Month: November 2022

On February 28, 1979, Junek, Hans; Mittelbach, Martin published an article.Synthetic Route of 5098-14-6 The title of the article was Syntheses with nitriles, LIV. Reduction of oximinomalonitrile to aminomalonitrile using Raney catalysts. And the article contained the following:

An improved synthesis of aminomalononitrile H2NCH(CN)2 (I) by using Raney-catalyst for the reduction of HON:C(CN)2 (II) at H2-pressure of 4 atm and 20° was given. Due to the reactivity of II some new derivatives of oximinocyanoacetamide are obtained by O- and N-acylation. Condensation of III with benzilmonoxime gave 2-amino-5,6-diphenylpyrazinecarbonitrile; with N-phenylformamidate 2-amino-2,2-dicyano-1-(N-phenylimino)-acetaldehyde was obtained. The experimental process involved the reaction of 2-Aminomalononitrile 4-methylbenzenesulfonate(cas: 5098-14-6).Synthetic Route of 5098-14-6

The Article related to reduction oximinomalonitrile, malononitrile oximino, aminomalononitrile, acetamide oximinocyano, pyrazinecarbonitrile, cyclocondensation aminomalodinitrile benzil oxime, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines and other aspects.Synthetic Route of 5098-14-6

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 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 December 30, 2021, Vu, Binh; Dominique, Romyr; Li, Hongju; Fahr, Bruce; Chen, Yi published a patent.COA of Formula: C13H17BN2O2 The title of the patent was Methods and aromatic compounds for restoring mutant p53 function and their preparation. And the patent contained the following:

Mutations in oncogenes and tumor suppressors contribute to the development and progression of cancer. The disclosure describes compounds of formula I and methods that restore DNA binding affinity of p53 mutants. The compounds of the disclosure can bind to mutant p53 and restore the ability of the p53 mutant to bind DNA and activate downstream effectors involved in tumor suppression. The disclosed compounds of formula I can be used to reduce the progression of cancers that contain a p53 mutation. Compounds of formula I wherein X1 is CR7 and N; X2 is CR2 and N; R1 and R2 are independently alkyl, NR8R9, CONR8R9, NHCOR9, etc.; Q is NHCH2C(:CH2)CONH2, NHCOCH:CH2, NHCH2C(:CH2)CN, etc.; R5 is H, halo, (un)substituted aryl, (un)substituted heteroaryl, etc.; R6 is (un)substituted (mono/bi)cyclic aryl and (un)substituted (mono/bi)cyclic heteroaryl; R7, R8 and R9 are independently (un)substituted alkyl, (un)substituted alkenyl, (un)substituted cycloalkyl, etc.; and with provisions; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by a multistep procedure (procedure given). The invention compounds were evaluated for their DNA binding affinity of mutant p53 protein. The experimental process involved the reaction of 3-Amino-5-(tetramethyl-1,3,2-dioxaborolan-2-yl)benzonitrile(cas: 1036991-35-1).COA of Formula: C13H17BN2O2

The Article related to aromatic compound preparation restore mutant p53 function, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.COA of Formula: C13H17BN2O2

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

On May 26, 2011, Kim, Seon Mi; Lee, Min Hee; Kim, Jae Sun; Jung, Hoe Chul; Lee, So Young; Lee, Soo Min; Kim, Eun Jeong; Park, Eui Sun; Park, Sung Hoon; Lee, Bong Yong; Um, Key An published a patent.COA of Formula: C8H5BrFN The title of the patent was Preparation of gonadotropin releasing hormone receptor antagonists. And the patent contained the following:

Compound I [X = N-containing non-aromatic heterocycle or substituted non-aromatic heterocycle; Y = -(CR9aR9b)r-Z-R4; B = NR1R2 or OR1 where r = 0, 1, 2, 3; n = 2, 3, 4; Z = direct bond, O, S, CO, etc.; D = Q1, Q2, Q3, etc. where E = O, S, NR8; R1, R2 = independently H, (un)substituted C1-10 alkyl, (un)substituted C3-10 cycloalkyl, (un)substituted C6-12 aryl, etc.; R3a, R3b = independently H, (un)substituted C1-10 alkyl, (un)substituted C3-10 cycloalkyl, C1-10 alkoxy, etc.; R4 = H, substituted C1-10 alkyl, C3-10 cycloalkyl, (un)substituted C6-12 aryl, etc.; R5 = H, halogen, (un)substituted C1-6 alkyl, (un)substituted C3-10 cycloalkyl, etc.; R6 = H, (un)substituted C1-6 alkyl, (un)substituted C3-10 cycloalkyl, etc.;R8 = H, cyano, (un)substituted C1-10 alkyl, etc.; R9a, R9b = independently H, acyl, hydroxy, halogen, etc.; its stereoisomers or pharmaceutically acceptable salts] was prepared For example, II was prepared in a multistep synthesis. Compound I was claimed useful as gonadotropin releasing hormone (“”GnRH””) (known as LH releasing hormone) receptor antagonists for treatment of prostatic cancer, uterine cancer, and breast cancer, etc. The experimental process involved the reaction of 2-(Bromomethyl)-6-fluorobenzonitrile(cas: 1261686-95-6).COA of Formula: C8H5BrFN

The Article related to preparation gonadotropin releasing hormone receptor antagonist, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.COA of Formula: C8H5BrFN

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

On December 7, 2016, Gao, Yuzhe; Wang, Guocheng published a patent.Electric Literature of 1261686-95-6 The title of the patent was Preparation of xanthines as DPP-IV inhibitors. And the patent contained the following:

The invention relates to xanthine derivatives (e.g., I) and their pharmaceutically acceptable salts thereof, processes for preparing them, pharmaceutical preparations comprising them, and their as DPP-IV inhibitors for treating type II diabetes. For instance, the invention compound I was prepared via substitution of 8-bromo-3,9-dihydro-3-methyl-1H-purine-2,6-dione with 1-bromo-2-butyne followed by substitution with 2-(bromomethyl)-6-fluoro-benzonitrile, substitution with (R)-3-(Boc-amino)piperidine, and hydrolysis. The experimental process involved the reaction of 2-(Bromomethyl)-6-fluorobenzonitrile(cas: 1261686-95-6).Electric Literature of 1261686-95-6

The Article related to xanthine preparation antidiabetic dipeptidyl peptidase inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Electric Literature of 1261686-95-6

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

On June 11, 2020, Fu, Bang; Li, Yinlong; Ren, Wei; Chen, Jie; Liu, Xiangyong; Wang, Jiabing; Ding, Lieming published a patent.Recommanded Product: 882978-62-3 The title of the patent was Preparation of substituted pyrazolopyrimidines as tyrosine kinase inhibitors, compositions and methods thereof. And the patent contained the following:

The invention relates to compounds of formula I and isomerides, stereoisomers, tautomers, pharmaceutically acceptable salts, prodrugs, chelates, non-covalent complexes, and solvates thereof, methods of using the compounds as Trk inhibitors, and pharmaceutical compositions comprising such compds; their preparation and use in treating cancer. Compounds of formula I, wherein ring A is C5-6 heterocyclyl; ring B is 5-membered aromatic heterocyclyl; X and Z are independently C, N, O, and S; Y is C and N;R1 is absent, H, and C1-8 alkyl; R2 is H, C1-4 alkyl-NH2, C0-4 alkyl-OH, etc.; R3 absent, C3-10 heterocyclyl; R2 and R3 can be taken together to form 5- to 6-membered carbocyclyl, heterocyclyl, aryl, etc.; R4 is (un)substituted 5- to 6-membered heteroaryl, and isomerides, stereoisomers, tautomers, pharmaceutically acceptable salts, prodrugs, chelates, non-covalent complexes, and solvates thereof, are claimed. Example compound II was prepared by a multistep procedure (procedure given). The invention compounds were evaluated for their tyrosine kinase inhibitory activity (some data given). The experimental process involved the reaction of 4,5-Diamino-2-(trifluoromethyl)benzonitrile(cas: 882978-62-3).Recommanded Product: 882978-62-3

The Article related to substituted pyrazolopyrimidine tyrosine kinase inhibitor preparation treatment cancer, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Recommanded Product: 882978-62-3

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

On June 30, 2007, Abd El-Latif, Nehad A.; Amr, Abd El-Galil E.; Ibrahiem, Alhusain A. published an article.Formula: C12H7N3 The title of the article was Synthesis, reactions, and pharmacological screening of heterocyclic derivatives using nicotinic acid as a natural synthon. And the article contained the following:

A series of substituted pyridine derivatives were prepared from 3-acetylpyridine, which was prepared from the corresponding nicotinic acid as a natural starting material. Reaction of 3-acetylpyridine with indole-3-carboxaldehyde afforded the corresponding 3-β-(3-indolyl)(acryloyl)pyridine, which was treated with hydroxylamine hydrochloride in pyridine or acetic acid in the presence of sodium acetate to afford 3-β-(3-indolyl)(acryloyl)pyridine oxime and oxazole derivatives The oxime was treated with Et isothiocyanate or toluene-3,5-diisocyanate in refluxing dioxane to give the corresponding Et thiosemicarbazide and 3,5-bis(semicarbazide) derivative 3-β-(3-Indolyl)(acryloyl)pyridine was condensed with malononitrile in refluxing ethanol in the presence of piperidine as a catalyst to give a cyano(amino)pyran derivative, while it was condensed with Et cyanoacetate or malononitrile in the presence of ammonium acetate to yield (cyano)pyridone and cyano(amino)pyridine derivatives Cyclization of (acryloyl)pyridine with o-phenylenediamine in refluxing butanol led to the formation of the corresponding benzodiazepine via the intermediate A. Finally, cycloaddition reaction of (acryloyl)pyridine with thiourea yielded thioxopyrimidine, which was treated with chloroacetic acid to yield thiazolopyrimidine. An arylmethylene derivative was prepared by reacting thiazolopyrimidine with indole-3-carboxaldehyde or by treating thioxopyrimidine with indole-3-carboxaldehyde and chloroacetic acid in one step. The pharmacol. screening showed that many of the compounds thus prepared have good analgesic and anticonvulsant activities comparable to valdecoxib [i.e, 4-(5-methyl-3-phenyl-4-isoxazolyl)benzenesulfonamide] and carbamazepine as reference drugs. The experimental process involved the reaction of 2-((1H-Indol-3-yl)methylene)malononitrile(cas: 75629-62-8).Formula: C12H7N3

The Article related to nicotinic acid indolecarboxaldehyde thioxopyrimidine preparation analgesic anticonvulsant, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Formula: C12H7N3

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

Zhang, Xuqing; Ng, Raymond; Lanter, James; Sui, Zhihua published an article in 2007, the title of the article was Synthesis of novel pyrazolines via 1,3-dipolar cycloadditions of heterocyclic isopropenes.Name: 4,5-Diamino-2-(trifluoromethyl)benzonitrile And the article contains the following content:

An efficient and practical synthesis of novel pyrazoline structures was achieved through 1,3-dipolar cycloaddition of the corresponding heterocyclic isopropenes and diazo precursors. The experimental process involved the reaction of 4,5-Diamino-2-(trifluoromethyl)benzonitrile(cas: 882978-62-3).Name: 4,5-Diamino-2-(trifluoromethyl)benzonitrile

The Article related to heterocyclic isopropene preparation dipolar cycloaddition diazo compound, pyrazoline preparation, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Name: 4,5-Diamino-2-(trifluoromethyl)benzonitrile

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

Liu, Lu; Li, Lei; Mao, Shukuan; Wang, Xin; Zhou, Ming-Dong; Zhao, Yu-long; Wang, He published an article in 2020, the title of the article was Synthesis of pyrazolo[1,5-c]quinazoline derivatives through the copper-catalyzed domino reaction of o-alkenyl aromatic isocyanides with diazo compounds.Electric Literature of 13544-06-4 And the article contains the following content:

A novel copper-catalyzed domino reaction between o-alkenyl aromatic isocyanides and diazo compounds was developed under mild reaction conditions. Various o-alkenyl aromatic isocyanides were prepared from readily available reactants. The reaction provided a general and efficient method for synthesis of pyrazolo[1,5-c]quinazolines I [R1 = cyclohexyl, 2-thienyl, 2-naphthyl, etc.; R2 = H, 8-MeO, 7-Cl, etc.; R3 = OEt, OBn, 4-ClC6H4, etc.] by the formation of two rings and three new bonds in a single step from readily available acyclic starting materials. A mechanism involving a tandem (3+2) cyclization/elimination/intramol. aza-addition sequence was proposed. The experimental process involved the reaction of 2-(2-Nitro-4-(trifluoromethyl)phenyl)acetonitrile(cas: 13544-06-4).Electric Literature of 13544-06-4

The Article related to pyrazoloquinazoline preparation, ortho alkenyl aryl isocyanide diazo compound tandem copper catalyst, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Electric Literature of 13544-06-4

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts