Tag: 100-200

On January 31, 2009, Kaspady, Mohamed; Narayanaswamy, Venugopala Katharigatta; Raju, Mohana; Rao, Gopal Krishna published an article.Synthetic Route of 34662-29-8 The title of the article was Synthesis, antibacterial activity of 2,4-disubstituted oxazoles and thiazoles as bioisosteres. And the article contained the following:

Two series of 2-substituted aryl, heteroaryl and alkyl, 4-substituted aryl 1,3-oxazole (2a-k) and thiazole (4a-k) mol. scaffolds containing divalent bioisosteres, viz., oxygen and sulfur were synthesized by condensing substituted amides and thioamides with substituted phenacyl bromide in absolute ethanol medium. The structure of newly synthesized compounds was characterized by anal. and spectral (IR, 1H-NMR, 13C-NMR and LC-MS) methods. The synthesized compounds were evaluated for qual. (zone of inhibition) and quant. antibacterial activity (MIC) by agar cup plate and micro-titration methods, resp. Preliminary pharmacol. observations revealed that some of the substituents such as 2-alkyl and heteroaryl at second position, chloro and bromo at the fourth position of the aryl moiety and a divalent sulfur atom in the five-membered heterocyclic ring system influenced significantly the antibacterial activity when compared to its bioisostere counterpart 2-substituted aryl, heteroaryl and alkyl, 4-substituted aryl 1,3-oxazole systems. The experimental process involved the reaction of 3-Chloro-4-nitrobenzonitrile(cas: 34662-29-8).Synthetic Route of 34662-29-8

The Article related to antibacterial oxazole thiazole preparation sar, Microbial, Algal, and Fungal Biochemistry: Antimicrobial Sensitivity and other aspects.Synthetic Route of 34662-29-8

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On May 18, 2018, Guchhait, Sankar K.; Sisodiya, Shailendra; Saini, Meenu; Shah, Yesha V.; Kumar, Gulshan; Daniel, Divine P.; Hura, Neha; Chaudhary, Vikas published an article.Application In Synthesis of 2-((1H-Indol-3-yl)methylene)malononitrile The title of the article was Synthesis of Polyfunctionalized Pyrroles via a Tandem Reaction of Michael Addition and Intramolecular Cyanide-Mediated Nitrile-to-Nitrile Condensation. And the article contained the following:

A new approach for the synthesis of tetrasubstituted/functionalized NH-pyrroles from gem-diactivated acrylonitriles and TMSCN has been developed. The strategy utilizes the generation of vic-dinitrile via Michael addition and cyanide-mediated nitrile-to-nitrile cyclocondensation, which proceed in tandem guided by manifold roles of “CN”. An extended application to the production of fused pyrrole has also been realized. The experimental process involved the reaction of 2-((1H-Indol-3-yl)methylene)malononitrile(cas: 75629-62-8).Application In Synthesis of 2-((1H-Indol-3-yl)methylene)malononitrile

The Article related to diactivated acrylonitrile trimethylsilyl cyanide tandem michael addition cyclocondensation, pyrrole polyfunctionalized preparation, Heterocyclic Compounds (One Hetero Atom): Pyrroles and Pyrrolizines and other aspects.Application In Synthesis of 2-((1H-Indol-3-yl)methylene)malononitrile

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On July 19, 2013, Cao, Ying; Zhang, Song-Chen; Zhang, Min; Shen, Guang-Bin; Zhu, Xiao-Qing published an article.Product Details of 2510-01-2 The title of the article was Determination of Thermodynamic Affinities of Various Polar Olefins as Hydride, Hydrogen Atom, and Electron Acceptors in Acetonitrile. And the article contained the following:

A series of 69 polar olefins with various typical structures (X) were synthesized and the thermodn. affinities (defined in terms of the molar enthalpy changes or the standard redox potentials in this work) of the polar olefins obtaining hydride anions, hydrogen atoms, and electrons, the thermodn. affinities of the radical anions of the polar olefins (X•-) obtaining protons and hydrogen atoms, and the thermodn. affinities of the hydrogen adducts of the polar olefins (XH•) obtaining electrons in acetonitrile were determined using titration calorimetry and electrochem. methods. The pure C=C π-bond heterolytic and homolytic dissociation energies of the polar olefins (X) in acetonitrile and the pure C=C π-bond homolytic dissociation energies of the radical anions of the polar olefins (X•-) in acetonitrile were estimated The remote substituent effects on the six thermodn. affinities of the polar olefins and their related reaction intermediates were examined using the Hammett linear free-energy relationships; the results show that the Hammett linear free-energy relationships all hold in the six chem. and electrochem. processes. The information disclosed in this work could not only supply a gap of the chem. thermodn. of olefins as one class of very important organic unsaturated compounds but also strongly promote the fast development of the chem. and applications of olefins. The experimental process involved the reaction of 2-(2,3-Dihydro-1H-inden-1-ylidene)malononitrile(cas: 2510-01-2).Product Details of 2510-01-2

The Article related to thermodn affinity polar olefin hydride hydrogen atom electron acceptor, Physical Organic Chemistry: Other Reactions, Processes, and Spectra and other aspects.Product Details of 2510-01-2

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On October 31, 2020, Cao, Dongdong; Chen, Dingben; Chen, Gang; Mo, Hanjie; Xia, Zhijun; Li, Kai-bin; Yang, Jianguo published an article.Synthetic Route of 2510-01-2 The title of the article was Synthesis of Dibenzofurans Derivatives via Benzannulation of 2-Nitrobenzofurans and Alkylidene Malononitriles. And the article contained the following:

Although various methods for the preparation of dibenzofurans are available, an efficient, general synthesis of dibenzofurans from benzofurans remains an unsolved problem. Herein, we provide the first benzannulation of readily prepared 2-nitrobenzofurans with alkylidene malononitriles. This methodol. enables facile assembly of a wide variety of highly functionalized dibenzofurans in moderate to excellent yields under metal-free conditions. Gram-scale synthesis and further elaborations of the product were succesfully performed, demonstrating synthetic utility of this method. The experimental process involved the reaction of 2-(2,3-Dihydro-1H-inden-1-ylidene)malononitrile(cas: 2510-01-2).Synthetic Route of 2510-01-2

The Article related to nitrobenzofuran alkylidene malononitrile cyclization, dibenzofuran preparation, Heterocyclic Compounds (One Hetero Atom): Areno- and Diarenofurans and other aspects.Synthetic Route of 2510-01-2

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Sedighian, Hadi; Imani, Kaveh; Bazgir, Ayoob published an article in 2022, the title of the article was Ultrasound-assisted a domino three-component reaction to polycyclic selenopyrans synthesis.Recommanded Product: 2510-01-2 And the article contains the following content:

A novel and efficient three-component reaction of substituted benzoyl chlorides, potassium selenocyanate and vinyl malononitriles was developed for the synthesis of polycyclic selenopyrans via an ultrasound-assisted domino vinylogous nucleophilic reaction/intramol. selenocyclization/imine-enamine tautomerization reaction. Introducing a simple one-step method and use of available starting materials and mild reaction conditions are the most important advantages of this strategy. The experimental process involved the reaction of 2-(2,3-Dihydro-1H-inden-1-ylidene)malononitrile(cas: 2510-01-2).Recommanded Product: 2510-01-2

The Article related to vinylmalononitrile potassium selenocyanate benzoyl chloride tandem heterocyclization, benzoylimino fused selenopyran preparation ultrasonication, Heterocyclic Compounds (One Hetero Atom): Other 6-Membered Rings and other aspects.Recommanded Product: 2510-01-2

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On September 30, 2009, Goeker, Hakan; Alp, Mehmet; Ates-Alagoez, Zeynep; Yildiz, Sulhiye published an article.Application of 34662-29-8 The title of the article was Synthesis and potent antifungal activity against Candida species of some novel 1H-benzimidazoles. And the article contained the following:

A series of 47 novel N1-alkylated-2-aryl-5(6)-substituted-1H-benzimidazoles and their three novel indole analogs were synthesized and evaluated for in vitro antifungal activities against Candida species by the tube dilution method. The results showed that I and II, having pyridine at the position C-2, of benzimidazoles exhibited the greatest activity with MIC values of 6.25-3.12 μg/mL. Indole analogs III (R1 = H, R2 = Br; R1 = Pr, R2 = Br, CN) have no inhibitory activity. The experimental process involved the reaction of 3-Chloro-4-nitrobenzonitrile(cas: 34662-29-8).Application of 34662-29-8

The Article related to benzimidazole preparation nucleophilic substitution reduction aryl diamine benzaldehyde heterocyclization, fungal infection antifungal structure activity candida, Heterocyclic Compounds (More Than One Hetero Atom): Imidazoles and other aspects.Application of 34662-29-8

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On November 27, 2003, Cai, Sui Xiong; Jiang, Songchun; Kemnitzer, William E.; Zhang, Hong; Attardo, Giorgio; Denis, Real published a patent.Related Products of 75629-62-8 The title of the patent was Preparation of substituted 4-aryl-4H-pyrrolo[2,3-h]chromenes and analogs as activators of caspases and inducers of apoptosis and their uses against cancer and other disorders. And the patent contained the following:

The present invention is directed to substituted 4-aryl-4H-pyrrolo[2,3-h]chromenes and analogs thereof (shown as I; variables defined below; e.g. II). The present invention also relates to the discovery that compounds I are activators of caspases and inducers of apoptosis. Therefore, I can be used to induce cell death in a variety of clin. conditions in which uncontrolled growth and spread of abnormal cells occurs. The ability to activate the caspase cascade and induce apoptosis in human breast cancer cell lines T-47D and ZR-75-1 was measured for ∼50 examples of I, e.g. EC50 (nM) = 2.3 and 1.6, resp., for II. Although the methods of preparation are not claimed, ∼50 example preparations are included. For I: R1 = alkyl, cycloalkyl, cycloalkylalkyl, hydroxyalkyl, haloalkyl, alkoxyalkyl, aminoalkyl and oxiranylalkyl; R3 and R4 = H, halo, haloalkyl, aryl, fused aryl, carbocyclic, a heterocyclic group, a heteroaryl group, C1-10 alkyl, alkenyl, alkynyl, arylalkyl, arylalkenyl, arylalkynyl, heteroarylalkyl, heteroarylalkenyl, heteroarylalkynyl, carbocycloalkyl, heterocycloalkyl, hydroxyalkyl, aminoalkyl, carboxyalkyl, nitro, amino, cyano, acylamido, hydroxy, thiol, acyloxy, azido, alkoxy, carboxy, methylenedioxy, carbonylamido or alkylthio; R5 is H or C1-10 alkyl. A is (un)substituted and is aryl, heteroaryl, saturated carbocyclic, partially saturated carbocyclic, saturated heterocyclic, partially saturated heterocyclic or arylalkyl; D is (un)substituted and is a heteroaromatic, partially saturated (un)saturated heterocyclic fused ring, wherein said fused ring has 5 or 6 ring atoms, wherein one or two of said ring atoms are N atoms and the others of said ring atoms are C atoms. Y is CN, COR19, CO2R19 or CONR20R21, wherein R19, R20 and R21 = H, C1-10-alkyl, haloalkyl, aryl, fused aryl, carbocyclic, a heterocyclic group, a heteroaryl group, alkenyl, alkynyl, arylalkyl, arylalkenyl, arylalkynyl, heteroarylalkyl, heteroarylalkenyl, heteroarylalkynyl, carbocycloalkyl, heterocycloalkyl, hydroxyalkyl or aminoalkyl; or R20 and R21 are taken together with the N to form a heterocycle; and Z is NR22R23, NHCOR22N(COR23)2, N(COR22)(COR23), N:CHOR19 or N:CHR19 wherein R22 and R23 = H, C1-4 alkyl or aryl, or R22 and R23 are combined together with the group attached to them to form a heterocycle. The experimental process involved the reaction of 2-((1H-Indol-3-yl)methylene)malononitrile(cas: 75629-62-8).Related Products of 75629-62-8

The Article related to aryl pyrrolochromene analog preparation caspase activator apoptosis inducer, antitumor agent aryl pyrrolochromene analog preparation pharmaceutical composition, Heterocyclic Compounds (More Than One Hetero Atom): Imidazoles and other aspects.Related Products of 75629-62-8

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On May 10, 2001, McCauley, John A.; Theberge, Cory R.; Liverton, Nigel J.; Claremon, David A.; Claiborne, Christopher F. published a patent.Formula: C7H5FN2 The title of the patent was Preparation of 2-benzyl and 2-heteroaryl benzimidazole NMDA/NR2B antagonists. And the patent contained the following:

Novel benzimidazoles, substituted in the 2-position by substituted benzyl groups or heteroaryl groups, (I) [wherein R1, R2, R4, and R5 = independently H, Cl, F, OH, OMe, CF3, OCF3, NH2, CN, NO2, (amino)alkyl, aryl, alkylcarbonylamino, oxohydroxydibenzopyranyl-substituted carboxyphenylthioureido or carbonylaminoalkylcarbonylamino, R6SO2NH, R6SO2NMe, or R6SO2NHCH2; R3 = H, OH, NH2, alkylamino, arylamino, or :O; R6 = (un)substituted alkyl, (phenyl)alkenyl, Ph, naphthyl, or heterocyclic group; Y = O, NH, (CH2)nCO(CH2)n, or (CH2)nCHR3(CH2)n; n = 0-5; Ar may be substituted with 0-3 N atoms in positions 2, 3, 5, or 6] were prepared as effective NMDA NR2B glutamate receptor antagonists. For example, cycloaddition of phenylenediamine and (4-phenoxyphenyl)acetic acid in presence of EDC and HOBt in DMF afforded 2-(4-phenoxybenzyl)-1H-benzimidazole. Exptl. protocols for assessing the inhibition of NR1A/2B NMDA receptor activation (FLIPR assay) and determining the apparent dissociation constants against the human NR1A/NR2B receptor (binding assay) are given (no data). I are useful for relieving pain and treating depression, schizophrenia, Parkinson’s disease, or stroke (no data). The experimental process involved the reaction of 2-(6-Fluoropyridin-3-yl)acetonitrile(cas: 337965-61-4).Formula: C7H5FN2

The Article related to benzimidazole preparation analgesic, benzyl benzimidazole preparation glutamate receptor antagonist, heteroaryl benzimidazole preparation nmda nr2b antagonist, Heterocyclic Compounds (More Than One Hetero Atom): Imidazoles and other aspects.Formula: C7H5FN2

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On October 23, 2003, Shimojo, Masato; Taniguchi, Kana published a patent.Related Products of 34662-29-8 The title of the patent was Preparation of imidazoarenes as prostaglandin E2 subtype EP4 receptor antagonists for treatment of IL-6 involved diseases. And the patent contained the following:

The present invention relates to the use of a prostaglandin E2 (PGE2) subtype EP4 receptor ligand in the manufacture of a medicament for the treatment of interleukin 6 (IL-6) involved diseases, such as alc. cirrhosis, amyloidosis, atherosclerosis, cardiac disease, sclerosis, and organ transplantation reactions (no data). The invention also relates to the assay which comprises culturing peripheral whole blood with a test compound and determining the effect of the compound on PGE2-induced whole blood cells activation. Three hundred eighty title compounds I [wherein Y1-Y4 = N, CH, CL; R1 = H, (un)substituted alkyl, alkenyl, alkynyl, cycloalkyl, alkoxy, pyrrolidinyl, amino, etc.; A = (un)substituted 5-6 membered (un)substituted monocyclic (hetero)aromatic ring; B = halo-substituted alkylene, cycloalkylene, alkenylene, alkynylene, alkyleneoxy, etc., optionally substituted with an oxo or alkyl group; W = amino, O, S, bond, etc.; R2 = H, OH, alkyl, alkoxy; Z = 5-12 membered (un)substituted monocyclic or bicyclic (hetero)aryl; L = halo, alkyl, haloalkyl, OH, alkoxy, haloalkoxy, alkylthio, NO2, amino, etc.] were prepared Thus, cycloaddition of 2-[4-[(3-amino-4,6-dimethyl-2-pyridinyl)amino]phenyl]ethanol (4-step preparation given) with propionyl chloride in toluene provided 2-[4-(2-ethyl-5,7-dimethyl-3H-imidazo[4,5-b]pyridin-3-yl)phenyl]ethyl propionate, which was treated with aqueous LiOH to give the ethanol derivative (86%). Chlorination (90%) using thionyl chloride, conversion to the azide (85%), and Pd/C catalyzed hydrogenation afforded the amine (94%). Coupling of the amine with p-toluenesulfonyl isocyanate in CH2Cl2 gave II (56%). The latter significantly inhibited IL-6 secretion by PGE2 in ConA-stimulated human peripheral blood mononuclear cells (PBMC). The experimental process involved the reaction of 3-Chloro-4-nitrobenzonitrile(cas: 34662-29-8).Related Products of 34662-29-8

The Article related to imidazoarene preparation composition prostaglandin e2 ep4 antagonist, benzimidazole imidazopyridine preparation composition il6 disease, Heterocyclic Compounds (More Than One Hetero Atom): Imidazoles and other aspects.Related Products of 34662-29-8

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On April 16, 2021, Reutskaya, Elena; Sapegin, Alexander; Peintner, Stefan; Erdelyi, Mate; Krasavin, Mikhail published an article.Synthetic Route of 34662-29-8 The title of the article was Sulfur Oxidation Increases the Rate of HIRE-Type [1.4]Thiazepinone Ring Expansion and Influences the Conformation of a Medium-Sized Heterocyclic Scaffold. And the article contained the following:

The hydrated imidazoline ring expansion (HIRE-type) reaction was investigated for a series of di(hetero)arene-fused [1.4]thiazepinones in comparison with their sulfone counterparts. The sulfones were found to undergo ring expansion at a much higher rate compared to the thioethers, much in line with the current mechanistic understanding of the process. Moreover, the amide bond cis- and trans-isomers of the ring-expanded products were found, in the case of sulfones, to be stabilized through an intramol. hydrogen bond. The latter phenomenon was studied in detail by NMR experiments and corroborated by X-ray crystallog. information. The experimental process involved the reaction of 3-Chloro-4-nitrobenzonitrile(cas: 34662-29-8).Synthetic Route of 34662-29-8

The Article related to thiazepinone hydrated imidazoline ring expansion conformation sulfone, Heterocyclic Compounds (More Than One Hetero Atom): Other 7-Membered Rings and other aspects.Synthetic Route of 34662-29-8

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