Month: October 2022

On March 30, 2017, Ma, Dawei; Yu, Qiang; Yuan, Junying; Xia, Hongguang; Cai, Dongpo; Wang, Kailiang; Zhang, Chen; Xia, Shanghua published a patent.Application of 16230-24-3 The title of the patent was 2,4-Diamino-5-(trifluoromethyl)pyridine-1,3-diaminobenzene-acrylamide derivatives as EGFR kinase inhibitors and their preparation, pharmaceutical compositions and use in the treatment of cancer. And the patent contained the following:

The invention provides 2,4-diamino-5-(trifluoromethyl)pyridine-1,3-diaminobenzene-acrylamide derivatives of formula I as EGFR kinase inhibitors and the preparation method and use thereof. Compounds of formula I wherein X and Y are independently N, CH; provided that X and Y are not CH at the same time; R is (un)substituted 5- to 7-membered heterocyclic ring, -NH-(un)substituted 5- to 7-membered heterocyclic ring, etc.; and their preparation method, as well as their use as EGFR kinase inhibitors in the treatment of cancer thereof, are claimed. Compounds of formula I were prepared by using condensation and deacylation as the key steps. All the invention compounds were evaluated for their EGFR inhibitory activity. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).Application of 16230-24-3

The Article related to trifluoromethyl pyridine diaminobenzene acrylamide preparation egfr inhibitor treatment cancer, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Application of 16230-24-3

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

On April 5, 2017, Ma, Dawei; Yu, Qiang; Yuan, Junying; Xia, Hongguang; Cai, Dongpo; Wang, Kailiang; Zhang, Chen; Xia, Shanghua published a patent.Application In Synthesis of N-(3-Aminophenyl)acrylamide The title of the patent was 2,4-Diamino-5-(trifluoromethyl)pyridine-1,3-diaminobenzene-acrylamide derivatives as EGFR kinase inhibitors and their preparation, pharmaceutical compositions and use in the treatment of cancer. And the patent contained the following:

The invention provides EGFR kinase inhibitor and its preparation method and application.Specifically, the invention provides a compound shown in formula (I), wherein the definition of each group is as noted in the instruction book.Described compound is the effective EGFR inhibitor. The invention provides 2,4-diamino-5-(trifluoromethyl)pyridine-1,3-diaminobenzene-acrylamide derivatives of formula I as EGFR kinase inhibitors and the preparation method and use thereof. Compounds of formula I wherein X and Y are independently N, CH; provided that X and Y are not CH at the same time; R is (un)substituted 5- to 7-membered heterocyclic ring, -NH-(un)substituted 5- to 7-membered heterocyclic ring, etc.; and their preparation method, as well as their use as EGFR kinase inhibitors in the treatment of cancer thereof, are claimed. Compounds of formula I were prepared by using condensation and deacylation as the key steps. All the invention compounds were evaluated for their EGFR inhibitory activity. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).Application In Synthesis of N-(3-Aminophenyl)acrylamide

The Article related to trifluoromethyl pyridine diaminobenzene acrylamide preparation egfr inhibitor treatment cancer, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Application In Synthesis of N-(3-Aminophenyl)acrylamide

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Ahmed, Ahmed A. M.; Mekky, Ahmed E. M.; Sanad, Sherif M. H. published an article in 2022, the title of the article was New piperazine-based bis(thieno[2,3-b]pyridine) and bis(pyrazolo[3,4-b]pyridine) hybrids linked to benzofuran units: Synthesis and in vitro screening of potential acetylcholinesterase inhibitors.Category: amides-buliding-blocks And the article contains the following content:

Two series of piperazine-based bis(thieno[2,3-b]pyridines) I (Y = CN, COMe, CONH2, COOEt, COPh) and bis(pyrazolo[3,4-b]pyridines) II (Z = H, Me, OMe, Cl, COOEt) were prepared in good yields, utilizing the appropriate bis(pyridinethione). The first series was obtained by reacting the previous synthon with different α-halogenated reagents, whereas the second series was produced by reacting the synthon with various hydrazonyl chlorides, and then cyclizing the resulting bis(hydrazonothioates). At 50 and 100μM concentrations, the two series were screened as potential acetylcholinesterase inhibitors. The reference donepezil had inhibition percentages of 90.7 and 93.5 at the tested concentrations Generally, bis(thieno[2,3-b]pyridine) series was found to be more effective than the other series of bis(pyrazolo[3,4-b]pyridine). Bis(thieno[2,3-b]pyridine-2-carbonitrile) inhibited acetylcholinesterase the best, with inhibition percentages of 55.2 and 88.4 at 50 and 100μM concentrations, resp. Furthermore, when tested at a concentration of 25μg/mL, the prior hybrid demonstrated the best DPPH antioxidant activity, with an inhibition percentage of 81.5 when compared to the reference ascorbic acid (inhibition percentage of 88.7). The experimental process involved the reaction of 2-Chloroacetamide(cas: 79-07-2).Category: amides-buliding-blocks

The Article related to piperazine thienopyridine pyrazolopyridine benzofuran preparation acetylcholinesterase inhibitor antioxidant, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Category: amides-buliding-blocks

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

On April 30, 2015, Huang, Min-yi; Xu, Wei; Huang, Jun-jun; Huang, Ya-jian; Yuan, Mu published an article.Formula: C11H9NO3 The title of the article was Synthesis, crystal structure and biological activity of N-(2-hydroxy-3-(4-(2-methoxyphenyl)-piperazin-1-yl)propyl)quinoxaline-2-methanamide. And the article contained the following:

The title compound N-(2-hydroxy-3-(4-(2-methoxyphenyl)piperazin-1-yl)propyl)-quinoxaline-2-methanamide (I, C23H27N5O3, Mr = 421.50) was synthesized via a four-step reaction and characterized by 1H NMR, 13C NMR, ESIMS and single-crystal X-ray diffraction. The crystal is of monoclinic, space group P21/n with a = 12.108(2), b = 12.639(3), c = 14.601(3) Å, β = 104.87(3)°, V = 2,159.6(8) Å3, Z = 4, Dc = 1.296 g/cm3, S = 1.023, μ = 0.088 mm-1, F(000) = 896, R = 0.0392 and wR = 0.0983 for 2,836 observed reflections with I>2σ (I). The single-crystal X-ray structural anal. reveals that I is stabilized by intramol. and intermol. hydrogen bonds together with π-π interactions. The bioassay showed that I exhibited high selective activity for α1A/D vs. α1B-adrenoceptors subtype. The experimental process involved the reaction of 2-(Oxiran-2-ylmethyl)isoindoline-1,3-dione(cas: 5455-98-1).Formula: C11H9NO3

The Article related to methoxyphenylpiperazinylpropyl quinoxalinecarboxamide preparation adrenoceptor antagonistic activity crystal mol structure, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Formula: C11H9NO3

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

On June 27, 2022, Chen, Yantao; Kollback, Johanna; Aurell, Carl-Johan published an article.COA of Formula: C13H12N2O The title of the article was An Improved Synthesis of 1λ;6,2,4,6-Thiatriazine-1,3,5-trione Derivatives – the Sulfonimidamide-featured Triazinones. And the article contained the following:

N,N’-dicarbamoylation of 4-methylbenzenesulfonimidamide with carbonyldiimidazole, followed by a mono-nucleophilic substitution with amines and subsequential ring closure in one-pot, afforded 1λ6,2,4,6-thiatriazine-1,3,5-trione derivatives I [R = cyclohexyl, Ph, 3-pyridyl, etc.] in up to 83% yields. The protocol also worked well for aliphatic sulfonimidamides, such as Me sulfonimidamide. The experimental process involved the reaction of 1,3-Diphenylurea(cas: 102-07-8).COA of Formula: C13H12N2O

The Article related to thiatriazine dione derivative preparation, amine thiatriazine dione oxide tandem diacylation nucleophilic substitution cyclization, Heterocyclic Compounds (More Than One Hetero Atom): Other 6-Membered Rings, Three Or More Hetero Atoms and other aspects.COA of Formula: C13H12N2O

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

On April 9, 2015, Chen, Yi published a patent.Recommanded Product: 16230-24-3 The title of the patent was Preparation of substituted [(6-phenyl-4-methyl-3-oxo-3,4-dihydropyrazin-2-yl)amino]benzene derivatives as inhibitors of bruton’s tyrosine kinase. And the patent contained the following:

The present invention provides compounds I [R0 and R1 = independently H, alkyl, alkenyl, alkynyl, cycloalkyl, etc.; L = N(Rd)(CH2)m; Rd = H, alkyl, alkenyl, alkynyl, cycloalkyl or heterocycloalkyl; m = 0-4; R2 = H or alkyl; R3 = H, halo, alkyl, or hydroxyalkyl; R4 = W, X, Y or Z; R5, R6, R7, R8, R9, R10, R11 and R12 = independently H, alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, halo, or alkoxy], or their N-oxides, pharmaceutically acceptable salts, solvates, polymorphs or tautomers. For example, compound II was prepared by coupling of compound III (preparation given) with compound IV (preparation given) followed by hydrolysis. The Kd value of compound II for bruton’s tyrosine kinase (BTK) was 0.86 nM, which clearly shows that compound II is a highly potent BTK inhibitor. The invention compounds are useful as inhibitors of bruton’s tyrosine kinase for the treatment of neoplastic disease, autoimmune disease and inflammatory disorder. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).Recommanded Product: 16230-24-3

The Article related to phenylmethyloxodihydropyrazinylaminobenzene compound preparation bruton tyrosine kinase inhibitor, neoplastic disease autoimmune disease inflammatory disorder treatment, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Recommanded Product: 16230-24-3

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

On July 28, 2016, Chen, Yi published a patent.Safety of N-(3-Aminophenyl)acrylamide The title of the patent was Preparation of substituted [(6-phenyl-4-methyl-3-oxo-3,4-dihydropyrazin-2-yl)amino]benzene derivatives as selective Bruton’s tyrosine kinase inhibitors. And the patent contained the following:

The invention provides compounds I [R0 and R1 = independently H, alkyl, alkenyl, alkynyl, cycloalkyl, etc.; L = N(Rd)(CH2)m; Rd = H, alkyl, alkenyl, alkynyl, cycloalkyl or heterocycloalkyl; m = 0-4; R2 = H or alkyl; R3 = H, halo, alkyl, or hydroxyalkyl; R4 = W, X, Y or Z; R5, R6, R7, R8, R9, R10, R11 and R12 = independently H, alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, halo, or alkoxy], or their N-oxides, pharmaceutically acceptable salts, solvates, polymorphs or tautomers. For example, compound II was prepared by coupling of compound III (preparation given) with compound IV (preparation given) followed by hydrolysis. The Kd value of compound II for Bruton’s tyrosine kinase (BTK) was 0.86 nM, which clearly shows that compound II is a highly potent BTK inhibitor. The invention compounds are useful as inhibitors of Bruton’s tyrosine kinase for the treatment of neoplastic disease, autoimmune disease and inflammatory disorder. The experimental process involved the reaction of N-(3-Aminophenyl)acrylamide(cas: 16230-24-3).Safety of N-(3-Aminophenyl)acrylamide

The Article related to phenylmethyloxodihydropyrazinylaminobenzene compound preparation bruton tyrosine kinase inhibitor, neoplastic disease autoimmune disease inflammatory disorder treatment, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Safety of N-(3-Aminophenyl)acrylamide

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

On February 28, 2021, Przybylek, Maciej; Walczak, Patrycja; Ziolkowska, Dorota; Grela, Izabela; Cysewski, Piotr published an article.Product Details of 144-80-9 The title of the article was Studies on the solid-liquid equilibria and intermolecular interactions Urea binary mixtures with Sulfanilamide and Sulfacetamide. And the article contained the following:

The binary phase diagrams of Sulfanilamide-Urea (SN-U) and Sulfacetamide-Urea (SC-U) were measured using differential scanning calorimetry technique (DSC). Both examined mixtures were found to form simple binary eutectics. The limited miscibility in the solid state observed by DSC, proving inability of co-crystallization in new multi-mol. form, was also confirmed using PXRD and FTIR-ATR measurements of solid dispersions obtained via liquid assisted co-grinding. The lack of intermol. complex formation in the crystals does not imply the lack of interactions in the liquid state. Detailed characteristics of potential homo- and hetero-mol. pairs were offered using ab initio and the first principle quantum chem. computations. The obtained results happened to be strongly dependent on the applied level of theory. The importance of including the zero point energy contributions and electron correlation corrections was emphasized. It was found that the mole fraction of hetero-complexes with urea is the highest among all other constituents of studied systems at their eutectic points. Finally, the importance of intermol. interaction leading to complexes formation in the liquid state at saturated position was documented by computed values of solvation Gibbs free energy. Based on computed trends it was inferred that the eutectic mixtures can be interpreted as such equilibrium for which mutual solvation of all components is maximized. The experimental process involved the reaction of N-((4-Aminophenyl)sulfonyl)acetamide(cas: 144-80-9).Product Details of 144-80-9

The Article related to sulfanilamide sulfacetamide urea solid liquid equilibrium intermol interaction, Thermodynamics, Thermochemistry, and Thermal Properties: Calorimetry, Thermal Analysis, Thermogravimetry and other aspects.Product Details of 144-80-9

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Alsudairi, Amell; Lajami, Amal; Kendrick, Ian; Mukerjee, Sanjeev; Abraham, K. M. published an article in 2019, the title of the article was Correlating ionic conductivity, oxygen transport and ORR with structure of dialkylacetamide-based electrolytes for lithium-air batteries.Category: amides-buliding-blocks And the article contains the following content:

Chem. structures of lithium and tetrabutylammonium (TBA) salt solutions in N,N-dimethylacetamide (DMAc) and N,N-diethylacetamide (DEAc), two high Donor Number organic solvents, were studied. In LiX salt solutions (where X = PF6-, CF3SO3-, ClO4- and NO3-), solvation occurs when the Li+ bonds with the solvent’s carbonyl group forming Li+[O=C(CH3)N(CH3)2]nX- ion pairs. IR and 13C-NMR spectra are consistent with the ion pair being solvent-separated when the anion is PF6-, ClO4- or NO3-, and a contact ion pair in the case of CF3SO3-. Chem. interactions between TBA+ and the solvents to form conducting solutions appeared to be dipolar in nature. Ionic conductivities of TBA+ and Li+ electrolytes were measured and correlated with their viscosities. In 0.1M TBAPF6/DMAc, the O2 solubility and diffusion coefficient (3.09 × 10-6 mol/cm-3 and 5.09 × 10-5 cm2s-1, resp.) measured using microelectrode technique are typical of values measured in several TBA+ solutions Microelectrode voltammetry revealed steady-state limiting current behavior for oxygen reduction reactions (ORR) in TBAX/DMAc electrolytes indicating a reversible ORR process. Conversely, microelectrode current-voltage data for ORR in LiX/DMAc electrolytes revealed irreversible behavior mainly ascribed to the blockage of the electrode surface by insoluble ORR products. The ORR in DMAc correlated with its high Donor Number and the overall process conformed to the Hard-Soft Acid-Base theory. The experimental process involved the reaction of N,N-Diethylacetamide(cas: 685-91-6).Category: amides-buliding-blocks

The Article related to ionic conductivity oxygen transport dialkylacetamide electrolyte lithium battery, Electrochemical, Radiational, and Thermal Energy Technology: Energy-Conversion Devices and Their Components and other aspects.Category: amides-buliding-blocks

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

On August 29, 1980, Elliott, Arthur J.; Gibson, Martin S. published an article.Quality Control of 3-Nitro-4-chlorobenzenesulfonamide The title of the article was Hydrazides and thiohydrazides as sources of condensed oxadiazines and thiadiazines, including novel azo derivatives based on dithizone. And the article contained the following:

Condensation reactions of N’-phenylbenzohydrazide, N’-phenylbenzothiohydrazide, and dithizone with a variety of activated aromatic and heteroaromatic 1,2-dihalo and 1-halo-2-nitro compounds are described in which the hydrazide or thiohydrazide functions as a bidentate nucleophile. These reactions lead to derivatives of the 4H-1,3,4-benzoxadiazines e.g. I, and 4H-1,3,4-benzothiadiazines and analogous pyrimido-, pyrazino-, and quinoxalinooxadiazines and -thiadiazines, which are representative of new ring systems. The corresponding reaction of N’-phenylbenzothiohydrazide with chloranil proceeds with expulsion of S. The experimental process involved the reaction of 3-Nitro-4-chlorobenzenesulfonamide(cas: 97-09-6).Quality Control of 3-Nitro-4-chlorobenzenesulfonamide

The Article related to cyclocondensation hydrazide thiohydrazide, oxadiazine condensed, thiadiazine condensed, benzoxadiazine, benzothiadiazine, Heterocyclic Compounds (More Than One Hetero Atom): Other 6-Membered Rings, Three, Four, Or Five Hetero Atoms and other aspects.Quality Control of 3-Nitro-4-chlorobenzenesulfonamide

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics