Author: Jessica.F

On May 31, 2019, Vadivelu, Saravanan; Rajagopal, Sridharan; Burri, Raghunadha Reddy; Garapaty, Shivani; Sivanandhan, Dhanalakshmi; Thakur, Manish Kumar; Natarajan, Tamizharasan; Swamy, Indu N.; Nagaraju, Nagendra; Kanagaraj, Subramaniam; Mohd, Zainuddin; Sarkar, Sayantani; Samanta, Swapan Kumar; Hariprakash published a patent.COA of Formula: C11H9NO3 The title of the patent was Preparation of heterocyclic compounds as PRMT5 inhibitors. And the patent contained the following:

The invention relates to compounds of formula I and their analogs, tautomeric forms, stereoisomers, polymorphs, hydrates, solvates, pharmaceutically acceptable salts, pharmaceutical compositions, metabolites, and prodrugs thereof as PRMT5 inhibitors; their preparation and use in the treatment of and/or prevention of various diseases, including cancer and infectious diseases. Compounds of formula I wherein A is substituted isoquinolinyl, dihydroindenylamino; dashed bond is optional single or double bond; n = 0-1; m = 0-2; p = 1-2; q = 1-3; R1 – R6 are independently H, halo, OH, etc.; R7 is H, C1-6 (un)substituted alkyl, (un)substituted aryl, etc.; R8 is absent, H, halo, C1-6 alkyl, etc.; R10 is H, halo, OH, CN, etc.; X, Y and Z are independently NH and derivatives, O, S, etc.; W and B are independently N and C; and their analogs, tautomeric forms, stereoisomers, polymorphs, hydrates, solvates, pharmaceutically acceptable salts, pharmaceutical compositions, metabolites, and prodrugs thereof, are claimed. Example compound II was prepared by amidation of 6-(trifluoromethyl)imidazo[1,2-a]pyridine-2-carboxylic acid with 1-amino-3-(3,4-dihydroisoquinolin-2(1H)-yl)propan-2-ol. The invention compounds were evaluated for their PRMT5 inhibitory activity. From the assay, it was determined that compound II exhibited IC50 value ranged from 0.01-1 μM. The experimental process involved the reaction of 2-(Oxiran-2-ylmethyl)isoindoline-1,3-dione(cas: 5455-98-1).COA of Formula: C11H9NO3

The Article related to heterocycle preparation prmt5 inhibitor treatment cancer infection, Heterocyclic Compounds (More Than One Hetero Atom): Fused-Ring Systems With Two Or More Hetero Atoms, No More Than One Hetero Atom Per Ring and other aspects.COA of Formula: C11H9NO3

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

On May 31, 2019, Vadivelu, Saravanan; Rajagopal, Sridharan; Burri, Raghunadha Reddy; Garapaty, Shivani; Sivanandhan, Dhanalakshmi; Thakur, Manish Kumar; Natarajan, Tamizharasan; Swamy, Indu N.; Nagaraju, Nagendra; Kanagaraj, Subramaniam; Mohd, Zainuddin; Sarkar, Sayantani; Samanta, Swapan Kumar; Hariprakash published a patent.Application In Synthesis of 2-(Oxiran-2-ylmethyl)isoindoline-1,3-dione The title of the patent was Preparation of heterocyclic compounds as PRMT5 inhibitors. And the patent contained the following:

The invention relates to compounds of formula I and their analogs, tautomeric forms, stereoisomers, polymorphs, hydrates, solvates, pharmaceutically acceptable salts, pharmaceutical compositions, metabolites, and prodrugs thereof as PRMT5 inhibitors; their preparation and use in the treatment of and/or prevention of various diseases, including cancer and infectious diseases. Compounds of formula I wherein A is substituted isoquinolinyl, dihydroindenylamino; dashed bond is optional single or double bond; n = 0-1; m = 0-2; p = 1-2; q = 1-3; R1 – R6 are independently H, halo, OH, etc.; R7 is H, C1-6 (un)substituted alkyl, (un)substituted aryl, etc.; R8 is absent, H, halo, C1-6 alkyl, etc.; R10 is H, halo, OH, CN, etc.; X, Y and Z are independently NH and derivatives, O, S, etc.; W and B are independently N and C; and their analogs, tautomeric forms, stereoisomers, polymorphs, hydrates, solvates, pharmaceutically acceptable salts, pharmaceutical compositions, metabolites, and prodrugs thereof, are claimed. Example compound II was prepared by amidation of 6-(trifluoromethyl)imidazo[1,2-a]pyridine-2-carboxylic acid with 1-amino-3-(3,4-dihydroisoquinolin-2(1H)-yl)propan-2-ol. The invention compounds were evaluated for their PRMT5 inhibitory activity. From the assay, it was determined that compound II exhibited IC50 value ranged from 0.01-1 μM. The experimental process involved the reaction of 2-(Oxiran-2-ylmethyl)isoindoline-1,3-dione(cas: 5455-98-1).Application In Synthesis of 2-(Oxiran-2-ylmethyl)isoindoline-1,3-dione

The Article related to heterocycle preparation prmt5 inhibitor treatment cancer infection, Heterocyclic Compounds (More Than One Hetero Atom): Fused-Ring Systems With Two Or More Hetero Atoms, No More Than One Hetero Atom Per Ring and other aspects.Application In Synthesis of 2-(Oxiran-2-ylmethyl)isoindoline-1,3-dione

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

Mekky, Ahmed E. M.; Sanad, Sherif M. H.; Said, Ahmed Y.; Elneairy, Mohamed A. A. published an article in 2020, the title of the article was Synthesis, cytotoxicity, in-vitro antibacterial screening and in-silico study of novel thieno[2,3-b]pyridines as potential pim-1 inhibitors.Quality Control of 2-Chloroacetamide And the article contains the following content:

A novel series of thieno[2,3-b]pyridines I [R = Me, MeO; R1 = acetyl, ethoxycarbonyl, aminocarbonyl, etc.] was prepared via an one-step protocol in excellent yields. The protocol involved the reaction of pyridine-2(1H)-thiones I with the appropriate halogen containing reagents in ethanolic sodium ethoxide solution under stirring at 80°C for 2 h. The new thienopyridines were screened against different bacterial and fungal strains. Thieno[2,3-b]pyridine-2-carboxylate I [R = Me; R1 = ethoxycarbonyl] showed the most effective antibacterial activities against each of Staphylococcus aureus and Escherichia coli with MIC/MBC values of 9.9/19.8 and 19.8/39.5μM, resp., when compared with Ciprofloxacin. I [R = Me; R1 = ethoxycarbonyl] was the most effective compound against MRSA with inhibition zone of 16.2 ± 0.6 mm, when compared with Gentamicin. Moreover, I [R = Me; R1 = ethoxycarbonyl] exhibited the best cytotoxic activity against each of HEPG2 and MCF-7 cell lines with IC50 values of 25.7 and 30.53μM, resp., when compared with Doxorubicin. The in-silico study was performed to predict the capability of new thienopyridines as potential inhibitors of pim-1 kinase. The experimental process involved the reaction of 2-Chloroacetamide(cas: 79-07-2).Quality Control of 2-Chloroacetamide

The Article related to thienopyridine preparation antibacterial activity antitumor pim kinase inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Fused-Ring Systems With Two Or More Hetero Atoms, No More Than One Hetero Atom Per Ring and other aspects.Quality Control of 2-Chloroacetamide

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

On July 13, 2020, Sanad, Sherif M. H.; Mekky, Ahmed E. M. published an article.Synthetic Route of 79-07-2 The title of the article was Novel Nicotinonitriles and Thieno[2,3-b]pyridines as Potent Biofilm and COX-2 Inhibitors: Synthesis, In Vitro and In Silico Studies. And the article contained the following:

(Cyano)diaryl-substituted pyridine-2(1H)-thiones were used to prepare two novel series of nicotinonitriles I (R1 = 2-thienyl, R2 = 4-ClC6H4; R1 = 1,3-benzodioxol-5-yl, R2 = 2-thienyl; R1 = 3,5-dibromo-4-ethoxyphenyl, R2 = 4-MeC6H4; R3 = MeCO, CN, H2NCO, 4-ClC6H4CO) and thieno[2,3-b]pyridines II (R1-R3 as above) using piperazine as an eco-friendly catalyst under ultrasonic irradiation The in vitro antibacterial activities of both series were estimated against different Gram-pos. and neg. bacterial strains. Moreover, the most potent antibacterial derivatives were subjected to further evaluation of their cytotoxic activity against HEPG2 and MCF-7 cell lines as well as their capability to inhibit COX-2 enzyme. The compound I (R1 = 1,3-benzodioxol-5-yl; R2 = 2-thienyl; R3 = H2NCO) gave the least MIC/MBC values of 4.8/9.6, 4.8/9.6 and 9.6/19.7μM against each of Staphylococcus aureus, Escherichia coli and Streptococcus mutans, resp., when compared with Ciprofloxacin. This compound I also showed the best biofilm inhibition activities with IC50 values in the range of 5.2-7.3μM against S. aureus, S. mutans and E. coli bacterial strains when compared with Ciprofloxacin, the best cytotoxic activity against HEPG2 and MCF-7 cell lines with IC50 of 23.9 and 29.8μM, resp., when compared with Doxorubicin and revealed nearly inhibition activity equipotent to Celecoxib with IC50 of 0.12μM. The in silico study was performed to predict the capability of the novel nicotinonitriles and thienopyridines as potent inhibitors of COX-2 enzyme. The experimental process involved the reaction of 2-Chloroacetamide(cas: 79-07-2).Synthetic Route of 79-07-2

The Article related to nicotinonitrile thienopyridine preparation antibacterial antitumor antibiofilm cox2 inhibitor human, Heterocyclic Compounds (More Than One Hetero Atom): Fused-Ring Systems With Two Or More Hetero Atoms, No More Than One Hetero Atom Per Ring and other aspects.Synthetic Route of 79-07-2

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

On August 4, 2017, Matsuzawa, Akinobu; Noda, Hidetoshi; Kumagai, Naoya; Shibasaki, Masakatsu published an article.Reference of N,N-Diethylacetamide The title of the article was Direct Catalytic Asymmetric Aldol Addition of an α-CF3 Amide to Arylglyoxal Hydrates. And the article contained the following:

Direct asym. aldol addition of an α-CF3 amide to arylglyoxal hydrates was promoted by a chiral catalyst comprising a soft Lewis acidic Cu(I), a chiral bisphosphine ligand, and DBU. The 7-azaindoline moiety of the amide facilitates its enolization and stabilizes the thus-generated Cu enolate, furnishing enantioenriched aldol adducts. The experimental process involved the reaction of N,N-Diethylacetamide(cas: 685-91-6).Reference of N,N-Diethylacetamide

The Article related to asym aldol addition alpha trifluoromethyl amide arylglyoxal hydrate, copper catalyzed addition azaindoline moiety enantioenriched aldol adduct preparation, Heterocyclic Compounds (More Than One Hetero Atom): Fused-Ring Systems With Two Or More Hetero Atoms, No More Than One Hetero Atom Per Ring and other aspects.Reference of N,N-Diethylacetamide

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

Vallejo-Sanchez, Daniel; Amo-Ochoa, Pilar; Beobide, Garikoitz; Castillo, Oscar; Froeba, Michael; Hoffmann, Frank; Luque, Antonio; Ocon, Pilar; Perez-Yanez, Sonia published an article in 2017, the title of the article was Chemically Resistant, Shapeable, and Conducting Metal-Organic Gels and Aerogels Built from Dithiooxamidato Ligand.Application of 685-91-6 And the article contains the following content:

Metal-organic gels (MOGs) appear as a blooming alternative to well-known metal-organic frameworks (MOFs). Porosity of MOGs has a microstructural origin and not strictly crystalline like in MOFs; therefore, gelation may provide porosity to any metal-organic system, including those with interesting properties but without a porous crystalline structure. The easy and straightforward shaping of MOGs contrasts with the need of binders for MOFs. In this contribution, a series of MOGs based on the assembly of 1D-coordination polymer nanofibers of formula [M(DTA)]n (MII: Ni, Cu, Pd; DTA: dithiooxamidato) are reported, in which properties such as porosity, chem. inertness, mech. robustness, and stimuli-responsive elec. conductivity are brought together. The strength of the M-S bond confers an unusual chem. resistance, withstanding exposure to acids, alkalis, and mild oxidizing/reducing chems. Supercritical drying of MOGs provides ultralight metal-organic aerogels (MOAs) with densities as low as 0.03 g cm-3 and plastic/brittle behavior depending on the nanofiber aspect ratio. Conductivity measurements reveal a semiconducting behavior (10-12 to 10-7 S cm-1 at 298 K) that can be improved by doping (10-5 S cm-1). Moreover, it must be stressed that conductivity of MOAs reversibly increases (up to 10-5 S cm-1) under the presence of acetic acid. The experimental process involved the reaction of N,N-Diethylacetamide(cas: 685-91-6).Application of 685-91-6

The Article related to metal organic aerogel built dithiooxamidato ligand chem resistant, Electric Phenomena: Conduction and Conductivity, Semiconductivity, Resistance, Current Carriers, Galvanomagnetic and Acoustoelectric Effects and other aspects.Application of 685-91-6

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

Polonski, T. published an article in 1983, the title of the article was Optical activity of lactones and lactams – II. Chiroptical properties of 4-oxazolidinones.Recommanded Product: (S)-2-Hydroxy-N-methyl-2-phenylacetamide And the article contains the following content:

Several optically active 4-oxazolidinones (e.g., I) were obtained from amides or N-methylamides of α-hydroxy acids. Solvent and substituent effects on their CD were studied. The predominance of the envelope conformation was established for these compounds, the degree of puckering being enhanced by polar solvents. The folded form with the aromatic ring facing the oxazolidinone ring was observed for 5-benzyloxazolidinone derivatives The experimental process involved the reaction of (S)-2-Hydroxy-N-methyl-2-phenylacetamide(cas: 65645-88-7).Recommanded Product: (S)-2-Hydroxy-N-methyl-2-phenylacetamide

The Article related to cd oxazolidinone conformation, Physical Organic Chemistry: Stereochemistry and Stereochemical Relationships, Including Conformational Inversions and Rotational Isomerization and other aspects.Recommanded Product: (S)-2-Hydroxy-N-methyl-2-phenylacetamide

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

On January 22, 2021, Li, Yanxiong; Xu, Liang; Meng, Faming; Yu, Yonghai published a patent.Recommanded Product: 65645-88-7 The title of the patent was Preparation of (S)-1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethylamine and chiral catalyst thereof. And the patent contained the following:

The invention relates to preparation of (S)-1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethylamine and chiral catalyst thereof, which has the advantages of high yield and simple method, low cost, environmentally friendly and safety. The (S)-1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethylamine was prepared by the following steps: mixing 1-(3-ethoxy-4-methoxy Phenyl)-2-(methylsulfonyl)vinylamine, chiral catalyst I, acid and solvent, performing isomerization to obtain the final product; where R=hydrogen atom, C1-20 linear alkyl, C3-20 branched chain alkyl, C3-10 cycloalkyl, C3-10 heterocyclyl, C1-20 alkoxy, trifluoromethyl, halogen, amino, cyano, hydroxyl, nitro, ester, amide, substituted or unsubstituted C6-20 aryl, substituted or unsubstituted C5-20 heteroaryl. The experimental process involved the reaction of (S)-2-Hydroxy-N-methyl-2-phenylacetamide(cas: 65645-88-7).Recommanded Product: 65645-88-7

The Article related to preparation ethoxymethoxyphenylmethylsulfonylethylamine chiral catalyst isomerization, Benzene, Its Derivatives, and Condensed Benzenoid Compounds: Phenols, Thiophenols, and Derivatives Including Phenol and Thiophenol Ethers and Esters and other aspects.Recommanded Product: 65645-88-7

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

Ghafouri, Moloud; Moghadam, Majid; Mehrani, Kheirollah; Daneshvar, Anahita published an article in 2018, the title of the article was Supported ruthenium hydride catalysts for direct conversion of alcohols to carboxylic acids using styrene oxide as oxidant.Formula: C10H11NO3 And the article contains the following content:

In the present work, the ability of two ruthenium hydride catalysts supported on multiwall carbon nanotubes, [Ru-H@EDT-MWCNT], and gold nanoparticles cored triazine dendrimer, [Ru-H@AuNPs-TD], in the direct conversion of alcs. to carboxylic acids via transfer hydrogenation using styrene oxide as oxidant is reported. Different alcs. were successfully converted to their corresponding carboxylic acids. The results showed that these two heterogeneous catalysts are more efficient than the homogeneous counterpart. In addition, the catalysts were reused several times. The experimental process involved the reaction of 2-(4-Methylbenzamido)acetic acid(cas: 27115-50-0).Formula: C10H11NO3

The Article related to ruthenium hydride catalyst supported alc styrene oxide, carboxylic acid preparation, Benzene, Its Derivatives, and Condensed Benzenoid Compounds: Carboxylic Acids and Peroxycarboxylic Acids and Their Sulfur-Containing Analogs and Salts and other aspects.Formula: C10H11NO3

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

On February 4, 2015, Zhou, Xiaomeng; Wang, Qing; Zhao, Weihua; Xu, Songsong; Zhang, Wei; Chen, Junmin published an article.Electric Literature of 27115-50-0 The title of the article was Palladium-catalyzed ortho-arylation of benzoic acid derivatives via C-H bond activation using an aminoacetic acid bidentate directing group. And the article contained the following:

A highly efficient protocol for the palladium-catalyzed ortho-arylation of benzoic acid derivatives by aryl iodides is described with an aminoacetic acid based N,O bidentate directing group. This protocol can be applied to various benzoyl aminoacetic acids and aryl iodides with both electron-donating and electron-withdrawing groups. Remarkably, the nature of a new directing group drives selective C-H bond activation to afford only monoarylation products in good to excellent yields. The experimental process involved the reaction of 2-(4-Methylbenzamido)acetic acid(cas: 27115-50-0).Electric Literature of 27115-50-0

The Article related to benzoyl aminoacetic acid aryl iodide ortho arylation palladium catalyst, arylbenzoic amide acid preparation, Benzene, Its Derivatives, and Condensed Benzenoid Compounds: Carboxylic Acids and Peroxycarboxylic Acids and Their Sulfur-Containing Analogs and Salts and other aspects.Electric Literature of 27115-50-0

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