Tag: 100-200

On October 21, 2021, Arnold, Lee D.; Lopatin, Uri; Keung, Walter published a patent.Synthetic Route of 39919-70-5 The title of the patent was Preparation of peptidomimetics as inhibitors of cysteine proteases for treatment of viral infections including COVID-19. And the patent contained the following:

The invention is related to the preparation of broad spectrum, viral protease inhibitor compounds, e.g., I, comprising a warhead covalently bound to a 3CL protease inhibitor, wherein the inhibitor compound covalently binds to Cys on the protease, and wherein the inhibitor compound is active against multiple such as viruses caliciviruses, picornaviruses and coronaviruses. The compounds are contemplated to inhibit proteases, such as the 3C, CL- or 3CL-like protease. Thus, I was prepared by Ugi reaction between pyridine-3-carbaldehyde, 4-tert-butylaniline, (2R,4S)-1-tert-butoxycarbonyl-4-hydroxypyrrolidine-2-carboxylic acid and isocyanocyclohexane followed by cleavage of the tert-butoxycarbonyl group in II and treatment with BrCN. Select compounds of the invention were evaluated for their antiviral activity against COVID-19 (nCoV-2019, SARS-CoV2) Mpro in an enzymic assay and against human coronavirus 229E and OC43 in the cytopathic effect assays. The experimental process involved the reaction of 6-(tert-Butyl)pyridin-3-amine(cas: 39919-70-5).Synthetic Route of 39919-70-5

The Article related to peptidomimetic preparation viral cysteine protease inhibitor viral infection treatment, cysteine protease inhibitor antiviral sarscov2 covid19 mpro peptidomimetic preparation, covid19 treatment peptidomimetic preparation and other aspects.Synthetic Route of 39919-70-5

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On November 9, 2000, Dow, Robert Lee; Liu, Kevin Kun-Chin; Morgan, Bradley Paul; Swick, Andrew Gordon published a patent.Reference of 4-(Chloromethyl)-2-methoxy-6-methylpyridine The title of the patent was Preparation of nonracemic octahydrophenanthrene and other tricyclic derivatives as selective modulators of glucocorticoid receptors. And the patent contained the following:

Title compounds [e.g., I; D = CR7, CR7R16, N, NR7, O’ E = C, CR6, N; F = CR4, CR4R5, O; R = XR1; R1 = H, alkyl, acylalkyl, arylalkyl, etc.; R2 = H, halo, alkyl, alkoxy, etc.; R3 = H, alkyl, arylalkyl, etc.; 1 of R2,R3 = null when adjacent dashed line = bond; R4,R5 = H, cyano, alkyl, alkoxy, etc.; R4R5 = O; R6 = H, cyano, alkyl, alkoxy, OH, etc.; R7,R16 = H, halo, cyano, alkyl, etc.; R7R16 = O; R8R9 = atoms to complete a substituted heteroaromatic ring; R14,R15 = H, halo, alkyl, alkoxy, etc.; R14R15 = O when adjacent dashed lines = null; X = bond, CH2, CH(OH), CO; Z = (un)substituted CH2, -CH2CH2, -CH2CO, CO, etc.; dashed lines = optional bonds] were prepared as glucocorticoid receptor modulators (no data). E.g., 6-methoxy-2-tetralone was alkylated by formation of the pyrrolidine enamine and alkylation with benzyl bromide; the benzylated ketone then undergoes asym. Michael addition with Me vinyl ketone in the presence of (S)-(-)-α-methylbenzylamine followed by cyclocondensation with sodium methoxide to give a nonracemic methoxytetrahydrophenanthrenone derivative E.g., demethylation of the methoxytetrahydrophenanthrenone with boron trichloride, reduction of the enone with lithium and ammonia, addition of 1-lithiopropyne to the ketone, formation of the aryl triflate with triflic anhydride and carbonylation with carbon monoxide in the presence in the presence of palladium acetate and bis(diphenylphosphino)propanol gives an hydroxyoctahydrophenanthrenecarboxylic acid derivative which is coupled with 4-(aminomethyl)pyridine in the presence of trimethylaluminum to give the octahydrophenanthrenecarboxamide II as one of the title compounds The experimental process involved the reaction of 4-(Chloromethyl)-2-methoxy-6-methylpyridine(cas: 1227595-34-7).Reference of 4-(Chloromethyl)-2-methoxy-6-methylpyridine

The Article related to nonsteroidal glucocorticoid receptor selective agonist antagonist preparation, treatment obesity diabetes inflammation nonsteroidal glucocorticoid receptor modulator, glucocorticoid receptor modulator preparation and other aspects.Reference of 4-(Chloromethyl)-2-methoxy-6-methylpyridine

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Yang, Bing; Jiang, Xin; Guo, Qing; Lei, Tao; Zhang, Li-Ping; Chen, Bin; Tung, Chen-Ho; Wu, Li-Zhu published an article in 2016, the title of the article was Self-Assembled Amphiphilic Water Oxidation Catalysts: Control of O-O Bond Formation Pathways by Different Aggregation Patterns.Formula: C5H5NO3S And the article contains the following content:

The oxidation of water to mol. oxygen is the key step to realize water splitting from both biol. and chem. perspective. In an effort to understand how water oxidation occurs on a mol. level, a large number of mol. catalysts have been synthesized to find an easy access to higher oxidation states as well as their capacity to make O-O bond. However, most of them function in a mixture of organic solvent and water and the O-O bond formation pathway is still a subject of intense debate. Herein, we design the first amphiphilic Ru-bda (H2bda=2,2′-bipyridine-6,6′-dicarboxylic acid) water oxidation catalysts (WOCs) of formula [RuII(bda)(4-OTEG-pyridine)2] (1, OTEG=OCH2CH2OCH2CH2OCH3) and [RuII(bda)(PySO3Na)2] (2, PySO3-=pyridine-3-sulfonate), which possess good solubility in water. Dynamic light scattering (DLS), scanning electron microscope (SEM), critical aggregation concentration (CAC) experiments and product anal. demonstrate that they enable to self-assemble in water and form the O-O bond through different routes even though they have the same bda2- backbone. This work illustrates for the first time that the O-O bond formation pathway can be regulated by the interaction of ancillary ligands at supramol. level. The experimental process involved the reaction of Pyridine-3-sulfonic acid(cas: 636-73-7).Formula: C5H5NO3S

The Article related to self assembled amphiphilic water oxidation catalyst, control oxygen oxygen bond formation pathway different aggregation pattern, amphiphilic complexes, catalysis, ruthenium complex, self-assembly, water oxidation and other aspects.Formula: C5H5NO3S

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On August 6, 2007, Baysal, Akin; Aydemir, Murat; Durap, Feyyaz; Guemguem, Bahattin; Oezkar, Saim; Yildirim, Leyla Tatar published an article.Formula: C10H10N4 The title of the article was Synthesis and characterizations of 3,3′-bis(diphenylphosphinoamine)-2,2′-bipyridine and 3,3′-bis(diphenylphosphinite)-2,2′-bipyridine and their chalcogenides. And the article contained the following:

New bis(phosphinoamine) and bis(phosphinite) derivatives of 2,2′-bipyridine were prepared through a single step reaction of 3,3′-diamino-2,2′-bipyridine or 3,3′-dihydroxy-2,2′-bipyridine with diphenylchlorophosphine, resp. Their P = E chalcogenide phosphinates (E = O, S, Se) were also prepared All the new compounds were characterized by elemental anal., IR and NMR spectroscopies. The mol. structure of 3,3′-bis(diphenylthiophosphinate)-2,2′-bipyridine was elucidated by single-crystal x-ray crystallog. The experimental process involved the reaction of [2,2′-Bipyridine]-3,3′-diamine(cas: 75449-26-2).Formula: C10H10N4

The Article related to crystal structure bipyridinediyl bisthiophosphinate, mol structure bipyridinediyl bisthiophosphinate, bipyridine phosphinoamino phosphinite preparation oxidation, chalcogenide phosphinate bipyridine preparation and other aspects.Formula: C10H10N4

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On July 30, 1999, Franco, D.; Panyella, D.; Rocamora, M.; Gomez, M.; Clinet, J. C.; Muller, G.; Dunach, E. published an article.Recommanded Product: 2-(4,5-Dihydro-4,4-dimethyl-2-oxazolyl)pyridine The title of the article was Electrochemical cleavage of allyl aryl ethers and allylation of carbonyl compounds: umpolung of allyl-palladium species. And the article contained the following:

The electrochem., Pd-catalyzed cleavage of the carbon-oxygen bond of allyl aryl ethers has been examined; the method constitutes a new alternative for allyl ether deprotection. The allyl transfer from the allyl ether to the carbonyl group in 2-allyloxy benzaldehyde is reported and is an example of allyl-Pd reactivity umpolung. Pd(II) complexes, associated to several nitrogen ligands are efficient catalyst precursors for these electrochem. reactions. The experimental process involved the reaction of 2-(4,5-Dihydro-4,4-dimethyl-2-oxazolyl)pyridine(cas: 109660-12-0).Recommanded Product: 2-(4,5-Dihydro-4,4-dimethyl-2-oxazolyl)pyridine

The Article related to allyl aryl ether electrochem cleavage, electrochem ether cleavage catalyst palladium complex, aryl allyl ether deprotection electrochem cleavage, allylsalicylaldehyde allyl transfer palladium chloride catalyst and other aspects.Recommanded Product: 2-(4,5-Dihydro-4,4-dimethyl-2-oxazolyl)pyridine

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On June 5, 2014, Walsh, Shawn P.; Cato, Brian; Frie, Jessica L.; Kim, Dooseop; Pasternak, Alexander; Shi, Zhi-Cai published a patent.Recommanded Product: 868551-99-9 The title of the patent was Preparation of piperidine derivatives as inhibitors of the renal outer medullary potassium channel for treating cardiovascular diseases and edematous conditions. And the patent contained the following:

The present invention provides compounds of Formula I (wherein n = 0-1; the N-containing ring system is (un)substituted piperidinyl, etc.; R1 is -H, -OC1-3alkyl or -OH; R2 is -H or C1-3alkyl; R3 is -H, -F, -C1-3 alkyl or phenyl; or when n is 0, R2 and R3 are joined together to form a 4-6 member ring with the nitrogen and carbon to which each is attached; R4 and R5 are each independently -H or -C1-3-alkyl, or R4 and R5 are joined together with the carbon to which they are attached to form C3-6 cycloalkyl; Z1 is (un)substituted Ph, (un)substituted benzofuranyl, or (un)substituted benzopyranyl, and Z2 is a substituted N-containing heterocyclyl, (un)substituted Ph, etc.), and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and conditions associated with excessive salt and water retention. Synthetic procedures for preparing I are exemplified. Example compound II was prepared by reacting intermediates 1-oxo-N-(piperidin-4-yl)-1,3-dihydroisobenzofuran-5-carboxamide hydrochloride and (4-methyl-1-oxo-1,3-dihydro-2-benzofuran-5-yl)acetaldehyde. In the ROMK channel functional thallium flux assay, II had an IC50 of 0.01 μM. The experimental process involved the reaction of Methyl 5-amino-4-methylpicolinate(cas: 868551-99-9).Recommanded Product: 868551-99-9

The Article related to preparation piperidine derivative inhibitor renal medullary potassium channel, cardiovascular disease piperidine derivative inhibitor renal medullary potassium channel, edema treatment piperidine derivative inhibitor renal medullary potassium channel and other aspects.Recommanded Product: 868551-99-9

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On April 21, 2006, van Herrikhuyzen, Jeroen; Jonkheijm, Pascal; Schenning, Albertus P. H. J.; Meijer, E. W. published an article.Quality Control of [2,2′-Bipyridine]-3,3′-diamine The title of the article was The influence of hydrogen bonding and π-π stacking interactions on the self-assembly properties of C3-symmetrical oligo(p-phenylenevinylene) discs. And the article contained the following:

Three nonracemic C3-sym. oligophenylenevinylenes (OPV) are prepared and characterized; the UV/visible and IR spectra of the products in solution are determined and used to characterize the structures formed by self-assembly of the OPV. OPVs with triaminobenzene and benzenetricarboxamide cores show two-step transitions from helical stacks to molecularly dissolved species; the orientation of the amide relative to the core determines the stabilities and helicities of fibers in solution and the lengths of fibrils formed at surfaces. An OPV with a tris(2,2′-bipyridin-3-yl)benzenetricarboxamide core forms aggregates that show little chiral ordering but which remain present over a large temperature range; at surfaces, completely disordered structures exist as a result of competing types of π-π stacking interactions that differ in strength and orientation. The design of functional self-assembled architectures based on hydrogen bonding and π-π stacking interactions requires careful balancing of the topologies, directionalities and strengths of secondary interactions. 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 oligophenylenevinylene nonracemic preparation uv visible spectra self assembly, aggregation pi stacking hydrogen bonding interaction nonracemic oligophenylenevinylene, hydrogen bonding pi interaction self assembly sym oligophenylenevinylene disk and other aspects.Quality Control of [2,2′-Bipyridine]-3,3′-diamine

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On February 29, 1992, Alo, Babajide I.; Familoni, Oluwole B.; Marsais, Francis; Queguiner, Guy published an article.Safety of Pyridine-3-sulfonic acid The title of the article was Directed metalation of pyridinesulfonamides. Synthesis of pyridine-fused isothiazoles and 1,2-oxathioles. And the article contained the following:

4-Lithio-N-tert-butylpyridine-3-sulfonamide reacted with Ph2CO or CO2 to give the corresponding intermediates, which on appropriate treatment gave the addition product I (from Ph2CO reaction product) or isothiazolo[5,4-c]pyridin-3-one 1,1-dioxides II (R = H, Me3C) (from CO2 reaction product). Metalation of 2- and 4-[N,N-(dialkylamino)sulfonyl]pyridines with LiN(CHMe2)2 gave anions which reacted with Ph2CO to give carbinols, which cyclized thermally to 1,2-oxathiolo[3,4-b]- III and -[4,3-c]pyridine dioxide IV, resp. The experimental process involved the reaction of Pyridine-3-sulfonic acid(cas: 636-73-7).Safety of Pyridine-3-sulfonic acid

The Article related to sultone pyridine fused, sultam pyridine fused, pyridinesulfonamide directed lithiation, isothiazolopyridinone dioxide, oxathiolopyridine, aminosulfonylpyridine lithiated reaction benzophenone, intramol cyclocondensation sulfonylpyridylmethanol and other aspects.Safety of Pyridine-3-sulfonic acid

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On July 21, 2005, Kelly, Michael G.; Janagani, Satyanarayana; Wu, Guoxian; Kincaid, John; Lonergan, David; Fang, Yunfeng; Wei, Zhi-Liang published a patent.Related Products of 39919-70-5 The title of the patent was Preparation of bicycloheteroarylamines like 2,6-naphthyridinamines and pyrido[3,4-d]pyrimidinamine as ion channel ligands and uses thereof. And the patent contained the following:

Amine compounds (shown as I; or a pharmaceutically acceptable salt, solvate or prodrug thereof; and stereoisomers and tautomers thereof; variables defined below; e.g. 7-(3-chloropyridin-2-yl)-N-[4-(trifluoromethyl)phenyl]-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-4-amine (shown as II)) that are VR1 (VR = vanilloid receptor) antagonists are disclosed. The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of nonlimiting example, pain, inflammation, traumatic injury, and others. Compounds I are considered to be particularly beneficial as VR1 antagonists as certain compounds exhibit improved aqueous solubility and metabolic stability. For I: A and B = CH2, CR2’R2′, CO, CS and NR2′; Y = CH2, CR2’R2′ and NR2′; W and Z = CR4 and N, provided that W and Z both can not be N; R1 = (un)substituted aliphatic, alkyl, heteroalkyl, acyl, aryl, heteroaryl, aralkyl, heteroalkyl; each of R2 and R2′ = H, or (un)substituted C1-C6 alkyl, C1-C6 cycloalkyl, aryl and aralkyl; R3 = (un)substituted C1-C6 alkyl, aryl, heteroaryl, heteroalkyl, cycloalkyl, cycloheteroalkyl, cycloalkenyl, cycloheteroalkenyl, bicycloalkyl, bicycloheteroalkyl, bicycloalkenyl, bicycloheteroalkenyl, bicycloaryl, and bicycloheteroaryl ring. R4 = H, or (un)substituted alkyl, (un)substituted acyl, (un)substituted acylamino, (un)substituted alkylamino, (un)substituted alkylthio, (un)substituted alkoxy, (un)substituted alkoxycarbonyl, (un)substituted alkylarylamino, (un)substituted arylalkyloxy, amino, (un)substituted aryl, arylalkyl, (un)substituted sulfoxide, (un)substituted sulfone, (un)substituted mercapto, (un)substituted aminosulfonyl, (un)substituted arylsulfonyl, sulfuric acid, sulfuric acid ester, (un)substituted dihydroxyphosphoryl, (un)substituted aminodihydroxyphosphoryl, azido, carboxy, (un)substituted carbamoyl, carboxy, cyano, (un)substituted cycloalkyl, (un)substituted cycloheteroalkyl, (un)substituted dialkylamino, halo, heteroaryloxy, (un)substituted heteroaryl, (un)substituted heteroalkyl, hydroxy, nitro, and thio. Although the methods of preparation are not claimed, 62 example preparations are included. For example, II was prepared in 5 steps (90, 38, 91, 87, 26 % yields) starting from 1-benzyl-3-(ethoxycarbonyl)-4-piperidone hydrochloride, formamidine acetate and NaOMe/MeOH and involving intermediates 7-benzyl-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-4(3H)-one, 7-benzyl-4-chloro-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidine, 7-benzyl-N-[4-(trifluoromethyl)phenyl]-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-4-amine, and N-[4-(trifluoromethyl)phenyl]-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-4-amine. VR1 antagonist activity for 62 examples of I, capsaicin-induced VR1 current inhibition activity for 16 examples of I, reversal of thermal hyperalgesia in rats by II, pharmacokinetic profiles for 5 examples of I and plasma protein binding ability by II are reported. The experimental process involved the reaction of 6-(tert-Butyl)pyridin-3-amine(cas: 39919-70-5).Related Products of 39919-70-5

The Article related to naphthyridinamine pyridopyrimidinamine preparation vanilloid receptor antagonist, ion channel ligand naphthyridinamine pyridopyrimidinamine preparation, pain inflammation traumatic injury drug naphthyridinamine pyridopyrimidinamine preparation and other aspects.Related Products of 39919-70-5

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On October 15, 2007, Wang, Jian; Djukic, Brandon; Cao, Jingyi; Alberola, Antonio; Razavi, Fereidoon S.; Pilkington, Melanie published an article.HPLC of Formula: 75449-26-2 The title of the article was A novel bis tridentate bipyridine carboxamide ligand and its complexation to copper(II): synthesis, structure, and magnetism. And the article contained the following:

A new bis tridentate ligand 2,2′-bipyridine-3,3′-[2-pyridinecarboxamide] H2L1 which can bind transition metal ions was synthesized via the condensation of 3,3′-diamino-2,2′-bipyridine together with 2-pyridine carbonyl chloride. Two Cu(II) coordination compounds were prepared and characterized: [Cu2(L1)(hfac)2].3MeCN.H2O (1) and [Cu2(L1)Cl2].MeCN (2). The single-crystal x-ray structures reveal that complex 1 crystallizes in the triclinic space group P1̅, with a 12.7185(6), b 17.3792(9), c 19.4696(8) Å, α 110.827(2), β 99.890(3), γ 97.966(3)°, Z = 4, R = 0.0321 and Rw = 0.0826. Complex 2 crystallizes in the monoclinic space group P21/n with a 12.8622(12), b 9.6100(10), c 19.897(2) Å, β 102.027(3)°, Z = 4, R = 0.0409 and Rw = 0.1005. In both complexes the ligand is in the dianionic form and coordinates the divalent CuII ions via one amido and two pyridine N donor atoms. In 1, the coordination geometry around both CuII ions is best described as distorted trigonal bipyramidal where the remaining two coordination sites are satisfied by hexafluoroacetylacetonate counterions. In 2 both CuII ions adopt a (4 + 1) distorted square pyramidal geometry. One Cu forms a longer apical bond to an adjacent carbonyl O atom, whereas the second Cu is chelated to a neighboring Cu-Cl chloride ion to afford a μ-Cl-bridged dimerized [Cu2(L1)Cl2]2 complex. The magnetic susceptibility data for 1 (2 -270 K), reveal the occurrence of weak antiferromagnetic interactions between the CuII ions. In contrast, variable-temperature magnetic susceptibility measurements for 2 reveal more complex magnetic properties, with the presence of a weak antiferromagnetic exchange (J = -10.1 K) between the Cu ions in each dinuclear Cu complex and a stronger ferromagnetic exchange interaction (J = 32.9 K) between the CuII ions of the Cu(μ-Cl)2Cu dimeric bridging units. The experimental process involved the reaction of [2,2′-Bipyridine]-3,3′-diamine(cas: 75449-26-2).HPLC of Formula: 75449-26-2

The Article related to copper bipyridinepyridinecarboxamide preparation structure magnetic exchange, crystal structure copper bipyridinepyridinecarboxamide fluoroacac chloro dinuclear, exchange ferromagnetic antiferromagnetic copper bipyridinepyridinecarboxamide and other aspects.HPLC of Formula: 75449-26-2

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem