Tag: 100-200

Grivsky, Eugene M.; Hitchings, George H. published an article in 1974, the title of the article was Syntheses of 2-chloro-4-acetylaminobenzonitrile isomers and structurally related compounds with biological activities.Quality Control of 3-Chloro-4-nitrobenzonitrile And the article contains the following content:

Benzonitriles I, II, and III (Xn = 2-,3-Cl, 2-F, 2,6-, 2,4 -Cl2; NH2, NHCOR, NO2 in 2, 4, or 5 position; R = e.g., Me, H, CF3, CHCl2, CH2Cl, Et, Me2CH, Pr, CH:CHCO2H, CH2CH2CO2H) were prepared (5 I, 15 II and 88 III). E.g., reaction of 2,4-F-(O2N)C6H3CO2H with MeSO2NH2-PCl5 gave 96% I (Xn = 2-F, 4-NO2), which was reduced to give II (Xn = 2-F, 4-NH2), which was acetylated to give 95% III (Xn = 2-F, R = Me). III (Xn = 2-Cl, NHCOMe in 4 position) had LD50 (oral-mice)of 1800 mg/kg; and at 20 mg/kg (oral-mice) was an antide-pressant and at 25 and 50 mg kg (orally-rat), resp., was an anal-gesic and antipyretic. The experimental process involved the reaction of 3-Chloro-4-nitrobenzonitrile(cas: 34662-29-8).Quality Control of 3-Chloro-4-nitrobenzonitrile

The Article related to acetanalide cyano halo analgesic, antipyretic chloroacetamidobenzonitrile, antidepressant chloroacetamidobenzonitrile, Noncondensed Aromatic Compounds: Nitriles, Isonitriles, and Acyl Cyanides and other aspects.Quality Control of 3-Chloro-4-nitrobenzonitrile

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

On February 7, 2008, Aleman, Jose; Jacobsen, Christian Borch; Frisch, Kim; Overgaard, Jacob; Jorgensen, Karl Anker published an article.Application of 2510-01-2 The title of the article was Organocatalytic asymmetric vinylogous addition to quinones – formation of optically active α-aryl ketones. And the article contained the following:

The organocatalytic addition of dicyanoalkylidenes to quinones catalyzed by cinchona alkaloids to give 1,4-diketones with high diastereomeric ratios (up to >98:<2 dr) and enantioselectivities (up to 99% ee) has been developed; the optically active compounds obtained are useful for a number of transformations, e.g. the synthesis of optically active α-aryl ketones. The experimental process involved the reaction of 2-(2,3-Dihydro-1H-inden-1-ylidene)malononitrile(cas: 2510-01-2).Application of 2510-01-2

The Article related to quinone stereoselective addition alkylidenemalononitrile cinchona alkaloid catalyst, ketone aromatic asym synthesis, Benzene, Its Derivatives, and Condensed Benzenoid Compounds: Naphthalenes and other aspects.Application of 2510-01-2

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

On June 15, 2006, Feenstra, Roelof W.; Stoit, Axel; Terpstra, Jan-Willem; Pras-Raves, Maria L.; McCreary, Andrew C.; Van Vliet, Bernard J.; Hesselink, Mayke B.; Kruse, Cornelis G.; Van Scharrenburg, Gustaaf J. M. published a patent.Safety of 3-Chloro-4-nitrobenzonitrile The title of the patent was Preparation of aminoethoxybenzoxazole derivatives with a combination of partial dopamine-d2 receptor agonism and serotonin reuptake inhibition. And the patent contained the following:

Title compounds I [X = S or O; R1 = H, alkyl, CF3, OH , etc.; R2 = H, alkyl, halo, or CN; R3 = H or alkyl; R4 = H, alkyl or haloalkyl; T = (un)saturated, (un)substituted carbon chain wherein one carbon atom may optionally be replaced with a N atom; Ar = aryl or heteroaryl], and their pharmaceutically acceptable salts, are prepared and disclosed to possess capability of both serotonin reuptake inhibition and partial agonism on dopamine -D2 receptors. Thus, e.g., II was prepared by reaction of 2-(4-iodobutoxy)benzonitrile with the corresponding amine (preparation given). I are evaluated by dopamine-D2 and 5-HT reuptake binding assays, e.g., II demonstrate pKi values of 7.9 and 7.4 resp. The invention also relates to the use of a compound disclosed herein for the manufacture of a medicament giving a beneficial effect. The experimental process involved the reaction of 3-Chloro-4-nitrobenzonitrile(cas: 34662-29-8).Safety of 3-Chloro-4-nitrobenzonitrile

The Article related to aminoethoxy benzoxazole preparation dopamine d2 receptor serotonin reuptake inhibitor, cns agent aminoethoxybenzoxazole amine preparation, Heterocyclic Compounds (More Than One Hetero Atom): Oxazoles, Isoxazoles and other aspects.Safety of 3-Chloro-4-nitrobenzonitrile

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

On June 19, 2009, O’Shea, Paul D.; Gauvreau, Danny; Gosselin, Francis; Hughes, Greg; Nadeau, Christian; Roy, Amelie; Shultz, C. Scott published an article.COA of Formula: C6H3BrN2O The title of the article was Practical Synthesis of a Potent Bradykinin B1 Antagonist via Enantioselective Hydrogenation of a Pyridyl N-Acyl Enamide. And the article contained the following:

A practical and efficient synthesis of bradykinin B1 antagonist I is described. A convergent strategy was utilized which involved synthesis of three fragments: II, III and IV. Cross coupling of fragments II and III followed by amidation with IV enabled efficient synthesis of I in 19 steps total, a 35% overall yield from com. available 5-bromo-3-nitropyridin-2-ol. The key to the success of the synthesis was the development of a fluorodenitration step to install the fluorine in pyridine III and a catalytic enantioselective hydrogenation of N-acyl enamide V to set the stereochem. The experimental process involved the reaction of 5-Bromo-3-hydroxypicolinonitrile(cas: 1160936-51-5).COA of Formula: C6H3BrN2O

The Article related to fluorodenitration rhodium catalyst stereoselective hydrogenation acyl enamide, bradykinin b 1 antagonist stereoselective preparation, Heterocyclic Compounds (More Than One Hetero Atom): Oxazoles, Isoxazoles and other aspects.COA of Formula: C6H3BrN2O

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

On July 1, 2010, Li, Jianqi; Wang, Guan; Zhang, Guisen; Lv, Na; Jiao, Guangjun; Liu, Shicheng; Zhou, Shixia published a patent.Electric Literature of 34662-29-8 The title of the patent was Preparation of piperidinyl benzisoxazole derivatives as inhibitors of 5-HT2A receptor. And the patent contained the following:

The invention provides piperidinyl benzisoxazole derivatives with formula I [R = H, halo, (un)substituted alkyl, or alkoxy; X and Y independently = CH or N; Ra = H, halo, CN, (un)substituted alkyl, alkoxy, etc,], and their salts and hydrates, are prepared and disclosed. The invention compounds has antagonistic effect on 5-HT2A and has mediating effect on 5-hydroxytryptamine system such as reuptake inhibiting effect of 5-HT and so on. Thus, e.g., II was prepared by condensation reaction of N-(4-chlorobutyl)indole with 4-(6-fluorobenzisoxazol-3-yl)piperidine. II exhibited affinity to 5-HT2A with IC50 value of 1.659 nM and Ki value of 1.9806 nM. The compounds of the invention possess excellent analgesia, sedation activity, minimal toxicity and side effects. The invention also provides pharmaceutical compositions comprising the derivatives and their use. The experimental process involved the reaction of 3-Chloro-4-nitrobenzonitrile(cas: 34662-29-8).Electric Literature of 34662-29-8

The Article related to benzisoxazole piperidinyl preparation 5hta receptor inhibitor pain, Heterocyclic Compounds (More Than One Hetero Atom): Oxazoles, Isoxazoles and other aspects.Electric Literature of 34662-29-8

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

On February 3, 2011, Shibata, Norio; Kagawa, Takumi published a patent.Category: nitriles-buliding-blocks The title of the patent was preparation of trifluoromethylthiophenium derivative salts as trifluoromethylating agents. And the patent contained the following:

Provided are trifluoromethylthiophenium derivative salts useful as intermediates in the synthesis of drugs or agricultural chems., a process for production of the same, and a process for the production of trifluoromethyl-containing compounds using the same as the trifluoromethylating agent. Specifically, S-(trifluoromethyl) -benzo[b]thiophenium derivative salts represented by general formula I [ R1-4 = H, C1-10 alkyl, C1-10 alkoxy, F, Cl, Br, NO2, CN; R5 = C1-10 alkyl, (substituted) phenyl; X = anion] is prepared by reacting trifluoromethyl 2-ethynylphenyl sulfide II with an acid. Thus, 2-cyclopropyl-1-trifluoromethylbenzo[b]thiophenium triflate was prepared by reacting 1-cyclopropylethynyl-2-trifluoromethylsulfanylbenzene with trifluoromethanesulfonic acid. When Me 1-indanone-2-carboxylate was treated with 2-cyclopropyl-1-trifluoromethylbenzo[b]thiophenium triflate, 1-oxo-2-trifluoromethylindan-2-carboxylic acid Me ester was obtained. The experimental process involved the reaction of 2-(2,3-Dihydro-1H-inden-1-ylidene)malononitrile(cas: 2510-01-2).Category: nitriles-buliding-blocks

The Article related to trifluoromethylthiophenium derivative salt preparation trifluoromethylating agent, Heterocyclic Compounds (One Hetero Atom): Areno- and Diarenothiophenes and other aspects.Category: nitriles-buliding-blocks

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

On May 22, 2008, Ohlmeyer, Michael; Bohnstedt, Adolph; Kingsbury, Celia; Ho, Koc-Kan; Quintero, Jorge published a patent.Computed Properties of 138801-92-0 The title of the patent was Preparation of 7-substituted purine derivatives as immunosuppressants. And the patent contained the following:

Purinone derivatives of formula I [Q1, Q2 = (substituted) CH, N; Q3 = CH, N; R1-R3 = H, alkyl; R4 = alkyl, heterocyclyl, aryl, heteroaryl, etc.; R5 = alkyl, heterocyclyl, etc.; n = 0-3] are prepared for the prevention and treatment of autoimmune diseases, inflammatory disease, mast cell mediated disease and transplant rejection. Thus, II was prepared, and inhibited IL-2 induced IFN-γ production by >40% at 30 mg/kg in mice. The experimental process involved the reaction of 4-Oxochroman-6-carbonitrile(cas: 138801-92-0).Computed Properties of 138801-92-0

The Article related to purinone derivative preparation immunosuppressant, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Computed Properties of 138801-92-0

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

On April 17, 2014, Kilburn, John Paul; Rasmussen, Lars Kyhn; Jessing, Mikkel; Eldemenky, Eman Mohammed; Chen, Bin; Jiang, Yu; Hopper, Allen T. published a patent.Electric Literature of 337965-61-4 The title of the patent was Preparation of benzamides as P2X7 receptor antagonists. And the patent contained the following:

The title compounds I [R1 = Ph, pyridyl, pyrazinyl, etc.; R2 = cycloalkyl, alkoxy, Ph, etc.; R3 = H, F, alkyl, fluoroalkyl; or R2 and R3 can be combined with the carbon to which they are attached to form cyclohexyl, piperazinyl, piperidinyl, etc.; R4 = halo, fluoroalkyl, CN, etc.; R5 = halo, alkyl, fluoroalkyl, etc.; n = 0-3], useful in the treatment of diseases related with the activity of P2X7 receptor, were prepared For example, amidating [4-(4-chloro-phenyl)-tetrahydro-pyran-4-yl]-methylamine with 2,3-dimethylbenzoyl chloride afforded 66% II. Compounds I were tested in vitro for their ability to act as antagonists to the P2X7 receptor (data given for representative compounds I). Pharmaceutical composition comprising compound I is disclosed. The experimental process involved the reaction of 2-(6-Fluoropyridin-3-yl)acetonitrile(cas: 337965-61-4).Electric Literature of 337965-61-4

The Article related to benzamide preparation p2x7 receptor antagonist, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Electric Literature of 337965-61-4

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

On December 28, 2018, Bahuguna, Ashish; Kumar, Ashwani; Chhabra, Tripti; Kumar, Ajay; Krishnan, Venkata published an article.Name: 2-((1H-Indol-3-yl)methylene)malononitrile The title of the article was Potassium-Functionalized Graphitic Carbon Nitride Supported on Reduced Graphene Oxide as a Sustainable Catalyst for Knoevenagel Condensation. And the article contained the following:

A nanocomposite of potassium-functionalized graphitic carbon nitride (KGCN) and reduced graphene oxide (RGO) was fabricated by a facile hydrothermal method and used as a heterogeneous catalyst for Knoevenagel condensation and sustainable synthesis of aryl substituted chromenes. The prepared KGCN-RGO nanocomposite catalyst has been characterized by using various techniques, such as powder X-ray diffraction technique (PXRD), Fourier transform IR spectroscopy, SEM, transmission electron microscopy, thermogravimetric anal., and BET surface area anal. After detailed characterization, the nanocomposite was used as a heterogeneous catalyst to synthesize various aryl substituted chromenes in ethanol. The developed KGCN-RGO nanocatalyst also rendered good recyclability for the explored catalytic reactions. In addition, a high value of atom economy and a low value of E-factor are also key highlights of this green and sustainable catalytic protocol. The experimental process involved the reaction of 2-((1H-Indol-3-yl)methylene)malononitrile(cas: 75629-62-8).Name: 2-((1H-Indol-3-yl)methylene)malononitrile

The Article related to potassium functionalized graphitic carbon nitride knoevenagel condensation catalyst, Physical Organic Chemistry: Addition, Elimination, and Substitution Reactions and other aspects.Name: 2-((1H-Indol-3-yl)methylene)malononitrile

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

On July 31, 2008, Noritake, Shun; Shibata, Norio; Nakamura, Shuichi; Toru, Takeshi; Shiro, Motoo published an article.Application In Synthesis of 2-(2,3-Dihydro-1H-inden-1-ylidene)malononitrile The title of the article was Fluorinated Johnson reagent for transfer-trifluoromethylation to carbon nucleophiles. And the article contained the following:

A novel reagent, [(oxido)phenyl(trifluoromethyl)-λ4-sulfanylidene]dimethylammonium tetrafluoroborate has been developed for the electrophilic trifluoromethylation of carbon nucleophiles. The reagent was designed as a trifluorinated version of a Johnson-type methyl-transfer reagent. The first example of vinylogous trifluoromethylation of dicyanoalkylidenes is also demonstrated. The experimental process involved the reaction of 2-(2,3-Dihydro-1H-inden-1-ylidene)malononitrile(cas: 2510-01-2).Application In Synthesis of 2-(2,3-Dihydro-1H-inden-1-ylidene)malononitrile

The Article related to fluorinated johnson reagent transfer trifluoromethylation carbon nucleophile, Physical Organic Chemistry: Addition, Elimination, and Substitution Reactions and other aspects.Application In Synthesis of 2-(2,3-Dihydro-1H-inden-1-ylidene)malononitrile

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts