Tag: 100-200

On March 17, 2016, Kato, Taku; Sakamoto, Toshiaki; Niwa, Yasuki; Sawamoto, Daisuke; Ohtani, Naohito; Kanbe, Misaki published a patent.HPLC of Formula: 39919-70-5 The title of the patent was Preparation of aromatic carboxylic acid amides having TRPM8 blocking effect. And the patent contained the following:

Disclosed are compounds I [ring A = benzene or thiophene; X1 = CR11 or nitrogen atom; R11 = H or (un)substituted alkyl; X2, X3 = independently CH or nitrogen atom; ring C = monocyclic ring; R1 = (un)substituted alkyl, (un)substituted alkanoyl, cyano, etc.; R1 is substituted on the adjacent position to the point of attachment to ring B; R2 = H, (un)substituted alkyl or halo; R3 = cyano, -Ra, -N(Rb)(Rc), etc.; Ra = (un)substituted alkyl, (un)substituted non-aromatic heterocycle-methyl-, (un)substituted alkenyl, etc.; Rb = (un)substituted alkyl, (un)substituted alkenyl, (un)substituted cycloalkyl, etc.; Rc = H, (un)substituted alkyl, (un)substituted alkenyl, etc.; R4 = (un)substituted alkyl, (un)substituted alkanoyl, cyano, etc.; n = 0 or 1; R5 = H, (un)substituted alkyl, hydroxy, etc.; when n is 1, R4 and R5, together with ring C, may combine to form a bicyclic ring; or pharmacol. acceptable salts thereof]. For example, compound II was prepared from 5-bromo-3-fluoropyridine-2-carboxylic acid Et ester via conversion into 3-iodo-5-[2-(trifluoromethyl)phenyl]pyridine-2-carboxylic acid followed by amidation with 5-amino-2-trifluoromethylpyridine and reaction with 5-methyl-2-pyrrolidone. In TRPM8 blocking test, 361-example of I showed IC50 values (nmol/L) ranging from 0.2 to 2760, e.g., IC50 of II was 4 nmol/L. Of note, compounds I are useful for the treatment of chronic pain. The experimental process involved the reaction of 6-(tert-Butyl)pyridin-3-amine(cas: 39919-70-5).HPLC of Formula: 39919-70-5

The Article related to aromatic carboxylic acid amide preparation trpm8 blocker, chronic pain treatment aromatic carboxylic acid amide trpm8 blocking, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.HPLC of Formula: 39919-70-5

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On December 7, 2017, Kato, Taku; Sakamoto, Toshiaki; Niwa, Yasuki; Sawamoto, Daisuke; Otani, Naohito; Kanbe, Misaki published a patent.COA of Formula: C9H14N2 The title of the patent was Preparation of aromatic carboxylic acid amides having TRPM8 blocking effect. And the patent contained the following:

Disclosed are compounds I [ring A = benzene or thiophene; X1 = CR11 or nitrogen atom; R11 = H or (un)substituted alkyl; X2, X3 = independently CH or nitrogen atom; ring C = monocyclic ring; R1 = (un)substituted alkyl, (un)substituted alkanoyl, cyano, etc.; R1 is substituted on the adjacent position to the point of attachment to ring B; R2 = H, (un)substituted alkyl or halo; R3 = cyano, -Ra, -N(Rb)(Rc), etc.; Ra = (un)substituted alkyl, (un)substituted non-aromatic heterocycle-methyl-, (un)substituted alkenyl, etc.; Rb = (un)substituted alkyl, (un)substituted alkenyl, (un)substituted cycloalkyl, etc.; Rc = H, (un)substituted alkyl, (un)substituted alkenyl, etc.; R4 = (un)substituted alkyl, (un)substituted alkanoyl, cyano, etc.; n = 0 or 1; R5 = H, (un)substituted alkyl, hydroxy, etc.; when n is 1, R4 and R5, together with ring C, may combine to form a bicyclic ring; or pharmacol. acceptable salts thereof]. For example, compound II was prepared from 5-bromo-3-fluoropyridine-2-carboxylic acid Et ester via conversion into 3-iodo-5-[2-(trifluoromethyl)phenyl]pyridine-2-carboxylic acid followed by amidation with 5-amino-2-trifluoromethylpyridine and reaction with 5-methyl-2-pyrrolidone. In TRPM8 blocking test, 361-example of I showed IC50 values (nmol/L) ranging from 0.2 to 2760, e.g., IC50 of II was 4 nmol/L. Of note, compounds I are useful for the treatment of chronic pain. The experimental process involved the reaction of 6-(tert-Butyl)pyridin-3-amine(cas: 39919-70-5).COA of Formula: C9H14N2

The Article related to aromatic carboxylic acid amide preparation trpm8 blocker, chronic pain treatment aromatic carboxylic acid amide trpm8 blocking, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.COA of Formula: C9H14N2

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Balicki, R.; Kaczmarek, L.; Sobotka, W.; Ejmocki, Z. published an article in 1989, the title of the article was Insect chitin formation inhibitors. III. Synthesis and activity of some bis[3-(2,6-dihalobenzoyl)-1-ureido]bipyridines.COA of Formula: C10H10N4 And the article contains the following content:

Eight title compounds I (R, R1 = Cl, F) were prepared in 69-89% yields by a 4-step procedure starting from nitriles II. I have significant activity against house-flies (no data). The experimental process involved the reaction of [2,2′-Bipyridine]-3,3′-diamine(cas: 75449-26-2).COA of Formula: C10H10N4

The Article related to ureidobipyridine preparation insecticide, bipyridine ureido preparation insecticide, insect chitin formation inhibitor, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.COA of Formula: C10H10N4

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On March 24, 2009, Yuan, Chester Chenguang published a patent.Name: 6-(tert-Butyl)pyridin-3-amine The title of the patent was Preparation of substituted arylamine derivatives, particularly 2-aminonicotinamides, as antitumor agents. And the patent contained the following:

The invention is related to the preparation of a compound or a pharmaceutically acceptable derivative thereof, wherein the compound is 3-[(7-isoquinolinyl)amino]-N-[3-methyl-4-(1-methylethyl)phenyl]-3-pyridinecarboxamide are prepared and to its use as an effective agent for treatment of angiogenesis and related diseases such as cancer. Thus, acylation of 7-amino-4,4-dimethyl-3,4-dihydro-1H-isoquinoline-2-carboxylic acid tert-Bu ester with 2-chloropyridine-3-carbonyl chloride, followed by amination of the chloride intermediate (no data) with 7-aminoisoquinoline and deprotection gave 2-[(7-isoquinolinyl)amino]-N-(1,2,3,4-tetrahydro-4,4-dimethyl-7-isoquinolinyl)-3-piperidinecarboxamide monohydrochloride. Selected compounds of the invention inhibited VEGF-stimulated HUVEC proliferation at a level below 1 μM. In the tumor model, compounds of the invention are active at doses less than 150 mpk. The experimental process involved the reaction of 6-(tert-Butyl)pyridin-3-amine(cas: 39919-70-5).Name: 6-(tert-Butyl)pyridin-3-amine

The Article related to arylamine preparation antitumor angiogenesis inhibitor, pyridinecarboxamide amino preparation neoplasm vegf inhibitor, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.Name: 6-(tert-Butyl)pyridin-3-amine

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Breant, P.; Marsais, F.; Queguiner, G. published an article in 1983, the title of the article was Regioselective lithiation of 3-pyridylsulfonic acid derivatives: a convenient route to various new 4-substituted 3-pyridylsulfonamides.Computed Properties of 636-73-7 And the article contains the following content:

Pyridinesulfonamides I [NR2 = piperidino, morpholino, pyrrolidino; R1 = C(OH)Ph2, (un)substituted α-hydroxybenzyl] were prepared from lithiopyridines II and the resp. carbonyl compounds Amide III was treated at -60° with (Me2CH)2NH and BuLi in Et2O, PhCHO in Et2O was added at -70°, and the mixture was stirred 2 h at -70° to give I [NR2 = piperidino, R1 = PhCH(OH)]. The experimental process involved the reaction of Pyridine-3-sulfonic acid(cas: 636-73-7).Computed Properties of 636-73-7

The Article related to addition lithiopyridinesulfonamide benzaldehyde, pyridinesulfonamide hydroxybenzyl, hydroxybenzylpyridinesulfonamide, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.Computed Properties of 636-73-7

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On February 28, 1985, Sakamoto, Takao; Kaneda, Sohichi; Nishimura, Sumiko; Yamanaka, Hiroshi published an article.Computed Properties of 97483-79-9 The title of the article was Site-selectivity in the cyanation of 3-substituted pyridine 1-oxides with trimethylsilanecarbonitrile. And the article contained the following:

Treatment of pyridine 1-oxides I (R = Br, Cl, F, OMe, NMe2, Me, Et, Ph, CONEt2, CO2Et, cyano) with Me3SiCN gave 2- and 6-cyanopyridines II and III. The II – III ratio was strongly influenced by R, with II being the only product when R = F, OMe, NMe2. Nitropyridine 1-oxides underwent deoxygenation but not cyanation with Me3SiCN. The experimental process involved the reaction of Ethyl 6-cyanopicolinate(cas: 97483-79-9).Computed Properties of 97483-79-9

The Article related to pyridine oxide trimethylsilyl cyanide cyanation, cyanopyridine, deoxygenation pyridine oxide trimethylsilyl cyanide, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.Computed Properties of 97483-79-9

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On December 31, 1985, Kaczmarek, Lukasz published an article.Electric Literature of 75449-26-2 The title of the article was Bipyridines. Part XVIII. On the synthesis of [2,2′-bipyridin]-3-ol and other novel 2,2′-bipyridine derivatives from [2,2′-bipyridine]-3,3′-diamine. And the article contained the following:

Diazotization of bipyridinediamine I (R = R1 = NH2) in AcOH gave hydroxylamines I (R = NHOH, R1 = H, Ac); however, diazotization of Cu(II) complex of I (R = R1 = NH2) gave bipyridinamine I (R = NH2, R1 = H). Diazotization of the latter gave bipyridinol I (R = OH, R1 = H). The experimental process involved the reaction of [2,2′-Bipyridine]-3,3′-diamine(cas: 75449-26-2).Electric Literature of 75449-26-2

The Article related to bipyridinediamine diazotization, bipyridinamide preparation diazotization, bipyridinol, bipyridinehydroxylamine, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.Electric Literature of 75449-26-2

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Cremlyn, Richard J.; Jones, Graham P.; Swinbourne, Fred J.; Yung, Kin published an article in 1980, the title of the article was Some reactions of pyridine-3-sulfonyl chloride.Reference of Pyridine-3-sulfonic acid And the article contains the following content:

Reaction of pyridine-3-sulfonyl chloride-HCl (I) with hydrazine gave the hydrazide from which a semicarbazide and a series of hydrazones were obtained. The chem. shifts of the NH protons of the hydrazones were correlated with the Hammett σ-constants of the substituents. With NaN3 I gave the azide which reacted with both norbornene and Ph3P. I was hydrolyzed to the sulfonic acid by boiling with EtOH. Reaction of the hydrazide with β-diketones afforded the pyrazoles, e.g. II. The intermediate sulfonohydrazones were isolated in each case; however, the product with Et acetoacetate could not be cyclised to the pyrazole. The mass spectra of the pyrazoles are briefly discussed. The experimental process involved the reaction of Pyridine-3-sulfonic acid(cas: 636-73-7).Reference of Pyridine-3-sulfonic acid

The Article related to pyridinesulfonyl chloride reaction, nmr pyridinesulfonyl hydrazone hammett constant, pyrazole pyridylsulfonyl, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.Reference of Pyridine-3-sulfonic acid

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On May 19, 2022, Kopf, Sara; Liu, Jiali; Franke, Robert; Jiao, Haijun; Neumann, Helfried; Beller, Matthias published an article.Recommanded Product: 109660-12-0 The title of the article was Base-Mediated Remote Deuteration of N-Heteroarenes – Broad Scope and Mechanism. And the article contained the following:

Using KOtBu as base and DMSO-d6 as deuterium source, a general and applicable method was presented for the selective deuteration of a set of nitrogen-containing heterocycles (pyridines, azines and bioactive mols.). Exptl. and DFT mechanistic studies indicated that this reaction proceeded via deprotonation of the substrates by the dimsyl anion. The relative thermodn. stability of the heterocycle anions determines the distribution and degree of deuteration. The experimental process involved the reaction of 2-(4,5-Dihydro-4,4-dimethyl-2-oxazolyl)pyridine(cas: 109660-12-0).Recommanded Product: 109660-12-0

The Article related to heteroarene deuterated dimethyl sulfoxide regioselective deuteration, deuterated heteroarene preparation, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.Recommanded Product: 109660-12-0

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On February 28, 1990, Sobotka, Wieslaw; Styczynska, Bogumila; Balicki, Roman; Kozlowska, Margarita; Krzeminska, Alicja; Kaczmarek, Lukasz; Ejmocki, Zdzislaw published a patent.Quality Control of [2,2′-Bipyridine]-3,3′-diamine The title of the patent was Preparation of new bis[3-(2,6-disubstituted benzoyl)-1-ureyl]bipyridines as insecticides. And the patent contained the following:

Title compounds I (R, R1 = H, C1-4 alkoxy, halo, CF3) are prepared by reaction of corresponding disubstituted benzoyl isocyanates with bipyridine diamines in an inert solvent at 20-120°. For example, 4,4′-bipyridine-3,3′-diamine reacted with 2 mol equiv 2,6-ClFC6H3CONCO in CH2Cl2 at 40° to give 86.3% title compound II. Eight I showed varying degrees of effectiveness as chitin synthesis inhibitors when applied to larval Musca domestica. The experimental process involved the reaction of [2,2′-Bipyridine]-3,3′-diamine(cas: 75449-26-2).Quality Control of [2,2′-Bipyridine]-3,3′-diamine

The Article related to benzoylureylbipyridine preparation insecticide, bipyridine benzoylureyl preparation chitin inhibitor, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.Quality Control of [2,2′-Bipyridine]-3,3′-diamine

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem