Tag: M.W=150-200

Xu, Jun; Yang, Tianjiao; Wang, Jiayi; Song, Gonghua published the artcile< Multistep Synthesis and Nematicidal Activity of 2-(8-azabicyclo[3.2.1]octan-3-yl)-3-imino-2,3-dihydro-1H-isoindol-1-One Derivatives>, Computed Properties of 611-19-8, the main research area is azabicyclooctanyl iminoisoindolone preparation nematicidal SAR.

Novel 2-(8-azabicyclo[3.2.1]octan-3-yl)-3-imino-2,3-dihydro-1H-isoindol-1-ones I [R = H, 5-F, 6-MeO, 5-Cl; R1 = Me, benzyl, 4-chlorobenzyl, etc.; R2 = tert-Bu, cyclohexyl, 2-MeOC6H4, etc.] which derived from 5-HT3 receptor antagonists hexahydroazepinylbenzamides were designed and synthesized through isocyanide insertion reaction. All target compounds I were evaluated against pinewood nematodes B. xylophilus and root-knot nematodes M. incognita. Good lethal rate (75%) for I [R = 5-Cl, R1= Me, R2 = tert-butyl] and serious nervous curl effect against pinewood nematodes B. xylophilus for I [R = H, R1= Me, R2 = tert-butyl] were observed at 10 mg/l. The inhibition activities of I [R = H, R1= Me, R2 = 2-MeOC6H4, etc.] against root-knot nematodes M. incognita were 84% at 160 mg/l and 60% at 20 mg/l for in-vitro test and test tube test, resp.

Chemistry of Heterocyclic Compounds (New York, NY, United States) published new progress about Azabicyclic compounds Role: AGR (Agricultural Use), BSU (Biological Study, Unclassified), RCT (Reactant), SPN (Synthetic Preparation), BIOL (Biological Study), USES (Uses), RACT (Reactant or Reagent), PREP (Preparation). 611-19-8 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H6Cl2, Computed Properties of 611-19-8.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Zeng, Miao; Xue, Jing-Wen; Jiang, Hongwu; Li, Kaiwen; Chen, Yunong; Chen, Zhuqi; Yin, Guochuan published the artcile< Decarboxylative Addition of Propiolic Acids with Indoles to Synthesize Bis(indolyl)methane Derivatives with a Pd(II)/LA Catalyst>, Product Details of C9H5ClO2, the main research area is bisindolylmethane preparation; propiolic acid indole decarboxylative addition palladium Lewis catalyst.

The present work introduces a Pd(II)/LA-catalyzed (LA: Lewis acid) decarboxylative addition reaction for the synthesis of bis(indolyl)methane derivatives The presence of Lewis acid such as Sc(OTf)3 triggered Pd(II)-catalyzed decarboxylative addition of propiolic acids with indoles to offer the bis(indolyl)methane derivatives in moderate to good yields, whereas neither Pd(II) nor Lewis acid alone was active for this synthesis. The catalytic efficiency of Pd(OAc)2 was highly dependent on the Lewis acidity of the added Lewis acid, i.e., a stronger Lewis acid provided a higher yield of the bis(indolyl)methane derivatives Meanwhile, this Pd(II)/LA-catalyzed decarboxylative addition reaction showed good tolerance toward versatile electron-rich or -deficient substituents on the indole skeleton and on the benzyl ring of propiolic acids. The studies on the in situ 1H NMR kinetics of this Pd(II)/Sc(III) catalysis disclosed the formation of a transient vinyl-Pd(II)/Sc(III) intermediate generated by the pyrrole addition to the alkynyl-Pd(II)/Sc(III) species after decarboxylation, which was scarcely observed before.

Journal of Organic Chemistry published new progress about Addition reaction (decarboxylative). 3240-10-6 belongs to class chlorides-buliding-blocks, and the molecular formula is C9H5ClO2, Product Details of C9H5ClO2.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Gunia-Krzyzak, Agnieszka; Zeslawska, Ewa; Sloczynska, Karolina; Zelaszczyk, Dorota; Sowa, Aleksandra; Koczurkiewicz-Adamczyk, Paulina; Ol, Justyna Popi; Nitek, Wojciech; Pekala, Elzbieta; Marona, Henryk published the artcile< S(+)-(2E)-N-(2-Hydroxypropyl)-3-Phenylprop-2-Enamide (KM-568): a novel cinnamamide derivative with anticonvulsant activity in animal models of seizures and epilepsy>, SDS of cas: 17082-09-6, the main research area is cinnamamide derivative anticonvulsant epilepsy seizure neurotoxicity mutagenicity; anticonvulsant; antiseizure, cinnamamide derivatives; crystallography; drug development; epilepsy; preclinical safety evaluation.

Epilepsy is one of the most frequent neurol. disorders affecting about 1% of the world’s human population. Despite availability of multiple treatment options including antiseizure drugs, it is estimated that about 30% of seizures still remain resistant to pharmacotherapy. Searching for new antiseizure and antiepileptic agents constitutes an important issue within modern medicinal chem. Cinnamamide derivatives were identified in preclin. as well as clin. studies as important drug candidates for the treatment of epilepsy. The cinnamamide derivative presented here: S(+)-(2E)-N-(2-hydroxypropyl)-3-phenylprop-2-enamide (S(+)-N-(2-hydroxypropyl)cinnamamide, compound KM-568) showed anticonvulsant activity in several models of epilepsy and seizures in mice and rats. It was active in genetic animal model of epilepsy (Frings audiogenic seizure-susceptible mouse model, ED50=13.21 mg/kg, i.p.), acute seizures induced elec. (max electroshock test ED50=44.46 mg/kg mice i.p., ED50=86.6 mg/kg mice p.o., ED50=27.58 mg/kg rats i.p., ED50=30.81 mg/kg rats p.o., 6-Hz psychomotor seizure model 32mA ED50=71.55 mg/kg mice i.p., 44 mA ED50=114.4 mg/kg mice i.p.). Chronic seizures induced elec. (corneal kindled mouse model ED50=79.17 mg/kg i.p., hippocampal kindled rat model ED50=24.21 mg/kg i.p., lamotrigine-resistant amygdala kindled seizure model in rats ED50=58.59 mg/kg i.p.), acute seizures induced chem. (s.c. metrazol seizure threshold test ED50=104.29 mg/kg mice i.p., ED50=107.27 mg/kg mice p.o., ED50=41.72 mg/kg rats i.p., seizures induced by picrotoxin in mice ED50=94.11 mg/kg i.p.) and pilocarpine-induced status epilepticus model in rats (ED50=279.45 mg/kg i.p., ED97=498.2 mg/kg i.p.). The chem. structure of the compound including configuration of the chiral center was confirmed by NMR spectroscopy, LC/MS spectroscopy, elemental anal., and crystallog. Compound KM-568 was identified as a moderately stable derivative in an in vitro mouse liver microsome system. According to the Ames microplate format mutagenicity assay performed, KM-568 was not a base substitution or frameshift mutagen. Cytotoxicity evaluation in two cell lines (HepG2 and H9c2) proved the safety of the compound in concentrations up to 100μM. Based on the results of anticonvulsant activity and safety profile S(+)-(2E)-N-(2-hydroxypropyl)-3-phenylprop-2-enamide could be proposed as a new lead compound for further preclin. studies on novel treatment options for epilepsy.

International Journal of Molecular Sciences published new progress about Anticonvulsants. 17082-09-6 belongs to class chlorides-buliding-blocks, and the molecular formula is C9H7ClO, SDS of cas: 17082-09-6.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Kawamata, Yu; Hayashi, Kyohei; Carlson, Ethan; Shaji, Shobin; Waldmann, Dirk; Simmons, Bryan J.; Edwards, Jacob T.; Zapf, Christoph W.; Saito, Masato; Baran, Phil S. published the artcile< Chemoselective Electrosynthesis Using Rapid Alternating Polarity>, Related Products of 118-45-6, the main research area is electrochem chemoselective reduction ketone rapid alternating polarity.

Challenges in the selective manipulation of functional groups (chemoselectivity) in organic synthesis have historically been overcome either by using reagents/catalysts that tunably interact with a substrate or through modification to shield undesired sites of reactivity (protecting groups). Although electrochem. offers precise redox control to achieve unique chemoselectivity, this approach often becomes challenging in the presence of multiple redox-active functionalities. Historically, electrosynthesis has been performed almost solely by using d.c. (DC). In contrast, applying a.c. (AC) has been known to change reaction outcomes considerably on an anal. scale but has rarely been strategically exploited for use in complex preparative organic synthesis. Here we show how a square waveform employed to deliver elec. current-rapid alternating polarity (rAP)-enables control over reaction outcomes in the chemoselective reduction of carbonyl compounds, one of the most widely used reaction manifolds. The reactivity observed cannot be recapitulated using DC electrolysis or chem. reagents. The synthetic value brought by this new method for controlling chemoselectivity is vividly demonstrated in the context of classical reactivity problems such as chiral auxiliary removal and cutting-edge medicinal chem. topics such as the synthesis of PROTACs.

Journal of the American Chemical Society published new progress about Carbonyl group. 118-45-6 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H3ClO3, Related Products of 118-45-6.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Khajehzadeh, Mostafa; Moghadam, Majid; Jamehbozorgi, Saeed published the artcile< Synthesis and characterization of a new poly(N-heterocyclic carbene Cu complex) immobilized on nano-silica, (CuII-NHCs)n@nSiO2, and its application as an efficient and reusable catalyst in the synthesis of benzimidazoles, benzothiazoles, 1,2,3-triazoles, bis-triazoles and Sonogashira-Hagihara reactions>, COA of Formula: C7H6Cl2, the main research area is benzimidazole benzothiazole triazole preparation; aryl benzyl halide aldehyde acetylene Sonogashira Hagihara reaction; poly heterocyclic carbene copper complex catalyst preparation.

The present study describes the synthesis and characterization of a new poly(N-heterocyclic carbene Cu complex) immobilized on nano silica, (CuII-NHCs)n@nSiO2. The (CuII-NHCs)n@nSiO2 dendritic polymer was characterized by FT-IR, TGA, UV-vis, FE-SEM, TEM and ICP-OES techniques. The catalytic activity of this new catalyst was studied in the synthesis of benzimidazoles I (Ar = 2-MeC6H4, 3-BrC6H4, 4-ClC6H4, etc.), benzothiazoles II, 1,2,3-triazoles III (R1 = H, 2-Br, 4-Cl, etc.), bis-triazoles and Sonogashira-Hagihara cross-coupling reactions. The (CuII-NHCs)n@nSiO2 heterogeneous catalyst showed the advantages such as high efficiency, good to excellent yield, short reaction times, easy separation and high reusability of the catalyst.

Inorganica Chimica Acta published new progress about Alkynes, aryl Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 611-19-8 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H6Cl2, COA of Formula: C7H6Cl2.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Xu, Dan; Yao, Zhengjun; Zhou, Jintang published the artcile< Mechanical and thermal properties of a novel bismaleimide matrix resin for high-performance composite materials>, Name: 5-Chloroisobenzofuran-1,3-dione, the main research area is amino polythioetherimide bismaleimidodiphenyl methane diallylbisphenol resin mech thermal property.

A novel bismaleimide matrix resin of amino-polythioetherimide (PTEI-N)/4,4′-bismaleimidodiphenyl methane (BDM)/2,2′-diallylbisphenol A (BA) was prepared Mech. measurements, dynamic thermomech. anal., thermogravimetric anal. (TGA), and microanalyses were conducted to assess the mech. properties, thermal resistance, and morphol. of the modified resin. Results demonstrate that the addition of PTEI-N has significant effects on the mech. properties of the BDM/BA system. Compared with the pure BDM/BA resin, the PTEI-N/BDM/BA system markedly improves the tensile strength, flexural strength, and impact strength, given an appropriate amount of PTEI-N. Scanning electron microscopic and energy-dispersive spectroscopic results show that PTEI-N is distributed uniformly in the BDM/BA system, and the interfacial compatibility between the PTEI-N and BDM/BA phase is excellent. TGA shows that the BDM/BA resin continues to exhibit good thermal resistance with a suitable dosage of PTEI-N. These changes in properties are closely correlated with the addition of PTEI-N. The PTEI-N/BDM/BA resin system shows potential applications in many fields.

High Performance Polymers published new progress about Bending strength. 118-45-6 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H3ClO3, Name: 5-Chloroisobenzofuran-1,3-dione.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Li, He; Zhang, Yijun; Liu, Dinghua; Liu, Xiaoqin published the artcile< An improved method for the synthesis of phenylacetic acid derivatives via carbonylation>, Related Products of 611-19-8, the main research area is phenylacetic acid preparation; benzyl chloride carbonylation palladium catalyst.

A series of phenylacetic acid derivatives RCH2CO2H [R = 2-ClC6H4, 4-MeC6H4, 2,4-Cl2C6H3, etc.] was synthesized via bistriphenylphosphine palladium dichloride catalyzed carbonylation reaction of benzyl chloride derivatives in presence of tetraethylammonium chloride and sodium hydroxide as reagents and xylene as solvent at 80°C under a CO atm. 2,4-Dichlorophenylacetic acid was obtained in a maximum yield of 95% from 2,4-dichlorobenzyl chloride using the same reaction system.

Journal of Chemical Research published new progress about Aralkyl chlorides Role: RCT (Reactant), RACT (Reactant or Reagent). 611-19-8 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H6Cl2, Related Products of 611-19-8.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Fuchs, Richard; Bloomfield, Jordan J. published the artcile< Transmission of electronic effects by the cyclopropane ring. Rates of alkaline hydrolysis of ethyl cis- and trans-2-phenylcyclopropanecarboxylates>, Formula: C10H9ClO2, the main research area is .

The rates of alk. hydrolysis of a series of m- and p-substituted Et β-phenylpropionates and of Et trans- and cis-2-(substituted phenyl)cyclopropanecarboxylates in 7.8% ethanol at 30° were measured. A comparison of Hammett ρ-values for these series, Et cis- and trans-cinnamates, and Et phenylpropiolates indicates that the influence of substituents on the reactivity increases in the six ester series in the order given above.

Journal of Organic Chemistry published new progress about Hydrolysis. 90940-40-2 belongs to class chlorides-buliding-blocks, and the molecular formula is C10H9ClO2, Formula: C10H9ClO2.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Saito, Yuta; Higashihara, Tomoya; Ueda, Mitsuru published the artcile< Highly refractive and photosensitive polyimide>, Application of C8H3ClO3, the main research area is refractive photosensitive polyimide.

A highly refractive sulfur-containing photosensitive polyimide (PSPI) based on the PI from 4,4′-[p-thiobis(phenylenesulfanyl)]diphthalic anhydride (3SDEA) and 4,4′-thiodianiline (SDA), 4,4′-methylenebis[2,6-bis(methoxymethyl)phenol] (MBMP) as a crosslinker, and (5-propylsulfonyloxyimino-5H-thiophen-2-ylidene)-(2-methylphenyl)acetonitrile (PTMA) as a photoacid generator has been developed. The matrix polymer showed high transparency in the g-line region and the high reflective index of 1.7452 and low birefringence of 0.0081. The PSPI consisting of the PI (84.8 wt%), MBHP (11.0 wt%), and PTMA (4.2 wt%) exhibited the high sensitivity (D0.5) of 36 mJ/cm2 and good contrast (γ0.5) of 5.1, resp., producing a clear neg.-tone line-and-space pattern with 8-μm resolution

Journal of Photopolymer Science and Technology published new progress about Dissolution. 118-45-6 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H3ClO3, Application of C8H3ClO3.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Xu, Yu; Cantwell, Lucas; Molosh, Andrei I.; Plant, Leigh D.; Gazgalis, Dimitris; Fitz, Stephanie D.; Dustrude, Erik T.; Yang, Yuchen; Kawano, Takeharu; Garai, Sumanta; Noujaim, Sami F.; Shekhar, Anantha; Logothetis, Diomedes E.; Thakur, Ganesh A. published the artcile< The small molecule GAT1508 activates brain-specific GIRK1/2 channel heteromers and facilitates conditioned fear extinction in rodents>, Synthetic Route of 31166-29-7, the main research area is GIRK1 GIRK2 channel activator preparation fear posttraumatic stress disorder; GIRK channels; PIP2; basolateral amygdala; medicinal chemistry; neurophysiology; phosphoinositide; potassium channel; small molecule; specific activator.

G-protein- gated inwardly-rectifying K+ (GIRK) channels are targets of Gi/o-protein-signaling systems that inhibit cell excitability. GIRK channels exist as homotetramers (GIRK2 and GIRK4) or heterotetramers with nonfunctional homomeric subunits (GIRK1 and GIRK3). Although they have been implicated in multiple conditions, the lack of selective GIRK drugs that discriminate among the different GIRK channel subtypes has hampered investigations into their precise physiol. relevance and therapeutic potential. Here, we report on a highly-specific, potent, and efficacious activator of brain GIRK1/2 channels. Using a chem. screen and electrophysiol. assays, we found that this activator, the bromothiophene-substituted small mol. GAT1508, is specific for brain-expressed GIRK1/2 channels rather than for cardiac GIRK1/4 channels. Computational models predicted a GAT1508- binding site validated by exptl. mutagenesis experiments, providing insights into how urea-based compounds engage distant GIRK1 residues required for channel activation. Furthermore, we provide computational and exptl. evidence that GAT1508 is an allosteric modulator of channel-phosphatidylinositol 4,5-bisphosphate interactions. Through brain-slice electrophysiol., we show that subthreshold GAT1508 concentrations directly stimulate GIRK currents in the basolateral amygdala (BLA) and potentiate baclofen-induced currents. Of note, GAT1508 effectively extinguished conditioned fear in rodents and lacked cardiac and behavioral side effects, suggesting its potential for use in pharmacotherapy for post-traumatic stress disorder. In summary, our findings indicate that the small mol. GAT1508 has high specificity for brain GIRK1/2 channel subunits, directly or allosterically activates GIRK1/2 channels in the BLA, and facilitates fear extinction in a rodent model.

Journal of Biological Chemistry published new progress about Allosteric modulators. 31166-29-7 belongs to class chlorides-buliding-blocks, and the molecular formula is C5H2Cl2O2S, Synthetic Route of 31166-29-7.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics