Month: October 2022

Gharpure, Santosh J.; Hande, Pankaj E.; Pandey, Surya K.; Samala, Ganesh published their research in Journal of Organic Chemistry in 2021. The article was titled 《TMSOTf-mediated formal [4 + 2] cycloaddition-retro-aza-Michael cascade of vinylogous carbamates for the synthesis of highly fluorescent pyridocarbazoles》.Recommanded Product: 3,6-Dibromo-9H-carbazole The article contains the following contents:

Trimethylsilyl trifluoromethanesulfonate (TMSOTf) mediated dimerization reaction of vinylogous carbamates of carbazoles gave highly fluorescent pyridocarbazoles through Povarov-type formal [4 + 2] cycloaddition-retro-aza-Michael cascade. The developed strategy was used to access indolo pyridocarbazole and quinolizinocarbazolone in an expeditious manner. Various coupling reactions were successfully performed on synthesized pyridocarbazoles to study the effect of electronics of substitution on photophys. properties. Synthesized carbazoles possess excellent photophys. properties with high quantum yields (ΦF). Fluorescent carbazole dicarboxylic acid showed potential as pH probe giving linear response to pH over a very wide range (7.0-3.0) reflecting high efficiency. In the experiment, the researchers used many compounds, for example, 3,6-Dibromo-9H-carbazole(cas: 6825-20-3Recommanded Product: 3,6-Dibromo-9H-carbazole)

3,6-Dibromo-9H-carbazole(cas: 6825-20-3) is used as a pharmaceutical intermediate, and also an important intermediate of synthesizing optoelectronic materials. It has been used as a reagent in the synthesis of P7C3-A20 which is a potent neuroprotective agent.Recommanded Product: 3,6-Dibromo-9H-carbazole

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Liu, Qi; Wang, Leqi; Hu, Xinping; Zhou, Chuhang; Tang, Yingwei; Ma, Yining; Wang, Xiaoxiao; Liu, Yan published their research in Journal of Chinese Pharmaceutical Sciences in 2021. The article was titled 《Fabrication of deoxycholic acid-modified polymeric micelles and their transmembrane transport》.Related Products of 539-74-2 The article contains the following contents:

Oral administration is the best way for the most patients due to the good compliance, and intestinal epithelium is the main barrier of oral drug absorption. In order to overcome the small intestine epithelial barrier to orally deliver water-insoluble drugs, deoxycholic acid (DA), a substrate of the intestinal bile acid transporters, conjugated poly (2-ethyl-2-oxazoline)-poly (D, L-lactide) (DA-PEOz-PLA) was designed and synthesized, and deoxycholic acid-modified polymeric micelles composed of DA-PEOz-PLA and mPEG-PLA were fabricated to encapsulate model drug coumarin 6 (C6) based on intestinal bile acid pathway. The structure of DA-PEOz-PLA was confirmed using 1H NMR and TLC, and the mol. weight measured by GPC was 10034 g/mol with a PDI of 1.51. The C6-loaded polymeric micelles with drug loading content of 0.085% were characterized to have 40.11 nm in diameter and uniform spherical morphol. observed by TEM. Furthermore, the deoxycholic acid-modified polymeric micelles were demonstrated to further enhance the transmembrane transport efficiency. The mechanic study evidenced that anchorage of deoxycholic acid onto the micelles surface enriched their transcellular transport pathway. Therefore, the designed deoxycholic acid-modified polymeric micelles might have a promising potential for oral delivery of water-insoluble drugs. The results came from multiple reactions, including the reaction of Ethyl 3-bromopropanoate(cas: 539-74-2Related Products of 539-74-2)

Ethyl 3-bromopropanoate(cas: 539-74-2) belongs to organobromine compounds.Most of the natural organobromine compounds are produced by marine organisms , and several brominated metabolites with antibacterial , antitumor , antiviral , and antifungal activity have been isolated from seaweed, sponges, corals, molluscs, and others. Related Products of 539-74-2

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Hou, Chao-Ping; Chen, Xin-Lun; Huang, Zhi-Jian; Lei, Yang; Xiao, Li-Min; Huang, Jian-Feng; Li, Shao-Yong; Liu, Jun-Min published an article in 2021. The article was titled 《Robust Heterogeneous Photocatalyst for Visible-Light-Driven Hydrogen Evolution Promotion: Immobilization of a Fluorescein Dye-Encapsulated Metal-Organic Cage on TiO2》, and you may find the article in ACS Applied Materials & Interfaces.SDS of cas: 6825-20-3 The information in the text is summarized as follows:

The design of artificial photocatalytic devices that simulates the ingenious and efficient photosynthetic systems in nature is promising. Herein, a metal-organic cage [Pd6(NPyCzPF)12]12+ (MOC-PC6) integrating 12 organic ligands NPyCzBP and 6 Pd2+ catalytic centers is designed, which is well defined to include organic dye fluorescein (FL) for constructing a supramol. photochem. mol. device (SPMD) FL@MOC-PC6. Photoinduced electron transfer (PET) between MOC-PC6 and the encapsulated FL has been observed by steady-state and time-resolved emission spectroscopy. FL@MOC-PC6 is successfully heterogenized with TiO2 by a facile sol-gel method to achieve a robust heterogeneous FL@MOC-PC6-TiO2. The close proximity between the Pd2+ catalytic site and FL included in the cage enables PET from the photoexcited FL to Pd2+ sites through a powerful intramol. pathway. The photocatalytic hydrogen production assessments of the optimized 4 wt % FL@MOC-PC6-TiO2 demonstrate an initial H2 production rate of 2402 μmol g-1 h-1 and a turnover number of 4356 within 40 h, enhanced by 15-fold over that of a homogeneous FL@MOC-PC6. The effect of the MOC content on photocatalytic H2 evolution (PHE) is investigated and the inefficient comparison systems, such as MOC-PC6, MOC-PC6-TiO2, FL-sensitized MOC-PC6/FL-TiO2, and analog FL/MOC-PC6-TiO2 with free FL, are evaluated. This study provides a creative and distinctive approach for the design and preparation of novel heterogeneous SPMD catalysts based on MOCs. In the experiment, the researchers used many compounds, for example, 3,6-Dibromo-9H-carbazole(cas: 6825-20-3SDS of cas: 6825-20-3)

3,6-Dibromo-9H-carbazole(cas: 6825-20-3) is used as a pharmaceutical intermediate, and also an important intermediate of synthesizing optoelectronic materials. It has been used as a reagent in the synthesis of P7C3-A20 which is a potent neuroprotective agent.SDS of cas: 6825-20-3

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Jankowska, Agnieszka; Satala, Grzegorz; Latacz, Gniewomir; Partyka, Anna; Lubelska, Annamaria; Pociecha, Krzysztof; Swierczek, Artur; Wilczynska, Natalia; Mordyl, Barbara; Bojarski, Andrzej J.; Wyska, Elzbieta; Chlon-Rzepa, Grazyna published an article in 2021. The article was titled 《Design and Synthesis of Novel Aminoalkanamides Targeting Neurodegeneration and Symptoms of Alzheimer′s Disease》, and you may find the article in Current Medicinal Chemistry.Safety of Ethyl 5-bromovalerate The information in the text is summarized as follows:

There is currently no drug that slows the process of neurodegeneration or alleviates the cognitive and depressive symptoms in patients with Alzheimer′s disease. Due to the increasing number of Alzheimer′s patients, there is an urgent need to develop novel drugs with neuroprotective, procognitive, and antidepressant properties. The aim of this study was to design, synthesize, and evaluate novel aminoalkanamides with serotonin 5-HT1A/5-HT7 receptor affinity and phosphodiesterase (PDE) inhibitory activity as a new approach to combat neurodegeneration and symptoms of Alzheimer′s disease. The newly designed compounds were synthesized using classical methods of organic chem. and tested in vitro for their receptor affinity, functional profile, enzyme inhibition, and ADME properties. The neuroprotective effect against H2O2-induced increase of reactive oxygen species level was tested in SH-SY5Y cells. The novel object recognition and forced swimming tests were used to evaluate the procognitive and antidepressant activity, resp. Synthesized aminoalkanamides were characterized as potent 5-HT1A receptor antagonists with addnl. 5-HT7 receptor antagonistic properties and PDE4B inhibitory activity. Selected compound 15 showed neuroprotective, procognitive, and antidepressant properties. In addition, compound 15 revealed suitable ADME properties expressed as good membrane permeability and high metabolic stability. This study revealed a new class of compounds that may be useful in the search for an effective drug in the alleviation of neurodegeneration and symptoms of Alzheimer′s disease. The results came from multiple reactions, including the reaction of Ethyl 5-bromovalerate(cas: 14660-52-7Safety of Ethyl 5-bromovalerate)

Ethyl 5-bromovalerate(cas: 14660-52-7) belongs to bromides. A variety of minor organobromine compounds are found in nature, but none are biosynthesized or required by mammals. Organobromine compounds have fallen under increased scrutiny for their environmental impact.Safety of Ethyl 5-bromovalerate

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Tan, Fei; Pu, Maoping; He, Jun; Li, Jinzhao; Yang, Jian; Dong, Shunxi; Liu, Xiaohua; Wu, Yun-Dong; Feng, Xiaoming published an article in 2021. The article was titled 《Catalytic Asymmetric Homologation of Ketones with α-Alkyl α-Diazo Esters》, and you may find the article in Journal of the American Chemical Society.Application of 3395-91-3 The information in the text is summarized as follows:

The homologation of ketones with diazo compounds was a useful strategy to synthesize one-carbon chain-extended acyclic such as PhC(O)CMeCO2MeR [R = allyl, Bn, CH2(2-naphthyl), etc.] or ring-expanded cyclic ketones e.g., I. However, the asym. homologation of acyclic ketones with α-diazo esters remains a challenge due to the lower reactivity and complicated selectivity. Herein, the enantioselective catalytic homologation of acetophenone and related derivatives with α-alkyl α-diazo esters was reported utilizing a chiral scandium(III) N,N’-dioxide as the Lewis acid catalyst. This reaction supplies a highly chemo-, regio-, and enantioselective pathway for the synthesis of optically active β-keto esters with an all-carbon quaternary center through highly selective alkyl-group migration of the ketones. Moreover, the ring expansion of cyclic ketones was accomplished under slightly modified conditions, affording a series of enantioenriched cyclic β-keto esters. D. functional theory calculations was carried out to elucidate the reaction pathway and possible working models that could explain the observed regio- and enantioselectivity. The experimental process involved the reaction of Methyl 3-bromopropanoate(cas: 3395-91-3Application of 3395-91-3)

Methyl 3-bromopropanoate(cas: 3395-91-3) belongs to bromides. A variety of minor organobromine compounds are found in nature, but none are biosynthesized or required by mammals. Organobromine compounds have fallen under increased scrutiny for their environmental impact.Application of 3395-91-3

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Grob, Nathalie M.; Schibli, Roger; Behe, Martin; Valverde, Ibai E.; Mindt, Thomas L. published an article in 2021. The article was titled 《1,5-Disubstituted 1,2,3-Triazoles as Amide Bond Isosteres Yield Novel Tumor-Targeting Minigastrin Analogs》, and you may find the article in ACS Medicinal Chemistry Letters.Application In Synthesis of Benzyl 2-bromoacetate The information in the text is summarized as follows:

1,5-Disubstituted 1,2,3-triazoles (1,5-Tz) are considered bioisosteres of cis-amide bonds. However, their use for enhancing the pharmacol. properties of peptides or proteins is not yet well established. Aiming to illustrate their utility, we chose the peptide conjugate [Nle15]MG11 (DOTA-DGlu-Ala-Tyr-Gly-Trp-Nle-Asp-Phe-NH2) as a model compound since it is known that the cholecystokinin-2 receptor (CCK2R) is able to accommodate turn conformations. Analogs of [Nle15]MG11 incorporating 1,5-Tz in the backbone were synthesized and radiolabeled with lutetium-177, and their pharmacol. properties (cell internalization, receptor binding affinity and specificity, plasma stability, and biodistribution) were evaluated and compared with [Nle15]MG11 as well as their previously reported analogs bearing 1,4-disubstituted 1,2,3-triazoles. Our investigations led to the discovery of novel triazole-modified analogs of [Nle15]MG11 with nanomolar CCK2R-binding affinity and 2-fold increased tumor uptake. This study illustrates that substitution of amides by 1,5-disubstituted 1,2,3-triazoles is an effective strategy to enhance the pharmacol. properties of biol. active peptides. In the part of experimental materials, we found many familiar compounds, such as Benzyl 2-bromoacetate(cas: 5437-45-6Application In Synthesis of Benzyl 2-bromoacetate)

Benzyl 2-bromoacetate(cas: 5437-45-6) belongs to benzyl acetate. Benzyl acetate is an aromatic chemical, usually appearing as a clear liquid with a moderate sweet-jasmine fragrance. This compound appears as a component of some of our fragrance blends.Application In Synthesis of Benzyl 2-bromoacetate

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Zhang, Hai-Lin; Yu, Ya-Ting; Wang, Yi; Tang, Qi; Yang, Shi-Ping; Liu, Jin-Gang published an article in 2021. The article was titled 《Visible light-controlled carbon monoxide delivery combined with the inhibitory activity of histone deacetylases from a manganese complex for an enhanced antitumor therapy》, and you may find the article in Journal of Inorganic Biochemistry.Synthetic Route of C5BrMnO5 The information in the text is summarized as follows:

Multifunctional drugs with synergistic effects have been widely developed to enhance the treatment efficiency of various diseases, such as malignant tumors. Herein, a novel bifunctional manganese(I)-based prodrug [MnBr(CO)3(APIPB)] (APIPB = N-(2-aminophen-yl)-4-(1H-imidazo[4,5-f] [1, 10] phenanthrolin-2-yl)benzamide) with inhibitory histone deacetylase (HDAC) activity and light-controlled carbon monoxide (CO) delivery was successfully designed and synthesized. [MnBr(CO)3(APIPB)] readily released CO under visible light irradiation (λ > 400 nm) through which the amount of released CO could be controlled by manipulating light power d. and illumination time. In the absence of light irradiation, the cytotoxic effect of [MnBr(CO)3(APIPB)] on cancer cells was greater than that of the com. available HDAC inhibitor MS-275. Consequently, with a combination of CO delivery and HDAC inhibitory activity, [MnBr(CO)3(APIPB)] showed a remarkably enhanced antitumor effect on HeLa cells (IC50 = 3.2μM) under visible light irradiation Therefore, this approach shows potential for the development of medicinal metal complexes for combined antitumor therapies. In the experimental materials used by the author, we found Bromopentacarbonylmanganese(I)(cas: 14516-54-2Synthetic Route of C5BrMnO5)

Bromopentacarbonylmanganese(I)(cas: 14516-54-2) has many other uses. It is used in the formation of (eta6-arene)tricarbonylmanganese(I) by reacting with arene (arene= hexamethyl benzene, 1,2,4,5-tetramethyl benzene, mesitylene, p-xylene and toluene) in the presence silver salt.Synthetic Route of C5BrMnO5

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Liu, Yan; Chen, Xiao-Lan; Li, Xiao-Yun; Zhu, Shan-Shan; Li, Shi-Jun; Song, Yan; Qu, Ling-Bo; Yu, Bing published an article in 2021. The article was titled 《4CzIPN-tBu-Catalyzed Proton-Coupled Electron Transfer for Photosynthesis of Phosphorylated N-Heteroaromatics》, and you may find the article in Journal of the American Chemical Society.Quality Control of 3,6-Dibromo-9H-carbazole The information in the text is summarized as follows:

2,4,5,6-Tetrakis(3,6-di-tert-butyl-9H-carbazol-9-yl)isophthalonitrile (4CzIPN-tBu) was developed as a photocatalyst for the phosphorus-radical-initiated cascade cyclization reaction of isocyanides. By using 4CzIPN-tBu as catalyst, we developed a visible-light-induced proton-coupled electron transfer strategy for the generation of phosphorus-centered radicals, via which a wide range of phosphorylated phenanthridines, quinolines, and benzothiazoles were successfully constructed. The experimental process involved the reaction of 3,6-Dibromo-9H-carbazole(cas: 6825-20-3Quality Control of 3,6-Dibromo-9H-carbazole)

3,6-Dibromo-9H-carbazole(cas: 6825-20-3) is used as a pharmaceutical intermediate, and also an important intermediate of synthesizing optoelectronic materials. It has been used as a reagent in the synthesis of P7C3-A20 which is a potent neuroprotective agent.Quality Control of 3,6-Dibromo-9H-carbazole

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

In 2022,Schwickert, Marvin; Fischer, Tim R.; Zimmermann, Robert A.; Hoba, Sabrina N.; Meidner, J. Laurenz; Weber, Marlies; Weber, Moritz; Stark, Martin M.; Koch, Jonas; Jung, Nathalie; Kersten, Christian; Windbergs, Maike; Lyko, Frank; Helm, Mark; Schirmeister, Tanja published an article in Journal of Medicinal Chemistry. The title of the article was 《Discovery of Inhibitors of DNA Methyltransferase 2, an Epitranscriptomic Modulator and Potential Target for Cancer Treatment》.COA of Formula: C4H7BrO2 The author mentioned the following in the article:

Selective manipulation of the epitranscriptome could be beneficial for the treatment of cancer and also broaden the understanding of epigenetic inheritance. Inhibitors of the tRNA methyltransferase DNMT2, the enzyme catalyzing the S-adenosylmethionine-dependent methylation of cytidine 38 to 5-methylcytidine, were designed, synthesized, and analyzed for their enzyme-binding and -inhibiting properties. For rapid screening of potential DNMT2 binders, a microscale thermophoresis assay was established. Besides the natural inhibitors S-adenosyl-L-homocysteine (SAH) and sinefungin (SFG), we identified new synthetic inhibitors based on the structure of N-adenosyl-2,4-diaminobutyric acid (Dab). Structure-activity relationship studies revealed the amino acid side chain and a Y-shaped substitution pattern at the 4-position of Dab as crucial for DNMT2 inhibition. The most potent inhibitors are alkyne-substituted derivatives, exhibiting similar binding and inhibitory potencies as the natural compounds SAH and SFG. CaCo-2 assays revealed that poor membrane permeabilities of the acids and rapid hydrolysis of an ethylester prodrug might be the reasons for the insufficient activity in cellulo. The experimental process involved the reaction of 4-Bromobutanoic acid(cas: 2623-87-2COA of Formula: C4H7BrO2)

4-Bromobutanoic acid(cas: 2623-87-2) belongs to carboxylic acids. The chief chemical characteristic of the carboxylic acids is their acidity. They are generally more acidic than other organic compounds containing hydroxyl groups but are generally weaker than the familiar mineral acids (e.g., hydrochloric acid, HCl, sulfuric acid, H2SO4, etc.).COA of Formula: C4H7BrO2

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

In 2022,Andrews, David M.; Cartic, Sharon; Cosulich, Sabina; Divecha, Nullin; Faulder, Paul; Flemington, Vikki; Kern, Oliver; Kettle, Jason G.; MacDonald, Ellen; McKelvie, Jennifer; Pike, Kurt G.; Roberts, Bryan; Rowlinson, Rachel; Smith, James M.; Stockley, Martin; Swarbrick, Martin E.; Treinies, Iris; Waring, Michael J. published an article in Bioorganic & Medicinal Chemistry. The title of the article was 《Identification and optimization of a novel series of selective PIP5K inhibitors》.Safety of 3,5-Dibromoaniline The author mentioned the following in the article:

Phosphatidyl inositol (4,5)-bisphosphate (PI(4,5)P2) plays several key roles in human biol. and the lipid kinase that produces PI(4,5)P2, PIP5K, has been hypothesized to provide a potential therapeutic target of interest in the treatment of cancers. To better understand and explore the role of PIP5K in human cancers there remains an urgent need for potent and specific PIP5K inhibitor mols. Following a high throughput screen of the AstraZeneca collection, a novel, moderately potent and selective inhibitor of PIP5K, 1, was discovered. Detailed exploration of the SAR for this novel scaffold resulted in the considerable optimization of both potency for PIP5K, and selectivity over the closely related kinase PI3Kα, as well as identifying several opportunities for the continued optimization of drug-like properties. As a result, several high quality in vitro tool compounds were identified (8, 20 and 25) that demonstrate the desired biochem. and cellular profiles required to aid better understanding of this complex area of biol.3,5-Dibromoaniline(cas: 626-40-4Safety of 3,5-Dibromoaniline) was used in this study.

3,5-Dibromoaniline(cas: 626-40-4) belongs to anime. Amine, any member of a family of nitrogen-containing organic compounds that is derived, either in principle or in practice, from ammonia (NH3). Naturally occurring amines include the alkaloids, which are present in certain plants; the catecholamine neurotransmitters (i.e., dopamine, epinephrine, and norepinephrine); and a local chemical mediator, histamine, that occurs in most animal tissues.Safety of 3,5-Dibromoaniline

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary