyrimidine (I) showed a highly agonistic effect on the 5-HT2C receptor, with excellent selectivity, as well as exceptional drug-like properties, including high plasma and microsomal stability, along with low CYP inhibition. Thus, pyrimidine (I) could be considered a viable lead compound as a 5-HT2C selective agonist.

Molecules published new progress about 5-HT receptors Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 374930-88-8 belongs to class piperazines, and the molecular formula is C13H19BrN4O2, Application In Synthesis of 374930-88-8.

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics