Day: October 11, 2022

Blizzard, Timothy A.; Chen, Helen; Kim, Seongkon; Wu, Jane; Bodner, Rena; Gude, Candido; Imbriglio, Jason; Young, Katherine; Park, Young-Whan; Ogawa, Aimie; Raghoobar, Susan; Hairston, Nichelle; Painter, Ronald E.; Wisniewski, Doug; Scapin, Giovanna; Fitzgerald, Paula; Sharma, Nandini; Lu, Jun; Ha, Sookhee; Hermes, Jeff; Hammond, Milton L. published an article on February 1 ,2014. The article was titled 《Discovery of MK-7655, a β-lactamase inhibitor for combination with Primaxin》, and you may find the article in Bioorganic & Medicinal Chemistry Letters.Recommanded Product: 1-Cbz-4-Methylaminopieridine The information in the text is summarized as follows:

β-Lactamase inhibitors with a bicyclic urea core and a variety of heterocyclic side chains were prepared and evaluated as potential partners for combination with imipenem to overcome class A and C β-lactamase mediated antibiotic resistance. The piperidine analog 3 (MK-7655) inhibited both class A and C β-lactamases in vitro. It effectively restored imipenem’s activity against imipenem-resistant Pseudomonas and Klebsiella strains at clin. achievable concentrations A combination of MK-7655 and Primaxin is currently in phase II clin. trials for the treatment of Gram-neg. bacterial infections. In the experiment, the researchers used many compounds, for example, 1-Cbz-4-Methylaminopieridine(cas: 405057-75-2Recommanded Product: 1-Cbz-4-Methylaminopieridine)

1-Cbz-4-Methylaminopieridine(cas: 405057-75-2) belongs to anime. Reduction of nitro compounds, RNO2, by hydrogen or other reducing agents produces primary amines cleanly (i.e., without a mixture of products), but the method is mostly used for aromatic amines because of the limited availability of aliphatic nitro compounds. Reduction of nitriles and oximes (R2C=NOH) also yields primary amines.Recommanded Product: 1-Cbz-4-Methylaminopieridine

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Ma, Wenjie; Wang, Na; Du, Yunchen; Tong, Tianze; Zhang, Leijiang; Andrew Lin, Kun-Yi; Han, Xijiang published an article on January 15 ,2019. The article was titled 《One-step synthesis of novel Fe3C@nitrogen-doped carbon nanotubes/graphene nanosheets for catalytic degradation of Bisphenol A in the presence of peroxymonosulfate》, and you may find the article in Chemical Engineering Journal (Amsterdam, Netherlands).Safety of Triacetonamine The information in the text is summarized as follows:

Developing novel carbocatalysts with available strategies for peroxymonosulfate (PMS) activation has become a popular topic in environmental remediation and protection fields. Herein, using com. K4Fe(CN)6 as the precursor, Fe3C@nitrogen-doped carbon nanotubes/graphene nanosheets (Fe3C@NCNTs/GNS) is synthesized by a direct high-temperature pyrolysis. Characterization results prove that Fe3C@NCNTs/GNS has a relatively high graphitization degree and rich nitrogen doping content, which endow it with excellent catalytic efficiency in PMS activation for powerful removal of Bisphenol A (BPA). Influences of catalyst/oxidant dosages, some inorganic anions, humic acid, and practical sewages are investigated in detail. For mechanism studies, it is found that tert-Bu alc. (TBA)/methanol fails to inhibit BPA degradation, and the primary reactive oxidative species (ROS) are superoxide radical (O·-2) and singlet oxygen (1O2). Discussion on the origin of 1O2 confirms that moderate modification of N atoms in graphitic carbon frameworks plays an essential role in inducing the non-radical mechanism. This work will provide new insights for the preparation of high-performance carbocatalysts in PMS activation and exploring critical roles of N-doping during non-radical processes. After reading the article, we found that the author used Triacetonamine(cas: 826-36-8Safety of Triacetonamine)

Triacetonamine(cas: 826-36-8) is a member of piperidine. Piperidine is ubiquitous structural motif widely occurred in diverse synthetically and naturally occurring bioactive molecules. Piperidines are an immensely important class of compounds medicinally: the piperidine ring is the most common heterocyclic subunit among FDA approved drugs.Safety of Triacetonamine

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

The author of 《Light-Mediated Formal Radical Deoxyfluorination of Tertiary Alcohols through Selective Single-Electron Oxidation with TEDA2+.》 were Aguilar Troyano, Francisco Jose; Ballaschk, Frederic; Jaschinski, Marcel; Oezkaya, Yasemin; Gomez-Suarez, Adrian. And the article was published in Chemistry – A European Journal in 2019. Quality Control of 4-(Pyridin-3-yl)piperidin-4-ol The author mentioned the following in the article:

The synthesis of tertiary alkyl fluorides through a formal radical deoxyfluorination process was described. This light-mediated, catalyst-free methodol. was fast and broadly applicable allowing for the preparation of C-F bonds from (hetero)benzylic, propargylic and non-activated tertiary alc. derivatives Preliminary mechanistic studies supported that the key step of the reaction is the single-electron oxidation of cesium oxalates-which are readily available from the corresponding tertiary alcs.-with in situ generated TEDA2+ (TEDA: N-(chloromethyl)triethylenediamine), a radical cation derived from Selectfluor. The experimental process involved the reaction of 4-(Pyridin-3-yl)piperidin-4-ol(cas: 50461-59-1Quality Control of 4-(Pyridin-3-yl)piperidin-4-ol)

4-(Pyridin-3-yl)piperidin-4-ol(cas: 50461-59-1) belongs to piperidines. Piperidine derivatives are also used in solid-phase peptide synthesis (SPPS) and many degradation reactions. Quality Control of 4-(Pyridin-3-yl)piperidin-4-ol

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Zuo, Shiyu; Guan, Zeyu; Zhang, Yiming; Yang, Fan; Li, Xiaohu; Li, Dongya published their research in Chemical Engineering Journal (Amsterdam, Netherlands) on December 15 ,2022. The article was titled 《Bidentate binuclear coordination configuration for peroxymonosulfate catalytic regulation through incorporation of CuFeOx to iron-based metal organic frameworks》.Synthetic Route of C9H17NO The article contains the following contents:

The scheme of coordination bridge modification provides a new vision for regulating the catalytic pathway, but how to change the surface coordination of peroxymonosulfate (PMS), thereby affecting the catalytic mechanism of PMS, is still an unknown field. In this, we found that MIL-101(Fe) is expected to control the surface catalytic pathway via the bidentate binuclear coordination configuration, thereby realizing the rapid oxidative detoxification of toxic organic pollutants and CO2 conversion. Introducing Cu on the surface of MIL-101(Fe) to change the surface chem. environment (MIL-101(Fe)/CuFeOx) can shift the catalytic pathway, thereby promoting a 14.5-fold improvement in Bisphenol A (BPA) oxidation kinetics (from 0.00697 min-1 to 0.101 min-1). Characterization, experiments, and d. functional theory (DFT) results show that Cu in the vicinity of Fe can tune the electronic structure and properties of Fe-O-Cu, thereby enhancing the electron transfer rate at the active center, facilitating electronic transitions and PMS adsorption. More importantly, shifting the binding configuration of PMS from monodentate mononuclear coordination on a single Fe center to bidentate binuclear coordination on Fe/Cu centers, shorter distance coordination structures and O-O pulling of PMS. The effect promoted PMS cleavage to generate more ROS and changed the catalytic pathway from the radical pathway to the 1O2 and high-valent metal species pathway. The free radical/non-radical pathway co-mediated by 1O2, high-valent metal species, ·OH and SO·-4 can effectively reduce the biotoxicity of toxic organic pollutants, and can utilize alkali environment captures CO2 as a stable carbonate for environmental use. This study provides a strategy for manipulating the catalytic pathway through coordination configuration and a feasible idea for CO2 conversion in wastewater treatment. The experimental part of the paper was very detailed, including the reaction process of Triacetonamine(cas: 826-36-8Synthetic Route of C9H17NO)

Triacetonamine(cas: 826-36-8) is a member of piperidine. Piperidine-containing compounds are also frequently employed in synthesis as ligands or auxiliaries. Accordingly, many efforts have been devoted to the development of novel methods for the synthesis of these compounds over the years.Synthetic Route of C9H17NO

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

In 2013,Sudhakar Babu, K.; Ravi Sankar, T.; Latha, J.; Ram Babu, B.; SwarnaKumari, M. published 《Synthesis and antibacterial activity of some novel 1-piperidin-4-yl-1,3-dihydro-2H-benzimidazol-2-one analogs》.Journal of Applicable Chemistry (Lumami, India) published the findings.HPLC of Formula: 622-26-4 The information in the text is summarized as follows:

Synthesis of some novel 1-piperidin-4-yl-1,3-dihydro-2H-benzimidazol-2-one derivatives were prepared from com. available 1,2-phenylenediamine. These compounds were tested for their antibacterial activity against gram pos. Streptococcus pyogenes and Staphylococcus aureus and against gram neg. Escherichia coli, Pseudomonas arsenous, Proteus vulgaris, Salmonella typhii bacterial cultures. The title compounds were highly active against Streptococcus pyogenes and Escherichia coli. In addition to this study using 2-(Piperidin-4-yl)ethanol, there are many other studies that have used 2-(Piperidin-4-yl)ethanol(cas: 622-26-4HPLC of Formula: 622-26-4) was used in this study.

2-(Piperidin-4-yl)ethanol(cas: 622-26-4) have been used as an intermediate in the synthetic preparation of cellular-active allosteric inhibitors of FAKHPLC of Formula: 622-26-4

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

In 2014,Sree Ram Babu, J.; Ravi Sankar, T.; Sudhakar Babu, K.; Latha, J. published 《Synthesis, characterization and biological evaluation of some novel disubstituted heterocyclic derivatives》.Journal of Chemical and Pharmaceutical Research published the findings.Recommanded Product: 2-(Piperidin-4-yl)ethanol The information in the text is summarized as follows:

Synthesis of disubstituted heterocyclic derivatives I [X = 3,4-(Cl)2; R = piperidin-1-yl, 4-hydroxypiperidin-1-yl, piperidin-4-ylmethanol, 2-(piperidin-4-yl)ethan-1-ol] were prepared from com. available 1,2-henylenediamine. The compounds I were tested for Gram pos.: Streptococcus pyogenes and Staphylococcus aureus. Gram neg.: Escherichia coli, Pseudomonas arzenous, Proteus vulgaris, Salmonella typhi bacterial cultures. The compounds I were found to be highly active against Streptococcus pyogenes and Escherichia coli.2-(Piperidin-4-yl)ethanol(cas: 622-26-4Recommanded Product: 2-(Piperidin-4-yl)ethanol) was used in this study.

2-(Piperidin-4-yl)ethanol(cas: 622-26-4) can be used to synthese ursolic acid derivatives, spiroimidazolidinone NPC1L1 inhibitors, neurokinin-2 receptor antagonists, antagonists for inhibition of platelet aggregation.Recommanded Product: 2-(Piperidin-4-yl)ethanol

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

In 2016,Babu, J. Sree Ram; Sankar, T. Ravi; Babu, K. Sudhakar; Latha, J. published 《Synthesis, characterization and biological evaluation of some novel disubstituted heterocyclic derivatives》.Journal of Chemical and Pharmaceutical Research published the findings.Recommanded Product: 2-(Piperidin-4-yl)ethanol The information in the text is summarized as follows:

Synthesis of some novel di-substituted 1-piperidin-4-yl(3,4-dibromphenyl)-1,3-dihydro-2H-benzimidazol-2-one derivatives (6A-6D) were prepared from com. available 1,2-henylenediamine. Compounds (6A-6D) were tested for Gram pos.: Streptococcus pyogenes and Staphylococcus aureus. Gram neg.: Escherichia coli, Pseudomonas arzenous, Proteus vulgaris, Salmonella typhi bacterial cultures. Compounds 6A-6D were found to be highly active against Streptococcus pyogenes and Escherichia coli. In the experiment, the researchers used many compounds, for example, 2-(Piperidin-4-yl)ethanol(cas: 622-26-4Recommanded Product: 2-(Piperidin-4-yl)ethanol)

2-(Piperidin-4-yl)ethanol(cas: 622-26-4) can be used to synthese ursolic acid derivatives, spiroimidazolidinone NPC1L1 inhibitors, neurokinin-2 receptor antagonists, antagonists for inhibition of platelet aggregation.Recommanded Product: 2-(Piperidin-4-yl)ethanol

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

In 2019,Chemical Communications (Cambridge, United Kingdom) included an article by Zhu, Ze-Fan; Tu, Jia-Lin; Liu, Feng. Recommanded Product: tert-Butyl 4-aminopiperidine-1-carboxylate. The article was titled 《Ni-Catalyzed deaminative hydroalkylation of internal alkynes》. The information in the text is summarized as follows:

A regioselective cis-hydroalkylation of internal alkynes with readily prepared Katritzky pyridinium salts for the synthesis of tri-substituted alkenes is described. This reaction is the first example of a metal-catalyzed hydroalkylation of an alkyne via C-N bond activation of an amine. The reaction demonstrates broad scope and functional group tolerance, allowing access to desired products with high diversity. Preliminary mechanistic studies indicate that a combination of an SET-initiated radical process and Ni-catalyzed alkylation could engage in the reaction, which makes it possible to bypass the traditional open-shell addition pathway.tert-Butyl 4-aminopiperidine-1-carboxylate(cas: 87120-72-7Recommanded Product: tert-Butyl 4-aminopiperidine-1-carboxylate) was used in this study.

tert-Butyl 4-aminopiperidine-1-carboxylate(cas: 87120-72-7) belongs to anime. Halogenation, in which one or more hydrogen atoms of an amine is replaced by a halogen atom, occurs with chlorine, bromine, and iodine, as well as with some other reagents, notably hypochlorous acid (HClO). With primary amines the reaction proceeds in two stages, producing N-chloro- and N,N-dichloro-amines, RNHCl and RNCl2, respectively. With tertiary amines, an alkyl group may be displaced by a halogen.Recommanded Product: tert-Butyl 4-aminopiperidine-1-carboxylate

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

In 2022,Tolentino, Kirsten T.; Mashinson, Viktoriya; Vadukoot, Anish K.; Hopkins, Corey R. published an article in Bioorganic & Medicinal Chemistry Letters. The title of the article was 《Discovery and characterization of benzyloxy piperidine based dopamine 4 receptor antagonists》.Application of 109384-19-2 The author mentioned the following in the article:

The dopamine receptor 4 (D4R) is highly expressed in both motor, associative and limbic subdivisions of the cortico-basal ganglia network. Due to the distribution in the brain, there is mounting evidence pointing to a role for the D4R in the modulation of this network and its subsequent involvement in L-DOPA induced dyskinesias in Parkinson′s disease. As part of our continued effort in the discovery of novel D4R antagonists, we report the discovery and characterization of a new 3- or 4-benzyloxypiperidine scaffold as D4R antagonists. We report several D4R selective compounds (>30-fold vs. other dopamine receptor subtypes) with improved in vitro and in vivo stability over previously reported D4R antagonists.tert-Butyl 4-hydroxypiperidine-1-carboxylate(cas: 109384-19-2Application of 109384-19-2) was used in this study.

tert-Butyl 4-hydroxypiperidine-1-carboxylate(cas:109384-19-2) is a 4-hydroxypyridine with a boc protecting group used in the preparation of neurologically active agents and other pharmaceutical compounds.Application of 109384-19-2

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Recommanded Product: tert-Butyl 4-aminopiperidine-1-carboxylateIn 2019 ,《Discovery of a potent histone deacetylase (HDAC) 3/6 selective dual inhibitor》 appeared in European Journal of Medicinal Chemistry. The author of the article were Soumyanarayanan, Uttara; Ramanujulu, Pondy Murugappan; Mustafa, Nurulhuda; Haider, Shozeb; Fang Nee, Adina Huey; Tong, Jie Xin; Tan, Kevin S. W.; Chng, Wee Joo; Dymock, Brian W.. The article conveys some information:

Herein, we report the discovery of a dual histone deacetylase inhibitor displaying a unique HDAC3/6 selectivity profile. An initial strategy to merge two epigenetic pharmacophores resulted in the discovery of potent HDAC6 inhibitors with selectivity over HDAC1. Screening in an HDAC panel revealed addnl. low nanomolar inhibition only against HDAC3. Low micromolar antiproliferative activities against two breast cancer and four hematol. cancer cell lines was supported by pharmacodynamic studies on a preferred mol., 24c, substantiating the HDAC inhibitory profile in cells. Apoptosis was identified as one of the main cell death pathways. Modeling studies of 24c against HDAC1,2,3 and 6 further provided insights on the orientation of specific residues relevant to compound potency, explaining the observed HDAC3/6 selectivity. A subset of the compounds also exhibited good antimalarial activities, particularly against the chloroquine-resistant strain K1 of P.falciparum. In vitro studies revealed a favorable DMPK profile warranting further investigation of the therapeutic potential of these compounds The results came from multiple reactions, including the reaction of tert-Butyl 4-aminopiperidine-1-carboxylate(cas: 87120-72-7Recommanded Product: tert-Butyl 4-aminopiperidine-1-carboxylate)

tert-Butyl 4-aminopiperidine-1-carboxylate(cas: 87120-72-7) belongs to anime. In organic chemistry, amines are compounds and functional groups that contain a basic nitrogen atom with a lone pair. Amines are formally derivatives of ammonia (NH3), wherein one or more hydrogen atoms have been replaced by a substituent such as an alkyl or aryl group (these may respectively be called alkylamines and arylamines; amines in which both types of substituent are attached to one nitrogen atom may be called alkylarylamines).Recommanded Product: tert-Butyl 4-aminopiperidine-1-carboxylate

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem