Month: November 2022

Sisto, Francesca; Carradori, Simone; Guglielmi, Paolo; Traversi, Carmen Beatrice; Spano, Mattia; Sobolev, Anatoly P.; Secci, Daniela; Di Marcantonio, Maria Carmela; Haloci, Entela; Grande, Rossella; Mincione, Gabriella published an article in 2020, the title of the article was Synthesis and biological evaluation of carvacrol-based derivatives as dual inhibitors of H. pylori strains and AGS cell proliferation.Quality Control of 4-(Bromomethyl)-1,1′-biphenyl And the article contains the following content:

This study reports on the synthesis, structural assessment, microbiol. screening against several strains of H. pylori and antiproliferative activity against human gastric adenocarcinoma (AGS) cells of a large series of carvacrol-based compounds Structural analyses consisted of elemental anal., 1H/13C/19F NMR spectra and crystallog. studies. The structure-activity relationships evidenced that among ether derivatives the substitution with specific electron-withdrawing groups (CF3 and NO2) especially in the para position of the benzyl ring led to an improvement of the antimicrobial activity, whereas electron-donating groups on the benzyl ring and ethereal alkyl chains were not tolerated with respect to the parent compound (MIC/MBC = 64/64 μg/mL). Ester derivatives (coumarin-carvacrol hybrids) displayed a slight enhancement of the inhibitory activity up to MIC values of 8-16 μg/mL. The most interesting compounds exhibiting the lowest MIC/MBC activity against H. pylori (among others, compounds 16 and 39 endowed with MIC/MBC values ranging between 2/2 to 32/32 μg/mL against all the evaluated strains) were also assayed for their ability to reduce AGS cell growth with respect to 5-Fluorouracil. Some derivatives can be regarded as new lead compounds able to reduce H. pylori growth and to counteract the proliferation of AGS cells, both contributing to the occurrence of gastric cancer. The experimental process involved the reaction of 4-(Bromomethyl)-1,1′-biphenyl(cas: 2567-29-5).Quality Control of 4-(Bromomethyl)-1,1′-biphenyl

The Article related to helicobacter gastric adenocarcinoma cell proliferation, ags cells, helicobacter pylori, carvacrol, coumarin, drug resistance, dual agent, semi-synthesis, Placeholder for records without volume info and other aspects.Quality Control of 4-(Bromomethyl)-1,1′-biphenyl

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Wang, Sheng; Zhang, Fuwu; Yu, Guocan; Wang, Zhantong; Jacobson, Orit; Ma, Ying; Tian, Rui; Deng, Hongzhang; Yang, Weijing; Chen, Zhi-Yi; Chen, Xiaoyuan published an article in 2020, the title of the article was Zwitterionic-to-cationic charge conversion polyprodrug nanomedicine for enhanced drug delivery.Product Details of 574-98-1 And the article contains the following content:

Zwitterionic surface modification is a promising strategy for nanomedicines to achieve prolonged circulation time and thus effective tumor accumulation. However, zwitterion modified nanoparticles suffer from reduced cellular internalization efficiency. A polyprodrug-based nanomedicine with zwitterionic-to-cationic charge conversion ability (denoted as ZTC-NMs) was developed for enhanced chemotherapeutic drug delivery. The polyprodrug consists of pH-responsive poly(carboxybetaine)-like zwitterionic segment and glutathione-responsive camptothecin prodrug segment. The ZTC-NMs combine the advantages of zwitterionic surface and polyprodrug. Compared with conventional zwitterionic surface, the ZTC-NMs can respond to tumor microenvironment and realize ZTC surface charge conversion, thus improve cellular internalization efficiency of the nanomedicines. This ZTC method offers a strategy to promote the drug delivery efficiency and therapeutic efficacy, which is promising for the development of cancer nanomedicines. The experimental process involved the reaction of 2-(2-Bromoethyl)isoindoline-1,3-dione(cas: 574-98-1).Product Details of 574-98-1

The Article related to polyprodrug nanomedicine zwitterionic cationic charge conversion drug delivery, charge conversion, nanomedicine, polyprodrug, triggered drug release, zwitterionic, Placeholder for records without volume info and other aspects.Product Details of 574-98-1

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On October 21, 2021, Xiong, Yuan; Donovan, Katherine A.; Eleuteri, Nicholas A.; Kirmani, Nadia; Yue, Hong; Razov, Anthony; Krupnick, Noah M.; Nowak, Radoslaw P.; Fischer, Eric S. published an article.Recommanded Product: 2-(2-Bromoethyl)isoindoline-1,3-dione The title of the article was Chemo-proteomics exploration of HDAC degradability by small molecule degraders. And the article contained the following:

Targeted protein degradation refers to the use of small mols. that recruit a ubiquitin ligase to a target protein for ubiquitination and subsequent proteasome-dependent degradation While degraders have been developed for many targets, key questions regarding degrader development and the consequences of acute pharmacol. degradation remain, specifically for targets that exist in obligate multi-protein complexes. Here, we synthesize a pan-histone deacetylase (HDAC) degrader library for the chemo-proteomic exploration of acute degradation of a key class of chromatin-modifying enzymes. Using chemo-proteomics, we not only map the degradability of the zinc-dependent HDAC family identifying leads for targeting HDACs 1-8 and 10 but also explore important aspects of degrading epigenetic enzymes. We discover cell line-driven target specificity and that HDAC degradation often results in collateral loss of HDAC-containing repressive complexes. These findings potentially offer a new mechanism toward controlling chromatin structure, and our resource will facilitate accelerated degrader design and development for HDACs. The experimental process involved the reaction of 2-(2-Bromoethyl)isoindoline-1,3-dione(cas: 574-98-1).Recommanded Product: 2-(2-Bromoethyl)isoindoline-1,3-dione

The Article related to hdac degradability small mol degrader chemoproteomics exploration, e3 ligase, hdac, imid, protac, collateral degradation, degrader, targeted degradation, ubiquitin, Placeholder for records without volume info and other aspects.Recommanded Product: 2-(2-Bromoethyl)isoindoline-1,3-dione

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On July 23, 2020, Watterson, Scott Hunter; O’Malley, Daniel; Gavai, Ashvinikumar V.; Gong, Hua; Tarby, Christine M. published a patent.Electric Literature of 1196157-51-3 The title of the patent was Heterocyclic NLRP3 modulators, for use in the treatment of cancer. And the patent contained the following:

The present invention provides compounds of Formula (I), wherein all of the variables are as defined herein. These compounds are modulators of NLRP3, which may be used as medicaments for the treatment of proliferative disorders, such as cancer in a subject (e.g., a human). The experimental process involved the reaction of 2-Amino-6-bromonicotinic acid(cas: 1196157-51-3).Electric Literature of 1196157-51-3

The Article related to heterocyclic nlrp3 modulator cancer, Pharmaceuticals: Formulation and Compounding and other aspects.Electric Literature of 1196157-51-3

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On June 30, 2019, Kawano, Teruhiro; Watari, Ryo; Kayaki, Yoshihito; Ikariya, Takao published an article.Name: 2-(2-Bromoethyl)isoindoline-1,3-dione The title of the article was Catalytic Hydrogenation of Carboxamides with a Bifunctional Cp*Ru Catalyst Bearing an Imidazol-2-ylidene with a Protic Aminoethyl Side Chain. And the article contained the following:

Synthesis of a Cp*Ru complex bearing an NH2-functionalized N-heterocyclic carbene (C-NH) I (R = CH3) was achieved by treatment of Cp*RuBr(isoprene) with an equimolar amount of a silver complex, which was generated from Ag2O and 1-(2-aminoethyl)-3-methylimidazolium bromide, in CH3CN at room temperature The new Cp*RuBr(C-NH) complex I showed a higher catalytic performance than the related Cp*RuCl(P-NH) and Cp*RuCl(N-NH) complexes. In the reaction of N-arylcarboxamides R1C(O)NR2R3 (R1 = H, C6H5, pyridin-3-yl; R2 = R3 = CH3; R2 = H, R3 = C6H5; R2R3 = -C(O)(CH2)3-, etc.), the amine products R2R3NH were obtained in satisfactory yields under mild temperature conditions. The experimental process involved the reaction of 2-(2-Bromoethyl)isoindoline-1,3-dione(cas: 574-98-1).Name: 2-(2-Bromoethyl)isoindoline-1,3-dione

The Article related to amine preparation, carboxamide hydrogenation ruthenium catalyst, General Organic Chemistry: Synthetic Methods and other aspects.Name: 2-(2-Bromoethyl)isoindoline-1,3-dione

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Torres, Gerardo M.; Liu, Yi; Arndtsen, Bruce A. published an article in 2020, the title of the article was A dual light-driven palladium catalyst: Breaking the barriers in carbonylation reactions.Application of 574-98-1 And the article contains the following content:

Transition metal-catalyzed coupling reactions have become one of the most important tools in modern synthesis. However, an inherent limitation to these reactions is the need to balance operations, because the factors that favor bond cleavage via oxidative addition ultimately inhibit bond formation via reductive elimination. Here, we describe an alternative strategy that exploits simple visible-light excitation of palladium to drive both oxidative addition and reductive elimination with low barriers. Palladium-catalyzed carbonylations can thereby proceed under ambient conditions, with challenging aryl or alkyl halides and difficult nucleophiles, and generate valuable carbonyl derivatives such as acid chlorides, esters, amides, or ketones in a now-versatile fashion. Mechanistic studies suggest that concurrent excitation of palladium(0) and palladium(II) intermediates is responsible for this activity. The experimental process involved the reaction of 2-(2-Bromoethyl)isoindoline-1,3-dione(cas: 574-98-1).Application of 574-98-1

The Article related to palladium catalyst carbonylation alkyl halide aryl carbon monoxide, General Organic Chemistry: Synthetic Methods and other aspects.Application of 574-98-1

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On August 1, 2022, Djukanovic, Dimitrije; Ganiek, Maximilian A.; Nishi, Kohei; Karaghiosoff, Konstantin; Mashima, Kazushi; Knochel, Paul published an article.Electric Literature of 2567-29-5 The title of the article was Preparation of Functionalized Amides Using Dicarbamoylzincs. And the article contained the following:

Authors report a new convenient preparation of dicarbamoylzincs of type (R1R2NCO)2Zn by the treatment of ZnCl2 and formamides R1R2NCHO with LiTMP in THF (15°C, 15 min) or by the reaction of formamides R1R2NCHO with TMP2Zn (25°C, 16 h). This second method tolerates sensitive groups such as an ester, ketone or nitro function. Reaction of these dicarbamoylzincs with allylic, benzylic, aryl, alkenyl bromides, acid chlorides, aldehydes or enones provided various polyfunctional amides in 47-97% yields. The experimental process involved the reaction of 4-(Bromomethyl)-1,1′-biphenyl(cas: 2567-29-5).Electric Literature of 2567-29-5

The Article related to amide preparation dicarbamoylzinc, amides, carbamoyl, lithium, metalation, zinc, General Organic Chemistry: Synthetic Methods and other aspects.Electric Literature of 2567-29-5

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On October 13, 2021, Zimmermann, Birte M.; Ngoc, Trung Tran; Tzaras, Dimitrios-Ioannis; Kaicharla, Trinadh; Teichert, Johannes F. published an article.Category: bromides-buliding-blocks The title of the article was A Bifunctional Copper Catalyst Enables Ester Reduction with H2: Expanding the Reactivity Space of Nucleophilic Copper Hydrides. And the article contained the following:

Employing a bifunctional catalyst based on a copper(I)/NHC complex and a guanidine organocatalyst, catalytic ester reductions to alcs. with H2 as terminal reducing agent are facilitated. The approach taken here enables the simultaneous activation of esters through hydrogen bonding and formation of nucleophilic copper(I) hydrides from H2, resulting in a catalytic hydride transfer to esters. The reduction step is further facilitated by a proton shuttle mediated by the guanidinium subunit. This bifunctional approach to ester reductions for the first time shifts the reactivity of generally considered “soft” copper(I) hydrides to previously unreactive “hard” ester electrophiles and paves the way for a replacement of stoichiometric reducing agents by a catalyst and H2. The experimental process involved the reaction of 2-(2-Bromoethyl)isoindoline-1,3-dione(cas: 574-98-1).Category: bromides-buliding-blocks

The Article related to bifunctional azaheterocyclic carbene copper catalyst guanidine ester reduction alc, General Organic Chemistry: Synthetic Methods and other aspects.Category: bromides-buliding-blocks

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On June 18, 2021, Luedtke, Matthew W.; Pisano, Joseph; Paquin, Lucas; Walker, Joel; Madalengoitia, Jose S. published an article.Computed Properties of 574-98-1 The title of the article was Broadening the Scope of the Zwitterionic 1,3-Diaza-Claisen Rearrangement through a Tethering Strategy. And the article contained the following:

Expansion of the scope of the 1,3-diaza-Claisen rearrangement beyond bridged-bicyclic tertiary allylic amines has been investigated through a tethering strategy. Isothioureas tethered to tertiary allylic amines are converted to carbodiimides through a reaction with AgOTf/Et3N. Intramol. cyclization of the tertiary allylic amine to the carbodiimide equilibrates with a zwitterionic intermediate. Heating the carbodiimide/zwitterion affords a rearrangement product. Heating carbodiimide/zwitterion with a deuterated allyl group results in the scrambling of the deuterium label, which is consistent with an ionic mechanism involving heterolytic cleavage of the allylic C-N bond, followed by trapping of the allyl cation at either terminal carbon. The ionic mechanism is attributed to silver salt contamination since pushing deuterium-labeled carbodiimide/zwitterion through silica gel prior to heating results in clean deuterium transposition consistent with a sigmatropic mechanism, and adding back silver salts results in deuterium scrambling. Overall, the tethering strategy broadens the scope of the rearrangement to simpler allylic substrates. D. functional theory (DFT) calculations of the sigmatropic rearrangement are in agreement with reactivity trends observed with reactions run under silver-free conditions. The experimental process involved the reaction of 2-(2-Bromoethyl)isoindoline-1,3-dione(cas: 574-98-1).Computed Properties of 574-98-1

The Article related to zwitterionic diaza claisen rearrangement sothiourea tethered tertiary allylic amine, General Organic Chemistry: Synthetic Methods and other aspects.Computed Properties of 574-98-1

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

On June 1, 2022, Liu, Yi; Zhou, Cuihan; Jiang, Meijing; Arndtsen, Bruce A. published an article.Synthetic Route of 574-98-1 The title of the article was Versatile Palladium-Catalyzed Approach to Acyl Fluorides and Carbonylations by Combining Visible Light- and Ligand-Driven Operations. And the article contained the following:

The development of a general palladium-catalyzed carbonylative method to synthesize acyl fluorides RC(O)F (R = n-Bu, cyclohexyl, 4-methylphenyl, pyridin-3-yl, etc.) from aryl, heteroaryl, alkyl, and functionalized organic halides RX was described. Mechanistic anal. suggests that the reaction proceeds via the unique, synergistic combination of visible light photoexcitation of Pd(0) to induce oxidative addition with a ligand-favored reductive elimination. These together create a unidirectional catalytic cycle that is uninhibited by the classical effect of carbon monoxide coordination. Coupling the catalytic formation of acyl fluorides with their subsequent nucleophilic reactions has opened a method to perform carbonylation reactions with unprecedented breadth, including the assembly of highly functionalized carbonyl-containing products. The experimental process involved the reaction of 2-(2-Bromoethyl)isoindoline-1,3-dione(cas: 574-98-1).Synthetic Route of 574-98-1

The Article related to acyl fluoride preparation, acyl halide carbon monoxide photochem carbonylation palladium catalyst, General Organic Chemistry: Synthetic Methods and other aspects.Synthetic Route of 574-98-1

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary