Month: November 2022

On January 31, 1993, Yu, Euy Kyung; Ryu, Seoung Ryuall published an article.Recommanded Product: 2-Aminomalononitrile 4-methylbenzenesulfonate The title of the article was Studies on the synthesis of the 2-desamino and 2-desamino-2-methyl analogs of aminopterin intermediate at pteridine-C7 side chain. And the article contained the following:

Title aminopterin intermediates I (R = H, Me, NH2) were prepared from pyrazine II. Thus, dithiobisbenzoate III was reduced by NaBH4 and then treated with II to give pyrazine IV. The cyclization of IV with RC(:NH)NH2.HCl (R = H, Me, NH2) in the presence of NaOEt followed by basic hydrolysis gave I (R = H, Me, NH2). The experimental process involved the reaction of 2-Aminomalononitrile 4-methylbenzenesulfonate(cas: 5098-14-6).Recommanded Product: 2-Aminomalononitrile 4-methylbenzenesulfonate

The Article related to aminopterin intermediate pteridine c side chain, desamino analog aminopterin intermediate, Amino Acids, Peptides, and Proteins: Amino Acids and other aspects.Recommanded Product: 2-Aminomalononitrile 4-methylbenzenesulfonate

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

On December 3, 2003, Suga, A.; Kubota, H.; Miura, M.; Sasuga, D.; Moritani, H. published a patent.SDS of cas: 34662-29-8 The title of the patent was Preparation of tetrahydropyranalkyl carboxamide derivatives as inhibitors of apo β-related lipoprotein secretion. And the patent contained the following:

A novel tetrahydropyran derivative which has an excellent apo B-related lipoprotein secretion-inhibiting activity of the following general formula (I) or a salt thereof are prepared wherein R1 and R3 are the same or different and each represents H or lower alkyl; R2 is H, halogen, Ra-lower alkyl, or R20O-CO-; Ra is H, R21O-CO-, R22R23N-, R24R25N-CO-, R26O-cyano, or optionally-substituted hetero ring; R4, R5, R6 and R7 are the same or different and each is H, halogen, haloalkyl, cyano, lower alkyl, lower alkyl-O-, R21O-CO-lower alkyl-, R27-CO-, or R28R29N-S(O)2-; R8 and R9 are the same or different and each is H, lower alkyl, R30-lower alkyl-, R31R32N-, optionally- substituted hetero ring, or R33R34R35C-; R8 and R9 may together form optionally-substituted hetero ring-; X is N or CR36; R20, R22 to R26, R28, R29, R32 and R36 are the same or different and each is H or lower alkyl; R21 is H, lower alkyl, or aryl-lower alkyl-; R27 is HO-, lower alkyl-O-, or optionally-substituted hetero ring-, or lower alkyl-O-; R30 represents optionally-substituted aryl, optionally-substituted hetero ring-, or lower alkyl-O-; R31 represents optionally-substituted aryl, or optionally-substituted hetero ring-; R33 represents HO-lower alkyl-, or optionally-substituted hetero ring-lower alkyl-; R34 represents optionally-substituted aryl-. Thus, e.g., II was prepared by hydrolysis of corresponding Et ester (preparation given). In assays to evaluate apo β-related lipoprotein secretion-inhibiting activity, selected compounds of I possessed IC50 values ranging from 1.7-40 nM. As inhibitors of apo β-related lipoprotein secretion, I have excellent blood cholesterol and triglyceride-lowering effect, and are useful as remedies for hyperlipemia, arteriosclerosis, obesity and pancreatitis. The experimental process involved the reaction of 3-Chloro-4-nitrobenzonitrile(cas: 34662-29-8).SDS of cas: 34662-29-8

The Article related to pyran tetrahydro derivative preparation lipoprotein secretion inhibitor, pyranalkylcarboxamide derivative preparation hyperlipemia arteriosclerosis obesity pancreatitis, Heterocyclic Compounds (One Hetero Atom): Pyrans and other aspects.SDS of cas: 34662-29-8

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

On May 31, 1987, Morales-Rios, M. S.; Espineira, J.; Joseph-Nathan, P. published an article.Related Products of 75629-62-8 The title of the article was Carbon-13 NMR spectroscopy of indole derivatives. And the article contained the following:

The chem. shifts of 298 naturally occurring and synthetic compounds containing the indole chromophoric group are listed. Substituent effects on 13C chem. shifts (SCS) induced by substitution on the heteroaromatic five-membered ring are discussed. The data provide a reference set for future 13C NMR investigations and highlight the need for unambiguous exptl. evidence to resolve controversial assignments for differently substituted representative indole derivatives Many original assignments have been changed, and values not considered to be unambiguously assigned are delineated. The 1J(CH) values for the parent indole were measured. 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 carbon nmr indole derivative, Alkaloids: Alkaloids Containing Two Nitrogen Atoms and other aspects.Related Products of 75629-62-8

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

On March 15, 2019, Yeh, Li-Hsuan; Wang, Hung-Kai; Pallikonda, Gangaram; Ciou, Yu-Lun; Hsieh, Jen-Chieh published an article.Quality Control of 2-(2-Nitro-4-(trifluoromethyl)phenyl)acetonitrile The title of the article was Palladium-Catalyzed Dual Annulation: A Method for the Synthesis of Norneocryptolepine. And the article contained the following:

A novel procedure for the Pd-catalyzed dual annulation reaction of I and derivatives to synthesize the norneocryptolepine derivatives involving the concerted construction of two central heterocycles is reported. The further methylation of norneocryptolepine (II) to afford its alkaloid analog neocryptolepine implies that synthesis of various neocryptolepine derivatives is feasible. The oxidative addition of Pd(0) is indicated as the key step to activate the intramol. addition of nitrile according to the mechanism study. The experimental process involved the reaction of 2-(2-Nitro-4-(trifluoromethyl)phenyl)acetonitrile(cas: 13544-06-4).Quality Control of 2-(2-Nitro-4-(trifluoromethyl)phenyl)acetonitrile

The Article related to norneocryptolepine synthesis dual annulation, Alkaloids: Alkaloids Containing Two Nitrogen Atoms and other aspects.Quality Control of 2-(2-Nitro-4-(trifluoromethyl)phenyl)acetonitrile

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

On August 18, 2005, Buchstaller, Hans-Peter; Burgdorf, Lars; Stieber, Frank; Amendt, Christiane; Grell, Matthias; Sirrenberg, Christian; Zenke, Frank published a patent.COA of Formula: C9H5F3N2O2 The title of the patent was Preparation of 1,3-diarylureas as inhibitors of raf and other kinases useful against cancer and other diseases. And the patent contained the following:

The present invention relates to bisarylurea derivatives (shown as I; variables defined below; e.g. 4-[4-[3-[4-chloro-5-methyl-2-(2-methylaminoethoxy)phenyl]ureido]phenoxy]pyridine-2-carboxylic acid methylamide (shown as II)), their use as inhibitors of raf-kinase (no data) and for the manufacture of a pharmaceutical composition and a method of treatment, comprising administering said pharmaceutical composition to a patient. Methods of preparation are claimed and >100 example preparations are included. For example, 1-[2-[2-[(tert-butoxycarbonyl)(methyl)amino]ethoxy]-5-(trifluoromethyl)phenyl]-3-[4-[[2-(methylcarbamoyl)pyridin-4-yl]oxy]phenyl]urea was prepared (87 %) by reacting tert-Bu [2-[2-amino-4-(trifluoromethyl)phenoxy]ethyl](methyl)carbamate (preparation given) with p-nitrophenyl chloroformate followed by N-methyl-4-(4-aminophenoxy)pyridine-2-carboxamide (preparation given) and DIPEA; deprotection gave 86 % 1-[2-[2-(methylamino)ethoxy]-5-(trifluoromethyl)phenyl]-3-[4-[[2-(methylcarbamoyl)pyridin-4-yl]oxy]phenyl]urea. For I: Ar1, Ar2 = aromatic hydrocarbons containing 6 to 14 C atoms and ethylenic unsaturated or aromatic heterocyclic residues containing 3 to 10 C atoms and one or two heteroatoms, = N, O and S; E, G, M, Q and U = C and N atoms, with the proviso that ≥1 of E, G, M, Q and U are C atoms and that X is bonded to a C atom. R7 = Het, OHet, N(R11)Het, (CR5R6)kHet, et al. or R7 = -SO2-CR8:CR8-, wherein both valencies are bound vicinally to Ar1; R8, R9 and R10 = H, A, cycloalkyl comprising 3 to 7 C atoms, Hal, et al.; Y = O, S, NR21, C(R22)-NO2, C(R22)-CN and C(CN)2; g = 1-3, preferably 1 or 2, p, r = 0-5; q = 0-4, preferably 0, 1 or 2; addnl. details are given in the claims. The experimental process involved the reaction of 2-(2-Nitro-4-(trifluoromethyl)phenyl)acetonitrile(cas: 13544-06-4).COA of Formula: C9H5F3N2O2

The Article related to aryl urea preparation raf kinase inhibitor antitumor agent, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.COA of Formula: C9H5F3N2O2

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

On September 30, 2018, Hebishy, Ali M. S.; Abdelhamid, Ismail A.; Elwahy, Ahmed H. M. published an article.Product Details of 75629-62-8 The title of the article was Synthesis of novel bis(dihydropyridine) and terpyridine derivatives. And the article contained the following:

A synthesis of novel bis(cyanopyridones) by the reaction of the appropriate bis(cyanoacetamide) with the corresponding arylidenemalononitrile in the presence of basic catalysts was reported. In some cases, the corresponding bis(2-cyano-3-arylacrylamide) derivatives were isolated from these reactions as single products. The multicomponent strategy for the synthesis of the target compounds was also investigated. The utility of bis(cyanoacetamides) as building blocks for novel bisquinolinones was also studied. The experimental process involved the reaction of 2-((1H-Indol-3-yl)methylene)malononitrile(cas: 75629-62-8).Product Details of 75629-62-8

The Article related to cyanopyridone preparation, cyanoacetamide arylidenemalonitrile michael addition cyclization, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.Product Details of 75629-62-8

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

Srour, Aladdin M.; Dawood, Dina H.; Saleh, Dalia O. published an article in 2021, the title of the article was Synthesis, 3D-pharmacophore modelling and 2D-QSAR study of new pyridine-3-carbonitriles as vasorelaxant active agents.Related Products of 75629-62-8 And the article contains the following content:

A new set of pyridine-3-carbonitriles conjugated with various five-membered ring systems at pyridinyl C-6 were designed and synthesized as vasorelaxant active agents. The majority of the new target derivatives exhibited noteworthy vasodilation efficacy and nine compounds were the most potent analogs with IC50 values = 220.7, 256.7, 164.1, 252.2, 229.8, 265.2, 247.9, 239.1 and 159.8μM, resp., which were superior to that of prazosin hydrochloride (IC50 = 272.8μM). Moreover, four compounds displayed significant α1-adrenergic receptor (α1-AR) blocking efficiency ranging from 65.38 to 87.86% compared with 89.34% for prazosin hydrochloride. Furthermore, a 2D-QSAR study and 3D-pharmacophore model were introduced to carry out compare-fit study for the designed mols. with the generated hypothesis and creating a statistically significant model. 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 pyridine carbonitrile preparation pharmacophore modeling vasorelaxant active agent hypertension, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.Related Products of 75629-62-8

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

On September 8, 2016, Rajkumar, Vadla; Babu, Srinivasarao Arulananda; Padmavathi, Rayavarapu published an article.HPLC of Formula: 75629-62-8 The title of the article was Regio- and diastereoselective construction of a new set of functionalized pyrrolidine, spiropyrrolidine and spiropyrrolizidine scaffolds appended with aryl- and heteroaryl moieties via the azomethine ylide cycloadditions. And the article contained the following:

Highly regio- and diastereoselective syntheses of a new set of functionalized pyrrolidines, spiro-pyrrolidine/pyrrolizidine oxindoles, spiroacenaphthylenolyl-pyrrolidines/pyrrolizidines and spiro-1,3-indandionolyl-pyrrolidines/pyrrolizidines appended with various aryl- and heteroaryl moieties via the azomethine ylide cycloaddition reaction are reported. The Ag-catalyzed [3+2] cycloaddition of azomethine ylides derived from N-benzylideneiminoglycinates with various arylidene/heteroarylidenemalononitriles gave C-3,C-5-aryl/heteroaryl substituted C-4,C-4-dicyanopyrrolidine-2-carboxylate scaffolds with good regio- and diastereoselectivity. Further, the [3+2] cycloaddition of azomethine ylides derived from the decarboxylative reactions of different 1,2-dicarbonyls and α-amino acids with the indole/pyrrole-based dipolarophiles were studied. In the context of enriching the library of functionalized spiropyrrolidine- and spiropyrrolizidine scaffolds, these reactions led to the assembling of various spiro-pyrrolidine/pyrrolizidine oxindoles, spiroacenaphthylenolyl-pyrrolidines/pyrrolizidines and spiro-1,3-indandionolyl-pyrrolidines/pyrrolizidines appended with the indolyl- and pyrrolyl moieties at the C-3 position of the spiro-pyrrolidine/pyrrolizidine rings. The stereochem. of the cycloadducts was assigned based on the single crystal x-ray structures of representative major diastereomers obtained from the azomethine ylide cycloaddition reactions. The experimental process involved the reaction of 2-((1H-Indol-3-yl)methylene)malononitrile(cas: 75629-62-8).HPLC of Formula: 75629-62-8

The Article related to spiropyrrolidine spiropyrrolizidine aryl azomethine ylide cycloaddition regio diastereoselective preparation, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.HPLC of Formula: 75629-62-8

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

On January 31, 2006, Zahouily, Mohamed; Bahlaouan, Bouchaib; Abrouki, Younes; Salah, Mohamed; Bahlaouan, Ouafa; Rayadh, Ahmed; Aadil, Mina; Sebti, Said published an article.Application In Synthesis of 2-(2,3-Dihydro-1H-inden-1-ylidene)malononitrile The title of the article was Natural phosphate and potassium fluoride doped natural phosphate as new catalysts for the Vilsmeier-Haack type reaction. And the article contained the following:

The catalytic activity of the inexpensive natural- or potassium fluoride doped- phosphates as bases was evaluated in a Vilsmeier-Haack type reaction. High efficiency, in term of chem. yields and reaction rates was found in the preparation of 2-chlor-3-cyanopyridines starting from 2-propylidene-malononitriles. 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 propylidene malononitrile vilsmeier haack reaction natural phosphate catalyst, pyridine chlor cyano preparation, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.Application In Synthesis of 2-(2,3-Dihydro-1H-inden-1-ylidene)malononitrile

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

On February 1, 2021, Yang, Bowen; Wu, Qian; Huan, Xiajuan; Wang, Yingqing; Sun, Yin; Yang, Yueyue; Liu, Tongchao; Wang, Xin; Chen, Lin; Xiong, Bing; Zhao, Dongmei; Miao, Zehong; Chen, Danqi published an article.Category: nitriles-buliding-blocks The title of the article was Discovery of a series of 1H-pyrrolo[2,3-b]pyridine compounds as potent TNIK inhibitors. And the article contained the following:

In an inhouse screening, 1H-pyrrolo[2,3-b]pyridine scaffold was found to have high inhibition on TNIK. Several series of compounds were designed and synthesized, among which some compounds had potent TNIK inhibition with IC50 values lower than 1 nM. Some compounds showed concentration-dependent characteristics of IL-2 inhibition. These results provided new applications of TNIK inhibitors and new prospects of TNIK as a drug target. The experimental process involved the reaction of 3-Amino-5-(tetramethyl-1,3,2-dioxaborolan-2-yl)benzonitrile(cas: 1036991-35-1).Category: nitriles-buliding-blocks

The Article related to pyrrolopyridine drug discovery synthesis potent tnik inhibitor, 1h-pyrrolo[2,3-b]pyridine, il-2 secretion inhibitory, tnik inhibitor, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.Category: nitriles-buliding-blocks

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts