Tag: 200-300

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 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 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 February 1, 2007, Ng, Raymond A.; Guan, Jihua; Alford, Vernon C.; Lanter, James C.; Allan, George F.; Sbriscia, Tifanie; Linton, Olivia; Lundeen, Scott G.; Sui, Zhihua published an article.Recommanded Product: 4,5-Diamino-2-(trifluoromethyl)benzonitrile The title of the article was Synthesis and SAR of potent and selective androgen receptor antagonists: 5,6-Dichloro-benzimidazole derivatives. And the article contained the following:

The synthesis and in vivo SAR of 5,6-dichloro-benzimidazole derivatives as novel selective androgen receptor antagonists were described. During screening of 2-alkyl benzimidazoles, it was found that a trifluoromethyl group greatly enhances antagonist activity in the prostate. Benzimidazole I was a potent AR antagonist in the rat prostate (ID50 = 0.15 mg/day). The experimental process involved the reaction of 4,5-Diamino-2-(trifluoromethyl)benzonitrile(cas: 882978-62-3).Recommanded Product: 4,5-Diamino-2-(trifluoromethyl)benzonitrile

The Article related to benzimidazole dichloro derivative preparation androgen receptor antagonist sar, Heterocyclic Compounds (More Than One Hetero Atom): Imidazoles and other aspects.Recommanded Product: 4,5-Diamino-2-(trifluoromethyl)benzonitrile

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Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

On April 13, 2006, Ng, Raymond; Sui, Zhihua; Guan, Jihua; Lanter, James C.; Alford, Vernon C., Jr. published a patent.Electric Literature of 882978-62-3 The title of the patent was Preparation of benzimidazole derivatives as selective androgen receptor modulators. And the patent contained the following:

Title compounds represented by the formula I [wherein R1 = H, alkyl, CH2-aryl, alkyl-OH, etc.; R2, R3 = independently H, halo, (halo)alkyl, etc.; n = 0 or 1; R4 = H, (halo)alkyl or OCOR8; R8 = (cyclo)alkyl, (hetero)aryl, aralkyl, etc.; R5 = H, halo or (halo)alkyl; R6 = (halo)alkyl, alkyl-OH, CH2-aryl, etc.; and pharmaceutically acceptable salts thereof] were prepared as selective androgen receptor modulators (SARMS). For example, oxidation of 2-(5,6-dichloro-1-ethyl-1H-benzimidazol-2-yl)-1-ethanesulfanylpropan-2-ol by mCPBA gave II. II showed activity in ventral prostate and seminal vesicle weight in vivo assay and ventral prostate and levator ani weight in vivo assay. Thus, I and their pharmaceutical compositions are useful for the treatment of disorders and conditions modulated by the androgen receptor. The experimental process involved the reaction of 4,5-Diamino-2-(trifluoromethyl)benzonitrile(cas: 882978-62-3).Electric Literature of 882978-62-3

The Article related to benzimidazole preparation selective androgen receptor modulator, Heterocyclic Compounds (More Than One Hetero Atom): Imidazoles and other aspects.Electric Literature of 882978-62-3

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

On April 13, 2006, Ng, Raymond; Sui, Zhihua; Guan, Jihua; Lanter, James C.; Alford, Vernon C., Jr. published a patent.COA of Formula: C8H6F3N3 The title of the patent was Preparation of benzimidazole derivatives as selective androgen receptor modulators. And the patent contained the following:

Title compounds represented by the formula I [wherein R1 = H, alkyl, CH2-aryl, alkyl-OH, etc.; R2 = H, halo, (halo)alkyl, etc.; n = 0 or 1; R10 = H, halo, (halo)alkyl or OCOR8; R8 = (cyclo)alkyl, (hetero)aryl, aralkyl, etc.; R11 = H or halo; or R10and R11 are taken together with the carbon atom to which they are bound to form CO, C=N(OH) or C=N(O-alkyl); R12 = (halo)alkyl, alkyl-OH, CH2-aryl, etc.; and pharmaceutically acceptable salts thereof] were prepared as selective androgen receptor modulators (SARMS). For example, oxidation of 2-(5,6-dichloro-1-ethyl-1H-benzimidazol-2-yl)-1-ethanesulfanylpropan-2-ol by mCPBA gave II. II showed activity in ventral prostate and seminal vesicle weight in vivo assay and ventral prostate and levator ani weight in vivo assay. Thus, I and their pharmaceutical compositions are useful for the treatment of disorders and conditions modulated by the androgen receptor. The experimental process involved the reaction of 4,5-Diamino-2-(trifluoromethyl)benzonitrile(cas: 882978-62-3).COA of Formula: C8H6F3N3

The Article related to benzimidazole preparation selective androgen receptor modulator, Heterocyclic Compounds (More Than One Hetero Atom): Imidazoles and other aspects.COA of Formula: C8H6F3N3

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

Thanassi, John W. published an article in 1975, the title of the article was Reactions of aminomalononitrile with electrophiles.Related Products of 5098-14-6 And the article contains the following content:

Aminomalononitrile reacted with electrophiles, aldehydes and CH2:CHCN, under very mild conditions of temperature and pH to produce intermediates which, after acid hydrolysis, yielded amino acids, glycine, DL-erythro- and DL-threo-β-hydroxyaspartic acids, DL-glutamic acid, DL-threonine and allothreonine. The mechanism of their formation and the possible significance of these reactions in prebiotic syntheses are discussed. The experimental process involved the reaction of 2-Aminomalononitrile 4-methylbenzenesulfonate(cas: 5098-14-6).Related Products of 5098-14-6

The Article related to aminomalononitrile electrophile reaction, aldehyde aminomalononitrile reaction, acrylonitrile aminomalononitrile reaction, amino acid biogenetic model, Synthesis of Amino Acids, Peptides, and Proteins: Amino Acids and other aspects.Related Products of 5098-14-6

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

On October 31, 1980, Taylor, Edward C.; Sun, Jung Hui published an article.Quality Control of 2-Aminomalononitrile 4-methylbenzenesulfonate The title of the article was A new synthesis of aminomalononitrile tosylate. And the article contained the following:

The title salt (I) was prepared from NaCH(CN)2. Thus, 2,4,6-Me3C6H2SO2ONH2 was added to NaCH(CN)2 in THF, the mixture stirred under N2 2.5 h at 0°, the 2,4,6-Me3C6H2SO3Na formed was separated, 4-MeC6H4SO3H added, and the mixture refrigerated overnight to give I. The experimental process involved the reaction of 2-Aminomalononitrile 4-methylbenzenesulfonate(cas: 5098-14-6).Quality Control of 2-Aminomalononitrile 4-methylbenzenesulfonate

The Article related to aminomalononitrile tosylate, malononitrile amino tosylate, Aliphatic Compounds: Nitriles, Isonitriles, and Acyl Cyanides and other aspects.Quality Control of 2-Aminomalononitrile 4-methylbenzenesulfonate

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Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

On March 2, 2016, Bujok, Robert; Wrobel, Zbigniew; Wojciechowski, Krzysztof published an article.Reference of 2-(2-Nitro-4-(trifluoromethyl)phenyl)acetonitrile The title of the article was Simple synthesis of 4-cyanoquinoline N-oxides. And the article contained the following:

4-Cyanoquinoline-N-oxides I (X = H, Cl, CF3, CN; Y = H, Cl, I, F, CF3, Ph, SPh, SMe; Z = H, Br) were obtained in the reactions of 2-nitrobenzyl cyanide carbanions with acrylonitrile. The experimental process involved the reaction of 2-(2-Nitro-4-(trifluoromethyl)phenyl)acetonitrile(cas: 13544-06-4).Reference of 2-(2-Nitro-4-(trifluoromethyl)phenyl)acetonitrile

The Article related to nitrobenzyl cyanide acrylonitrile base, cyanoquinoline oxide preparation, Heterocyclic Compounds (One Hetero Atom): Quinolines and Isoquinolines and other aspects.Reference of 2-(2-Nitro-4-(trifluoromethyl)phenyl)acetonitrile

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Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

Boche, Gernot; Mendiola, Javier; Rincon, Juan A.; Mateos, Carlos; Soriano, Jose Francisco; de Frutos, Oscar published an article in 2011, the title of the article was O-(mesitylsulfonyl)hydroxylamine.Recommanded Product: 2-Aminomalononitrile 4-methylbenzenesulfonate And the article contains the following content:

Synthesis, properties and applications of O-(mesitylsulfonyl)hydroxylamine as a reagent for electrophilic aminations, and for transfer of NH2 to electrophiles were reviewed. 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 review mesitylsulfonyl hydroxylamine preparation amination amino group transfer, Benzene, Its Derivatives, and Condensed Benzenoid Compounds: Reviews and other aspects.Recommanded Product: 2-Aminomalononitrile 4-methylbenzenesulfonate

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Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts