Tag: M.W=150-200

Sengmany, Stephane published the artcileSelective mono-amination of dichlorodiazines, Recommanded Product: 4-(6-Chloropyridazin-3-yl)morpholine, the main research area is amino chloro pyridazine pyrimidine chemoselective preparation; chemoselective monosubstitution dichloropyridazine dichloropyrimidine amine triethylamine ethanol; kinetics relative reactivity chemoselective monosubstitution dichloropyridazine dichloropyrimidine morpholine.

3,6-Dichloropyridazine, 4,6-dichloropyrimidine, 2,4-dichloropyrimidine, and 3,5-dichloropyridazine underwent chemoselective monosubstitution reactions with amines using triethylamine as a base in ethanol at either ambient temperature or reflux to give monoamino monochloro pyridazines and pyrimidines. The methodol. is general and efficient despite noticeable differences in reactivity between diazines; while dichloropyridazine and dichloropyrazine require several hours of heating at reflux for the reaction to proceed, dichloropyrimidines reach completion within minutes at room temperature

Tetrahedron published new progress about Amines Role: RCT (Reactant), RACT (Reactant or Reagent). 17259-32-4 belongs to class pyridazine, name is 4-(6-Chloropyridazin-3-yl)morpholine, and the molecular formula is C8H10ClN3O, Recommanded Product: 4-(6-Chloropyridazin-3-yl)morpholine.

Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

Sengmany, Stephane published the artcileAn electrochemical nickel-catalyzed arylation of 3-amino-6-chloropyridazines, Recommanded Product: 4-(6-Chloropyridazin-3-yl)morpholine, the main research area is arylaminopyridazine derivative electrochem preparation; aryl halide aminochloropyridazine electrochem arylation nickel catalyst.

3-Amino-6-aryl- and 3-amino-6-heteroarylpyridazines have been obtained in generally good yield using a nickel-catalyzed electrochem. cross-coupling between 3-amino-6-chloropyridazines and aryl or heteroaryl halides at room temperature Comparative experiments involving classical palladium-catalyzed reactions, such as Suzuki, Stille, or Negishi cross-couplings, reveal that the electrochem. method can constitute a reliable alternative tool for biaryl formation. A possible reaction mechanism is proposed on the basis of electrochem. analyses.

Journal of Organic Chemistry published new progress about Aryl halides Role: RCT (Reactant), RACT (Reactant or Reagent). 17259-32-4 belongs to class pyridazine, name is 4-(6-Chloropyridazin-3-yl)morpholine, and the molecular formula is C8H10ClN3O, Recommanded Product: 4-(6-Chloropyridazin-3-yl)morpholine.

Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

Ibrahim, Tamer H. published the artcileSynthesis of Some Novel 2,6-Disubstituted Pyridazin-3(2H)-one Derivatives as Analgesic, Anti-Inflammatory, and Non-Ulcerogenic Agents, Formula: C6H8ClN3, the main research area is alkyl phenoxypyridazinone preparation analgesic antiinflammatory ulcerogenic cyclooxygenase inhibitor SAR; benzyl aminopyridazinone preparation analgesic antiinflammatory ulcerogenic cyclooxygenase inhibitor SAR; aralkyl pyrazolylpyridazinone preparation analgesic antiinflammatory ulcerogenic cyclooxygenase inhibitor SAR; Analgesic activity; Anti-inflammatory; COX-1; COX-2; Pyridazinone.

Some novel 2,6-disubstituted pyridazine-3(2H)-one derivatives I [R1 = p-tolyl, benzyl, 2,6-di-MeC6H3, etc; R2 = Et, Ph, 4-Br-C6H4, phthalimido; X = N, O] and II [R3 = Ph, 4-Br-C6H4, phthalimido] were synthesized and evaluated for in-vitro cyclooxygenase-2 (COX-2) inhibitory efficacy. Compounds I [R1 = o-tolyl, R2 = phthalimido, X = O; R1 = o-tolyl, R2 = Et, X = O] and II [R3 = Ph] showed the most potent COX-2 inhibitory activity with IC50 values of 0.19, 0.11, and 0.24 μM, resp. The synthesized compounds with the highest COX-2 selectivity indexes were evaluated for their anti-inflammatory, analgesic, and ulcerogenic activities. Compounds I [R1 = o-tolyl, R2 = Et, X = O] and II [R3 = Ph] demonstrated the most potent and consistent anti-inflammatory activity over the synthesized compounds, which was significantly higher than that of celecoxib in the carrageenin rat paw edema model and with milder ulcer scoring than that of indomethacin in the ulcerogenicity screening.

Archiv der Pharmazie (Weinheim, Germany) published new progress about Analgesics. 7145-60-0 belongs to class pyridazine, name is 6-Chloro-N,N-dimethylpyridazin-3-amine, and the molecular formula is C6H8ClN3, Formula: C6H8ClN3.

Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

Moriya, Koichi; Shibuya, Katsuhiko; Hattori, Yumi; Tsuboi, Shinichi; Shiokawa, Kozo; Kagabu, Shinzo published the artcile< 1-Diazinylmethyl-2-nitromethylene- and 2-nitroimino-imidazolidines as new potential insecticides>, Reference of 120276-59-7, the main research area is insecticide diazinylmethyl nitromethylene imidazolidine; nitroiminoimidazolidine insecticide structure activity.

The insecticidal properties of diazinylmethylimidazolidines and compared them with the corresponding Ph and pyridyl homologs. Me group and chlorine atom were selected as ring substituents to simplify the comparison. The bioassay was carried out using green rice leafhoppers as test species.

Journal of Pesticide Science (International Edition) published new progress about Insecticides. 120276-59-7 belongs to class pyridazine, and the molecular formula is C5H4Cl2N2, Reference of 120276-59-7.

Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

Russell, Michael G. N.; Carling, Robert W.; Atack, John R.; Bromidge, Frances A.; Cook, Susan M.; Hunt, Peter; Isted, Catherine; Lucas, Matt; McKernan, Ruth M.; Mitchinson, Andrew; Moore, Kevin W.; Narquizian, Robert; Macaulay, Alison J.; Thomas, David; Thompson, Sally-Anne; Wafford, Keith A.; Castro, Jose L. published the artcile< Discovery of Functionally Selective 7,8,9,10-Tetrahydro-7,10-ethano-1,2,4-triazolo[3,4-a]phthalazines as GABAA Receptor Agonists at the α3 Subunit>, Formula: C5H4Cl2N2, the main research area is triazolophthalazine tetrahydroethano preparation human GABA receptor agonist acidity.

7,8,9,10-Tetrahydro-7,10-ethano-1,2,4-triazolo[3,4-a]phthalazine I (R1 = Ph; R2 = 2-pyridylmethyl) was previously identified as a potent partial agonist for the α3 receptor subtype with 5-fold selectivity in binding affinity over α1. This paper describes a detailed investigation of the substituents on this core structure at both the 3- and 6-positions. Despite evaluating a wide range of groups, the maximum selectivity that could be achieved in terms of affinity for the α3 subtype over the α1 subtype was 12-fold (for I [R1 = Ph; R2 = 4-(HOCH2)C6H4CH2]). Although most analogs showed no selectivity in terms of efficacy, some of them, e.g. I (R1 = Ph; R2 = 3,5-dimethyl-2-pyridylmethyl, pyrazol-1-ylmethyl), did show partial agonism at α1 and antagonism at α3. However, two analogs I (R1 = Ph; R2 = 1-methyl-1,2,4-triazol-3-ylmethyl, 2-propyl-1,2,4-triazol-3-ylmethyl), containing triazole substituents in the 6-position, showed significantly higher efficacy for the α3 subtype over the α1 subtype. This was the first indication that selectivity in efficacy in the required direction could be achieved in this series.

Journal of Medicinal Chemistry published new progress about Acidity. 120276-59-7 belongs to class pyridazine, and the molecular formula is C5H4Cl2N2, Formula: C5H4Cl2N2.

Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

Moriya, Koichi; Shibuya, Katsuhiko; Hattori, Yumi; Tsuboi, Shinichi; Shiokawa, Kozo; Kagabu, Shinzo published the artcile< Imidacloprid and analogous insecticides. IV. 1-Diazinylmethyl-2-nitromethylene- and 2-nitroimino-imidazolidines as new potential insecticides>, Synthetic Route of 120276-59-7, the main research area is diazinylmethyl imidazolidine insecticide.

Eight 1-diazinylmethylimidazolidines were prepared and their insecticidal activities were studied. 1-(2-Chloro-5-pyrimidinyl)methyl-2-(nitroimino)imidazolidine (I) was as effective as imidacloprid against green rice leafhoppers on rice seedlings in spray applications. Seven 1-(diazinylmethyl)-2-(nitromethylene)imidazolidines with or without a Cl or Me substituent on the diazine ring were less effective than I.

Nippon Noyaku Gakkaishi published new progress about Insecticides. 120276-59-7 belongs to class pyridazine, and the molecular formula is C5H4Cl2N2, Synthetic Route of 120276-59-7.

Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

Leivers, Martin; Miller, John F.; Chan, Stephanie A.; Lauchli, Ryan; Liehr, Sebastian; Mo, Wenyan; Ton, Tony; Turner, Elizabeth M.; Youngman, Michael; Falls, J. Greg; Long, Susan; Mathis, Amanda; Walker, Jill published the artcile< Imidazopyridazine Hepatitis C Virus Polymerase Inhibitors. Structure-Activity Relationship Studies and the Discovery of a Novel, Traceless Prodrug Mechanism>, Safety of 3-Chloro-6-(chloromethyl)pyridazine, the main research area is imidazopyridazine hepatitis C antiviral polymerase structure activity preparation.

By reducing the basicity of the core heterocycle in a series of HCV NS5B inhibitors, the hERG liability was reduced. The SAR was then systematically explored to increase solubility and enable dose escalation while retaining potency. During this exploration, a facile decarboxylation was noted and was exploited as a novel prodrug mechanism. The synthesis and characterization of these prodrugs and their utilization in chronic toxicity studies are presented.

Journal of Medicinal Chemistry published new progress about Antiviral agents. 120276-59-7 belongs to class pyridazine, and the molecular formula is C5H4Cl2N2, Safety of 3-Chloro-6-(chloromethyl)pyridazine.

Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

Liu, Yu-Xiu; Wei, Deng-Guo; Zhu, Ye-Rong; Liu, Shao-Hua; Zhang, Yong-Lin; Zhao, Qi-Qi; Cai, Bao-Li; Li, Yong-Hong; Song, Hai-Bin; Liu, Ying; Wang, Yong; Huang, Run-Qiu; Wang, Qing-Min published the artcile< Synthesis, Herbicidal Activities, and 3D-QSAR of 2-Cyanoacrylates Containing Aromatic Methylamine Moieties>, Electric Literature of 120276-59-7, the main research area is hetarylmethylaminoacrylate cyano preparation herbicidal; aminoacrylate cyano preparation herbicidal; arylmethylaminoacrylate cyano preparation herbicidal; cyanoacrylate aromatic methylamine preparation herbicidal.

A series of novel 2-cyanoacrylates containing different aromatic rings, e.g. I (R = MeS, Et, Me2CH; R1 = 4-ClC6H4, 6-bromo-3-pyridinyl, 2-ethoxy-5-thiazolyl, etc) were prepared, and their structures were characterized by 1H NMR, elemental anal., and single-crystal X-ray diffraction anal. Their herbicidal activities against four weeds and inhibition of photosynthetic electron transport against isolated chloroplasts (the Hill reaction) were evaluated. Both in vivo and in vitro data showed that the compounds containing benzene, pyridine, and thiazole moieties gave higher activities than those containing pyrimidine, pyridazine, furan, and THF moieties. To further explore the comprehensive structure-activity relationship on the basis of in vitro data, comparative mol. field anal. (CoMFA) was performed, and the results showed that a bulky and electroneg. group around the para-position of the aromatic rings would have the potential for higher activity, which offered important structural insights into designing highly active compounds prior to the next synthesis.

Journal of Agricultural and Food Chemistry published new progress about Herbicides. 120276-59-7 belongs to class pyridazine, and the molecular formula is C5H4Cl2N2, Electric Literature of 120276-59-7.

Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem

Russell, Michael G. N.; Carling, Robert W.; Atack, John R.; Bromidge, Frances A.; Cook, Susan M.; Hunt, Peter; Isted, Catherine; Lucas, Matt; McKernan, Ruth M.; Mitchinson, Andrew; Moore, Kevin W.; Narquizian, Robert; Macaulay, Alison J.; Thomas, David; Thompson, Sally-Anne; Wafford, Keith A.; Castro, Jose L. published the artcile< Discovery of Functionally Selective 7,8,9,10-Tetrahydro-7,10-ethano-1,2,4-triazolo[3,4-a]phthalazines as GABAA Receptor Agonists at the α3 Subunit>, COA of Formula: C5H4Cl2N2, the main research area is triazolophthalazine tetrahydroethano preparation human GABA receptor agonist acidity.

7,8,9,10-Tetrahydro-7,10-ethano-1,2,4-triazolo[3,4-a]phthalazine I (R1 = Ph; R2 = 2-pyridylmethyl) was previously identified as a potent partial agonist for the α3 receptor subtype with 5-fold selectivity in binding affinity over α1. This paper describes a detailed investigation of the substituents on this core structure at both the 3- and 6-positions. Despite evaluating a wide range of groups, the maximum selectivity that could be achieved in terms of affinity for the α3 subtype over the α1 subtype was 12-fold (for I [R1 = Ph; R2 = 4-(HOCH2)C6H4CH2]). Although most analogs showed no selectivity in terms of efficacy, some of them, e.g. I (R1 = Ph; R2 = 3,5-dimethyl-2-pyridylmethyl, pyrazol-1-ylmethyl), did show partial agonism at α1 and antagonism at α3. However, two analogs I (R1 = Ph; R2 = 1-methyl-1,2,4-triazol-3-ylmethyl, 2-propyl-1,2,4-triazol-3-ylmethyl), containing triazole substituents in the 6-position, showed significantly higher efficacy for the α3 subtype over the α1 subtype. This was the first indication that selectivity in efficacy in the required direction could be achieved in this series.

Journal of Medicinal Chemistrypublished new progress about Acidity. 120276-59-7 belongs to class pyridazine, and the molecular formula is C5H4Cl2N2, COA of Formula: C5H4Cl2N2.

Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem