Tag: 200-300

On September 23, 2021, Lancellotti, Patrizio; Oury, Cecile; Pirotte, Bernard; Musumeci, Lucia; Jacques, Nicolas; Goffin, Eric published a patent.Product Details of 85426-79-5 The title of the patent was Preparation of pyrimidine derivatives for prevention and treatment of Gram-negative bacterial infection, contamination and fouling. And the patent contained the following:

This invention relates to new pyrimidine derivatives I [X1 and X2 = (independently) N, (un)substituted CH (with the exception that if one of X1 or X2 is N, then the remaining of X1 or X2 = (un)substituted CH); Y = O or S; R1 and R2 = (independently) alkyl, cycloalkyl, aryl, etc.; R3-R7 = (independently) H, halo, alkyl, etc.] or pharmaceutically acceptable acid addition salts, together with a membrane penetrating agent, optionally with a detectable isotope and pharmaceutical composition for use in treatment or prevention of Gram-neg. bacterial infection in a host mammal in need of such treatment or prevention and use as inhibitors of Gram-neg. biofilm formation on a surface of biomaterial or medical device, particularly of cardiovascular device such as prosthetic heart valve or pacemakers. E.g., a multi-step synthesis of (1R,2S)-II, starting from 4,6-dichloro-2-(propylthio)pyrimidin-5-amine and methylamine, was disclosed. Antibacterial effects of representative compounds I together with Polymyxin B Nonapeptide (membrane penetrating agent) on Escherichia coli were examined (data given). A method of diagnosing or prognosing a Gram-neg. bacterial infection in a host mammal comprising using the pyrimidine derivatives I together with a membrane penetrating agent, was disclosed. The experimental process involved the reaction of 4-Chloro-6-(methylthio)-1H-pyrazolo[3,4-d]pyrimidine(cas: 85426-79-5).Product Details of 85426-79-5

The Article related to pyrimidine derivative pyrrolopyrimidinamine phenylcyclopropyl preparation gram neg bacterial infection, antibacterial combination chemotherapy membrane penetrating agent pyrrolopyrimidinamine phenylcyclopropyl preparation and other aspects.Product Details of 85426-79-5

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

Nicolaou, K. C.; Rhoades, Derek; Wang, Yanping; Totokotsopoulos, Sotirios; Bai, Ruoli; Hamel, Ernest published an article in 2015, the title of the article was Synthesis and Biological Evaluation of Novel Epothilone B Side Chain Analogues.Formula: C8H11BrN2O And the article contains the following content:

The design, synthesis, and biol. evaluation of a series of epothilone analogs with novel side chains equipped with an amino group are described. Their design facilitates potential conjugation to selective drug delivery systems such as antibodies. Their synthesis proceeded efficiently via Stille coupling of a readily available vinyl iodide and heterocyclic stannanes. Cytotoxicity studies and tubulin binding assays revealed two of these analogs, I (R = CF3, F), to be more potent than epothilones A-D and the anticancer agent ixabepilone, currently in clin. use. The experimental process involved the reaction of 5-Bromo-1-(tetrahydro-2H-pyran-2-yl)-1H-pyrazole(cas: 1187582-58-6).Formula: C8H11BrN2O

The Article related to epothilone b side chain analog preparation antitumor structure activity, tubulin binding epothilone b side chain analog, antibody-drug conjugates, anticancer agents, epothilones, organic synthesis, tubulin binding agents and other aspects.Formula: C8H11BrN2O

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

On March 12, 2009, Demeese, Jason; Gaudino, John; Neitzel, Alicia Tarin; Lunghofer, Paul; Jeongbeob, Seo; Hongqi, Tian; Young, Wendy B.; Sutherlin, Daniel P. published a patent.HPLC of Formula: 924909-16-0 The title of the patent was Preparation of pyrazolopyridines as tyrosine kinase inhibitors. And the patent contained the following:

Title compounds[I, II; X = O, S, NR10; W = O, S, SO, SO2; R1 = H, alkyl, alkenyl, alkynyl, CONR10R11, (substituted) carbocyclyl, heterocyclyl, aryl, heteroaryl, etc.; R2 = H, CF3, cyano, NR10R11, (substituted) alkyl, alkenyl, alkynyl, carbocyclyl, heterocyclyl, aryl, heteroaryl, etc.; R3 = (substituted) carbocyclyl, heterocyclyl, aryl, heteroaryl; R4 = H, F, Cl, Br, CF3, cyano, NR10R11, OR10, etc.; R10, R11 = H, (substituted) alkyl, alkenyl, alkynyl, carbocyclyl, heteroaryl, etc.], were prepared as c-MET kinase inhibitors (no data). Thus, title compound (III) was prepared in 13 steps from 2,2-dimethyl-1,3-dioxane-4,6-dione, 1-(4-methoxybenzyl)-1H-pyrazol-5-amine, 1,2-difluoro-4-nitrobenzene, 1-(4-fluorophenyl)hydrazine hydrochloride, 1,3-dioxane-4,6-dione, and tert-Bu 4-hydroxypiperidine-1-carboxylate. The experimental process involved the reaction of 1-(4-Methoxybenzyl)-1H-pyrazolo[3,4-b]pyridin-4-ol(cas: 924909-16-0).HPLC of Formula: 924909-16-0

The Article related to pyrazolopyridine preparation tyrosine kinase inhibitor, cmet kinase inhibitor piperidinyloxypyrazolopyridine preparation, cancer stroke diabetes hepatomegaly alzheimers treatment phenoxypyrazolopyridine preparation and other aspects.HPLC of Formula: 924909-16-0

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

On June 2, 2011, Demeese, Jason; Gaudino, John; Neitzel, Alicia Tarin; Lunghofer, Paul; Seo, Jeongbeob; Tian, Hongqi; Young, Wendy B.; Sutherlin, Daniel P. published a patent.Formula: C14H13N3O2 The title of the patent was Preparation of pyrazolopyridines as tyrosine kinase inhibitors. And the patent contained the following:

Compounds of Formulas Ia and Ib, and stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting receptor tyrosine kinases and for treating disorders mediated thereby. Methods of using compounds of Formula Ia and Ib, and stereoisomers, geometric isomers, tautomers, solvates and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathol. conditions are disclosed. Title compounds[I, II; X = O, S, NR10; W = O, S, SO, SO2; R1 = H, alkyl, alkenyl, alkynyl, CONR10R11, (substituted) carbocyclyl, heterocyclyl, aryl, heteroaryl, etc.; R2 = H, CF3, cyano, NR10R11, (substituted) alkyl, alkenyl, alkynyl, carbocyclyl, heterocyclyl, aryl, heteroaryl, etc.; R3 = (substituted) carbocyclyl, heterocyclyl, aryl, heteroaryl; R4 = H, F, Cl, Br, CF3, cyano, NR10R11, OR10, etc.; R10, R11 = H, (substituted) alkyl, alkenyl, alkynyl, carbocyclyl, heteroaryl, etc.], were prepared as c-MET kinase inhibitors (no data). Thus, title compound (III) was prepared in 13 steps from 2,2-dimethyl-1,3-dioxane-4,6-dione, 1-(4-methoxybenzyl)-1H-pyrazol-5-amine, 1,2-difluoro-4-nitrobenzene, 1-(4-fluorophenyl)hydrazine hydrochloride, 1,3-dioxane-4,6-dione, and tert-Bu 4-hydroxypiperidine-1-carboxylate. The experimental process involved the reaction of 1-(4-Methoxybenzyl)-1H-pyrazolo[3,4-b]pyridin-4-ol(cas: 924909-16-0).Formula: C14H13N3O2

The Article related to pyrazolopyridine preparation tyrosine kinase inhibitor, cmet kinase inhibitor piperidinyloxypyrazolopyridine preparation, cancer stroke diabetes hepatomegaly alzheimers treatment phenoxypyrazolopyridine preparation and other aspects.Formula: C14H13N3O2

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

On May 31, 2003, Kim, Dong Chan; Lee, Yeo Ran; Yang, Beom-Seok; Shin, Kye Jung; Kim, Dong Jin; Chung, Bong Young; Yoo, Kyung Ho published an article.Quality Control of 4-Chloro-6-(methylthio)-1H-pyrazolo[3,4-d]pyrimidine The title of the article was Synthesis and biological evaluations of pyrazolo[3,4-d]pyrimidines as cyclin-dependent kinase 2 inhibitors. And the article contained the following:

A series of 1,4,6-trisubstituted pyrazolo[3,4-d]pyrimidines capable of selectively inhibiting CDK2 activity were synthesized by derivatization at C-4, C-6 and N-1 with various amines and lower alkyl groups. For above synthetic compounds, biol. evaluation was carried out and structure-activity relationship was examined In the series, 4-anilino compounds exhibited better CDK2 inhibitory activity and antitumor activity compared to 4-benzyl compounds Two compounds having a 3-fluoroaniline group at C-4 showed comparable or superior CDK2 inhibitory activity to those of olomoucine and roscovitine as reference compounds In general, the unsubstituted compounds at N-1 possessed higher potency than the substituted compounds for the CDK2 inhibitory activity. As for EGFR inhibitory activity, most compounds did not have a significant activity. Two compounds exhibited potent cell growth inhibitory activity against human cancer cell lines, but their CDK2 inhibitory activities were slightly poorer than olomoucine. The experimental process involved the reaction of 4-Chloro-6-(methylthio)-1H-pyrazolo[3,4-d]pyrimidine(cas: 85426-79-5).Quality Control of 4-Chloro-6-(methylthio)-1H-pyrazolo[3,4-d]pyrimidine

The Article related to pyrazolopyrimidine preparation cyclin dependent kinase 2 inhibitor, cdk2 inhibitor pyrazolopyrimidine preparation, egfr inhibitor pyrazolopyrimidine preparation, antitumor agent pyrazolopyrimidine preparation and other aspects.Quality Control of 4-Chloro-6-(methylthio)-1H-pyrazolo[3,4-d]pyrimidine

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

On December 31, 2012, Ablajan, Keyume; Wang, Liju published an article.Synthetic Route of 36640-53-6 The title of the article was Convenient synthesis and characterization of hydrazone derivatives of 3-(2-naphthyl)-1-phenyl-pyrazole-4-carbaldehyde. And the article contained the following:

In order to obtain novel hydrazone derivatives containing pyrazole and thiazole rings which possess certain biol. activity, a series of 1-(3-β-naphthyl-1-phenylpyrazole-4-methylene)-2-(4-arylthiazol-2-yl)hydrazones I(R = Ph, 4-Me-C6H4, 4-MeO-C6H4, 4-Cl-C6H4, 4-NO2-C6H4, 4-Br-C6H4, 2-naphthyl) were synthesized via two different methods including multi step reactions and one-pot synthetic route using 3-β-naphthyl-1-phenyl-pyrazole-4-carbaldehyde as a starting intermediate. The products were obtained in good yield under ultrasonic irradiation condition rather than heating. The structures of products were characterized by 1H NMR, MS and elemental anal. The preliminary bioassay showed that compounds I(R = 4-Me-C6H4, 4-Cl-C6H4) possess obvious protective effects on the PC12 cells injury induced by H2O2. The experimental process involved the reaction of 3-(Naphthalen-2-yl)-1-phenyl-1H-pyrazole-4-carbaldehyde(cas: 36640-53-6).Synthetic Route of 36640-53-6

The Article related to naphthylphenylpyrazolemethyleneaiylthiazolylhydrazone preparation pc12 cell protection, naphthylphenylpyrazole carbaldehyde preparation hydrazinecarbothioamide arylcarbonylmethyl bromide cyclocondensation and other aspects.Synthetic Route of 36640-53-6

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

On December 31, 2007, Shelke, S. N.; Dalvi, N. R.; Gill, C. H.; Karale, B. K. published an article.Synthetic Route of 36640-53-6 The title of the article was Synthesis of various heterocycles from 3-(2-naphthalenyl)-1-phenyl-1H-pyrazole-4-carboxaldehyde. And the article contained the following:

Condensation of the title compound (I) with 2′-hydroxyacetophenones gave propenones II (R1 = H, Cl, Me; R2, R4 = H, Me; R3 = H, Cl, Me, Et, Br, F), which reacted with hydrazine to give pyrazolines III and with iodine in DMSO to give chromones IV. Reaction of IV with hydrazine gave bipyrazoles V. The experimental process involved the reaction of 3-(Naphthalen-2-yl)-1-phenyl-1H-pyrazole-4-carbaldehyde(cas: 36640-53-6).Synthetic Route of 36640-53-6

The Article related to pyrazolecarboxaldehyde condensation hydroxyacetophenone, pyrazolylpyrazoline aryl derivative preparation, pyrazolylchromone aryl derivative preparation, bipyrazole aryl derivative preparation and other aspects.Synthetic Route of 36640-53-6

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

《Chemical Validation of DegS As a Target for the Development of Antibiotics with a Novel Mode of Action》 was published in ChemMedChem in 2019. These research results belong to Bongard, Jens; Schmitz, Anna Laura; Wolf, Alex; Zischinsky, Gunther; Pieren, Michel; Schellhorn, Birgit; Bravo-Rodriguez, Kenny; Schillinger, Jasmin; Koch, Uwe; Nussbaumer, Peter; Klebl, Bert; Steinmann, Joerg; Buer, Jan; Sanchez-Garcia, Elsa; Ehrmann, Michael; Kaiser, Markus. Safety of 4-(4-(tert-Butyl)phenyl)-1H-pyrazol-3-amine The article mentions the following:

Despite the availability of hundreds of antibiotic drugs, infectious diseases continue to remain one of the most notorious health issues. In addition, the disparity between the spread of multidrug-resistant pathogens and the development of novel classes of antibiotics exemplify an important unmet medical need that can only be addressed by identifying novel targets. Herein we demonstrate, by the development of the first in vivo active DegS inhibitors based on a pyrazolo[1,5-a]-1,3,5-triazine scaffold, that the serine protease DegS and the cell envelope stress-response pathway σE represent a target for generating antibiotics with a novel mode of action. Moreover, DegS inhibition is synergistic with well-established membrane-perturbing antibiotics, thereby opening promising avenues for rational antibiotic drug design.4-(4-(tert-Butyl)phenyl)-1H-pyrazol-3-amine(cas: 1015845-73-4Safety of 4-(4-(tert-Butyl)phenyl)-1H-pyrazol-3-amine) was used in this study.

4-(4-(tert-Butyl)phenyl)-1H-pyrazol-3-amine(cas: 1015845-73-4) belongs to anime. Many important products require amines as part of their syntheses. Methylamine is utilized in the production of the analgesic meperidine (trade name Demerol) and the photographic developer Metol (trademark), and dimethylamine is used in the synthesis of the antihistamine diphenhydramine (trade name Benadryl), the solvent dimethylformamide (DMF), and the rocket propellant 1,1-dimethylhydrazine. The synthesis of the insect repellent N,N-diethyl-m-toluamide (DEET) incorporates diethylamine while that of the synthetic fibre Kevlar requires aromatic amines.Safety of 4-(4-(tert-Butyl)phenyl)-1H-pyrazol-3-amine

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

Product Details of 847818-74-0In 2013 ,《Preparation of a diverse purine-scaffold library via one-step palladium catalyzed cross-coupling》 appeared in Heterocycles. The author of the article were Taldone, Tony; Zatorska, Danuta; Patel, Hardik J.; Sun, Weilin; Patel, Maulik R.; Chiosis, Gabriela. The article conveys some information:

In an ongoing efforts to prepare Hsp90 inhibitors (heat-shock proteins HSP 90 inhibitors), various cross-coupling reactions (Suzuki, Stille, Heck, and Sonogashira) were used to construct a diverse library of substituted purines in a single step from PU-H71. The authors showed show that these reactions, particularly a Suzuki coupling, are highly efficient, do not require protection of the pendant amine and due to a wide variety of com. available substrates, allow for the rapid development of a diverse purine library. The products derived from these reactions will permit the exploration of the chem. space occupied by the key 6′-iodine of PU-H71 through mols. with diverse phys. and chem. properties with the potential to be useful for diseases in which Hsp90 is implicated. The synthesis of the target compounds was achieved using 6-amino-8-[(6-iodo-1,3-benzodioxolyl)thio]-N-(1-methylethyl)-9H-purine-9-propanamine as a key starting material in a reaction with boronic acid derivatives., alkenes, alkynes and organotin compounds (stannane compounds). The title compounds thus formed included 6-amino-N-(1-methylethyl)-8-[[6-(2-oxazolyl)-1,3-benzodioxolyl]thio]-9H-purine-9-propanamine (I) and related substances, such as derivatives of pyrimidine, pyrazine, imidazole, thiazole, alkenes, isoxazole, pyrazole , furan, pyrrole, pyridine, cyclohexane, cyclopentane, alkyne derivatives In the part of experimental materials, we found many familiar compounds, such as 1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 847818-74-0Product Details of 847818-74-0)

1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 847818-74-0) belongs to pyrazoles. Pyrazoles are commonly used scaffold molecules in drug discovery projects. The use of pyrazole derivatives is based on their analgesic, anti-inflammatory, antipyretic, antiarrhythmic, sedative, muscle relaxant, neuroleptic, anticonvulsant, monoamine oxidase inhibitory, antidiabetic and antibacterial activities. Product Details of 847818-74-0

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

The author of 《Palladium-Promoted DNA-Compatible Heck Reaction》 were Wang, Xuan; Sun, Hui; Liu, Jiaxiang; Zhong, Wenge; Zhang, Mingqiang; Zhou, Hu; Dai, Dongcheng; Lu, Xiaojie. And the article was published in Organic Letters in 2019. HPLC of Formula: 847818-74-0 The author mentioned the following in the article:

Optimal conditions for palladium-promoted Heck reaction on DNA were developed with good to excellent conversions. Versatility with either DNA-conjugated styrene/acrylamide or aryl iodide and a broad substrate scope of the corresponding coupling partners were established. Furthermore, robustness of the Heck reaction conditions on single-strand DNA and feasibility for DNA-encoded library production were demonstrated. After reading the article, we found that the author used 1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 847818-74-0HPLC of Formula: 847818-74-0)

1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 847818-74-0) belongs to pyrazoles. Pyrazoles are commonly used scaffold molecules in drug discovery projects. The use of pyrazole derivatives is based on their analgesic, neuroleptic, anticonvulsant, monoamine oxidase inhibitory, anti-inflammatory, antipyretic, antiarrhythmic, sedative, muscle relaxant, antidiabetic and antibacterial activities. HPLC of Formula: 847818-74-0

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics