Day: November 22, 2022

Development of an improved method to estimate the days of continuous drug ingestion, based on the micro-segmental hair analysis was written by Kuwayama, Kenji;Miyaguchi, Hajime;Kanamori, Tatsuyuki;Tsujikawa, Kenji;Yamamuro, Tadashi;Segawa, Hiroki;Okada, Yuki;Iwata, Yuko T.. And the article was included in Drug Testing and Analysis in 2021.Application In Synthesis of 2-(4-(1-Hydroxy-4-(4-(hydroxydiphenylmethyl)piperidin-1-yl)butyl)phenyl)-2-methylpropanoic acid The following contents are mentioned in the article:

To prove drug-related crimes, it is important to estimate the date on which a specific drug was ingested. Previously, we developed a method, “micro-segmental hair anal.”, to estimate the day of ingestion of a single-dose drug by segmenting a hair strand into 0.4-mm segments, which correspond to daily hair growth. In this study, the method was improved to estimate the days of continuous drug ingestion. The subjects ingested four hay-fever medicines (fexofenadine, epinastine, cetirizine, and loratadine) continuously (1-18 days) and chlorpheniramine as a single dose at intervals of several weeks as an internal temporal marker (ITM). The hair strands of the subjects were collected and subjected to a micro-segmental anal. The distribution curves of each hay-fever medicine in a hair strand had broad peaks reflecting the number of days of drug ingestion. The positions on the curves corresponding to the first and final ingestion days of hay-fever medicines were identified using the ITM. The positions were near the hair segments on both ends of full width at half maximum (W₂) of the broad peak. When the first and final days of continuous ingestion were estimated using W₂, independent of peak shape, the absolute average error from the actual ingestion days was approx. 2 days. Overall, we established a method to estimate the days of both single-dose and continuous drug ingestions. Furthermore, the method would be useful to investigate drug ingestion history in various scenes such as drug-related crimes and therapeutic drug monitoring. This study involved multiple reactions and reactants, such as 2-(4-(1-Hydroxy-4-(4-(hydroxydiphenylmethyl)piperidin-1-yl)butyl)phenyl)-2-methylpropanoic acid (cas: 83799-24-0Application In Synthesis of 2-(4-(1-Hydroxy-4-(4-(hydroxydiphenylmethyl)piperidin-1-yl)butyl)phenyl)-2-methylpropanoic acid).

2-(4-(1-Hydroxy-4-(4-(hydroxydiphenylmethyl)piperidin-1-yl)butyl)phenyl)-2-methylpropanoic acid (cas: 83799-24-0) belongs to piperidine derivatives. Piperidine and its derivatives have become increasingly popular in many synthetic schemes. Piperidine derivatives bearing a masked aldehyde function in the ε-position are easily transformed into quinolizidine compounds through intramolecular reductive amination.Application In Synthesis of 2-(4-(1-Hydroxy-4-(4-(hydroxydiphenylmethyl)piperidin-1-yl)butyl)phenyl)-2-methylpropanoic acid

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Continuous and automated slug flow nanoextraction for rapid partition coefficient measurement was written by Payne, Emory M.;Wells, Shane S.;Kennedy, Robert T.. And the article was included in Analyst (Cambridge, United Kingdom) in 2021.Name: 2-(4-(1-Hydroxy-4-(4-(hydroxydiphenylmethyl)piperidin-1-yl)butyl)phenyl)-2-methylpropanoic acid The following contents are mentioned in the article:

Octanol-water partition coefficients (log K_ow) are widely used in pharmaceutical and environmental chem. to assess the lipophilicity of compounds Traditionally log K_ow is determined using a shake-flask method that uses milliliters of sample and solvent and requires hours for preparation, extraction, and anal. Here, an automated system is reported for rapid log K_ow determination for an array of compounds using slug flow nanoextn. (SFNE) enabled by a microfluidic chip. In the method, an autosampler is used to introduce 1μL of sample into a microfluidic device that segments the injected volume into a series of 4 nL slugs that are each paired to an adjacent octanol slug. Each octanol-water phase pair is compartmentalized by an immiscible fluorous carrier fluid. During flow, rapid extraction occurs at each octanol-water interface. The resulting linear array of slugs flows into an online UV absorbance detector that is used to determine concentrations in the phases, allowing the log K_ow to be measured. The microfluidic device allows toggling between two-phase “aqueous plug” generation (aqueous sample separated by fluorous carrier fluid) and three-phase “phase pair” generation. In this way, online calibration for detection in the aqueous phase can be achieved. The method is applied to determining log K_ow for a panel of seven pharmaceutical compounds, including complete calibration curves, at three different pHs in under 2 h using 5μL of extraction standard and 2.9μL of octanol per extraction standard analyzed. This study involved multiple reactions and reactants, such as 2-(4-(1-Hydroxy-4-(4-(hydroxydiphenylmethyl)piperidin-1-yl)butyl)phenyl)-2-methylpropanoic acid (cas: 83799-24-0Name: 2-(4-(1-Hydroxy-4-(4-(hydroxydiphenylmethyl)piperidin-1-yl)butyl)phenyl)-2-methylpropanoic acid).

2-(4-(1-Hydroxy-4-(4-(hydroxydiphenylmethyl)piperidin-1-yl)butyl)phenyl)-2-methylpropanoic acid (cas: 83799-24-0) belongs to piperidine derivatives. Piperidine is a metabolite of cadaverine, a polyamine found in the human intestine. The piperidine and polyhydroxylated indolizidine derivatives have shown to be promising α-glucosidase inhibitors. The former are analogs of DNJ with an improved α-glucosidase inhibitory profile than that of DNJ. Boisson et al.Name: 2-(4-(1-Hydroxy-4-(4-(hydroxydiphenylmethyl)piperidin-1-yl)butyl)phenyl)-2-methylpropanoic acid

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Pharmacological Inhibition of Soluble Epoxide Hydrolase Ameliorates Chronic Ethanol-Induced Cardiac Fibrosis by Restoring Autophagic Flux was written by Zhou, Chi;Huang, Jin;Li, Qing;Zhan, Chenao;He, Ying;Liu, Jinyan;Wen, Zheng;Wang, Dao Wen. And the article was included in Alcoholism: Clinical & Experimental Research in 2018.Safety of 1-(1-Propionylpiperidin-4-yl)-3-(4-(trifluoromethoxy)phenyl)urea The following contents are mentioned in the article:

Background : Chronic drinking leads to myocardial contractile dysfunction and dilated cardiomyopathy, and cardiac fibrosis is a consequence of these alc. injuries. Soluble epoxide hydrolase (sEH) hydrolyzes epoxyeicosatrienoic acids (EETs) to less bioactive diols, and EETs have cardioprotective properties. However, the effects of sEH inhibition in ethanol (EtOH)-induced cardiac fibrosis are unknown. Methods : This study was designed to investigate the role and underlying mechanisms of sEH inhibition in chronic EtOH feeding-induced cardiac fibrosis. C57BL/6J mice were fed a 4% Lieber-DeCarli EtOH diet for 8 wk, and the sEH inhibitor 1-trifluoromethoxyphenyl-3-(1-propionylpiperidin-4-yl) urea (TPPU) was administered throughout the exptl. period. Results : The results showed that chronic EtOH intake led to cardiac dilatation, collagen deposition, and autophagosome accumulation, while TPPU administration ameliorated these effects. In vitro, treating primary cardiac fibroblasts (CFs) with EtOH resulted in CF activation, including alpha smooth muscle actin overexpression, collagen synthesis, and cell migration. Moreover, EtOH disturbed CF autophagic flux, as evidenced by the increased LC3 II/I ratio and SQSTM1 expression, and by the enhanced autophagosome accumulation. TPPU treatment prevented the activation of CF induced by EtOH and restored the impaired autophagic flux by suppressing mTOR activation. Conclusions : Taken together, these findings suggest that sEH pharmacol. inhibition may be a unique therapeutic strategy for treating EtOH-induced cardiac fibrosis. This study involved multiple reactions and reactants, such as 1-(1-Propionylpiperidin-4-yl)-3-(4-(trifluoromethoxy)phenyl)urea (cas: 1222780-33-7Safety of 1-(1-Propionylpiperidin-4-yl)-3-(4-(trifluoromethoxy)phenyl)urea).

1-(1-Propionylpiperidin-4-yl)-3-(4-(trifluoromethoxy)phenyl)urea (cas: 1222780-33-7) belongs to piperidine derivatives. Piperidine has a role as a reagent, a protic solvent, a base, a catalyst, a plant metabolite, a human metabolite and a non-polar solvent. Some chemotherapeutic agents have piperidine moiety within their structure, foremost among them, vinblastine and raloxifene.Safety of 1-(1-Propionylpiperidin-4-yl)-3-(4-(trifluoromethoxy)phenyl)urea

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

The Effect of Oxidative Stress on the Transport of the P-Glycoprotein Substrate through the Cell Monolayer was written by Shchulkin, A. V.;Abalenikhina, Yu. V.;Seidkulieva, A. A.;Chernykh, I. V.;Yakusheva, E. N.. And the article was included in Biochemistry (Moscow), Supplement Series A in 2021.Recommanded Product: 83799-24-0 The following contents are mentioned in the article:

P-glycoprotein (Pgp) is an ATP-dependent transmembrane protein involved in the efflux of lipophilic substances. The aim of this study was to evaluate the effect of oxidative stress on the transport of a Pgp substrate through the monolayer of Caco-2 cells overexpressing this transport protein. Oxidative stress was modeled by incubating the cells with H2O2. Exposure to H2O2 at concentrations of 10 and 50 μM for 3 h reduced the Pgp activity but not the content of Pgp, while the integrity of the cell monolayer did not change. The increase of the prooxidant concentration to 100 μM reduced the content of Pgp, violated the integrity of the cell monolayer, and increased the transcellular and paracellular transport of fexofenadine. A 24-h exposure to 0.1-1 μM H2O2 resulted in an increase in the content of Pgp mediated by the Nrf2 transcription factor, while the activity of the transport protein remained unchanged. At a prooxidant concentration of 10 μM, the Pgp activity decreased and the cell membrane permeability increased, while at concentrations of 50-100 μM, the content (100 μM) and activity of Pgp decreased, and the paracellular and transcellular permeability of the cell monolayer increased for fexofenadine, a substrate of the transport protein. Thus, H2O2 increased the transport of the Pgp substrate fexofenadine through the cell monolayer by inhibiting the activity of the transport protein, reducing its content, as well as violating the integrity of the cell membrane and intercellular contacts. The cells can adapt to these effects by increasing the content of Pgp. This study involved multiple reactions and reactants, such as 2-(4-(1-Hydroxy-4-(4-(hydroxydiphenylmethyl)piperidin-1-yl)butyl)phenyl)-2-methylpropanoic acid (cas: 83799-24-0Recommanded Product: 83799-24-0).

2-(4-(1-Hydroxy-4-(4-(hydroxydiphenylmethyl)piperidin-1-yl)butyl)phenyl)-2-methylpropanoic acid (cas: 83799-24-0) belongs to piperidine derivatives. The piperidine structural motif is present in numerous natural alkaloids. These include piperine, which gives black pepper its spicy taste. Industrially, piperidine is produced by the hydrogenation of pyridine, usually over a molybdenum disulfide catalyst. Pyridine can also be reduced to piperidine via a modified Birch reduction using sodium in ethanol.Recommanded Product: 83799-24-0

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Desorption of pharmaceuticals and illicit drugs from different stabilized sludge types across pH was written by Grabic, Roman;Ivanova, Lucia;Kodesova, Radka;Grabicova, Katerina;Vojs Stanova, Andrea;Imreova, Zuzana;Drtil, Miloslav;Bodik, Igor. And the article was included in Water Research in 2022.Recommanded Product: 83799-24-0 The following contents are mentioned in the article:

Pharmaceutical and illicit drug residues in sewage sludge may present important risks following direct application to agricultural soils, potentially resulting in uptake by plants. Leaching/desorption tests were performed on different types of stabilized sewage sludge originating from multiple treatment technologies in the Slovak Republic. Acid rain and base-rich condition of soil with different pH conditions were simulated to model the effect of widely varying pH (pH 2, 4, 7, 9, and 12) on the leaching/desorption of pharmaceuticals and illicit drugs. Twenty-nine of 93 target analytes were found above the limit of quantification in sludge or associated leachates. Total desorbed amounts of pharmaceuticals and illicit drugs ranged from 810 to 4000μg/kg, and 110 to 3600μg/kg of the dry mass of anaerobic and aerobic sludge, resp. Desorbed fractions were calculated as these values are normalized to initial sludge concentration and, therefore, were more suitable for qual. description of the behavior of individual compounds Using principal component anal., qual. anal. of the desorbed fraction confirmed the differences among sludge types, pharmaceuticals, and desorption pH. Desorbed fractions could not be related to the octanol/water distribution coefficient Desorbed fractions also did not reflect the expected ionization of studied mols. unless converted into their relative values. Generally, the lowest mobility was observed within the environmentally relevant pH range of 4-9, and high pH generally resulted in high desorption, especially in anaerobically stabilized sludges. This study involved multiple reactions and reactants, such as 2-(4-(1-Hydroxy-4-(4-(hydroxydiphenylmethyl)piperidin-1-yl)butyl)phenyl)-2-methylpropanoic acid (cas: 83799-24-0Recommanded Product: 83799-24-0).

2-(4-(1-Hydroxy-4-(4-(hydroxydiphenylmethyl)piperidin-1-yl)butyl)phenyl)-2-methylpropanoic acid (cas: 83799-24-0) belongs to piperidine derivatives. The piperidine moiety constitutes an important building block for the synthesis of a variety of bioactive natural products, alkaloids and other drugs. Some chemotherapeutic agents have piperidine moiety within their structure, foremost among them, vinblastine and raloxifene.Recommanded Product: 83799-24-0

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Synthesis and evaluation of aza-peptidyl inhibitors of the lysosomal asparaginyl endopeptidase, legumain was written by Lee, Jiyoun;Bogyo, Matthew. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2012.Safety of (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid The following contents are mentioned in the article:

Legumain or asparaginyl endopeptidase (AEP) is a lysosomal cysteine protease with a high level of specificity for cleavage of protein substrates after an asparagine residue. It is also capable of cleaving after aspartic acids sites when in the acidic environment of the lysosome. Legumain expression and activity is linked to a number of pathol. conditions including cancer, atherosclerosis and inflammation, yet its biol. role in these pathologies is not well-understood. Highly potent and selective inhibitors of legumain would not only be valuable for studying the functional roles of legumain in these conditions, but may have therapeutic potential as well. The authors describe here the design, synthesis and in vitro evaluation of selective legumain inhibitors based on the aza-asparaginyl scaffold. The authors synthesized a library of aza-peptidyl inhibitors with various non-natural amino acids and different electrophilic warheads, and characterized the kinetic properties of inactivation of legumain. The authors also synthesized fluorescently labeled inhibitors to investigate cell permeability and selectivity of the compounds The inhibitors have second order rate constants of up to 5 × 10⁴ M^-1 s^-1 and IC₅₀ values as low as 4 nM against recombinant mouse legumain. In addition, the inhibitors are highly selective toward legumain and have little or no cross-reactivity with cathepsins. Overall, the authors have identified several valuable new inhibitors of legumain that can be used to study legumain function in multiple disease models. This study involved multiple reactions and reactants, such as (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5Safety of (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid).

(S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5) belongs to piperidine derivatives. The piperidine moiety constitutes an important building block for the synthesis of a variety of bioactive natural products, alkaloids and other drugs. Industrially, piperidine is produced by the hydrogenation of pyridine, usually over a molybdenum disulfide catalyst. Pyridine can also be reduced to piperidine via a modified Birch reduction using sodium in ethanol.Safety of (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Synthesis and evaluation of aza-peptidyl inhibitors of the lysosomal asparaginyl endopeptidase, legumain was written by Lee, Jiyoun;Bogyo, Matthew. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2012.Synthetic Route of C21H21NO4 The following contents are mentioned in the article:

Legumain or asparaginyl endopeptidase (AEP) is a lysosomal cysteine protease with a high level of specificity for cleavage of protein substrates after an asparagine residue. It is also capable of cleaving after aspartic acids sites when in the acidic environment of the lysosome. Legumain expression and activity is linked to a number of pathol. conditions including cancer, atherosclerosis and inflammation, yet its biol. role in these pathologies is not well-understood. Highly potent and selective inhibitors of legumain would not only be valuable for studying the functional roles of legumain in these conditions, but may have therapeutic potential as well. The authors describe here the design, synthesis and in vitro evaluation of selective legumain inhibitors based on the aza-asparaginyl scaffold. The authors synthesized a library of aza-peptidyl inhibitors with various non-natural amino acids and different electrophilic warheads, and characterized the kinetic properties of inactivation of legumain. The authors also synthesized fluorescently labeled inhibitors to investigate cell permeability and selectivity of the compounds The inhibitors have second order rate constants of up to 5 × 10⁴ M^-1 s^-1 and IC₅₀ values as low as 4 nM against recombinant mouse legumain. In addition, the inhibitors are highly selective toward legumain and have little or no cross-reactivity with cathepsins. Overall, the authors have identified several valuable new inhibitors of legumain that can be used to study legumain function in multiple disease models. This study involved multiple reactions and reactants, such as (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5Synthetic Route of C21H21NO4).

(S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5) belongs to piperidine derivatives. Piperidine is a saturated organic heteromonocyclic parent, an azacycloalkane, a secondary amine and a member of piperidines. Fluorinated piperidines are also the subject of continued interest in medicinal chemistry, for example in the synthesis of selective dipeptidyl peptidase II (DPP II) inhibitors. Piperidine derivatives are also used in solid-phase peptide synthesis (SPPS) and many degradation reactions.Synthetic Route of C21H21NO4

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Chromatographic enantiomer separation using 9-amino-9-(deoxy)-epiquinine-derived chiral selectors: control of chiral recognition via introduction of additional stereogenic centers was written by Maier, Norbert M.;Greco, Elisa;Petrovaj, Jan;Lindner, Wolfgang. And the article was included in Acta Chimica Slovenica in 2012.Category: piperidines The following contents are mentioned in the article:

Three new cinchona-type chiral selectors were prepared by attaching N-pivaloyl-glycine, N-pivaloyl-(S)-valine and N-pivaloyl-(R)-valine segments to the C9-amino function of 9-amino-9-(deoxy)-epiquinine (eAQN), and immobilized to silica to provide the corresponding chiral stationary phases (CSPs). Evaluation of the chromatog. enantioseparation characteristics of these CSPs with a broad assortment of N-carbamoyl protected amino acids under polar organic mobile phase conditions revealed modest chiral recognition capabilities for N-Fmoc-, N-Cbz- and N-Boc-derivatives The enantioselective analyte binding to these CSPs is strictly controlled by the absolute stereochem. of the amino acid functionalities attached to the C9-amino group of the eAQN framework. Specifically, the CSP derived from (S)-valine-based selector exhibits preferential binding of N-carbamoyl-(S)-amino acids, while the CSPs featuring (R)-valine- and the glycine-derived selectors show opposite enantioselective binding preference. The observed impact of analyte structure on enantioselectivity and the specific preferences in enantioselective binding point to chiral recognition mechanisms capitalizing on intermol. ion pairing, hydrogen bonding and subtle steric interactions, with the latter making the crucial contributions to stereodiscrimination. The finding that the chiral recognition characteristics of epiquinine can be readily controlled via incorporation of addnl. stereogenic centers remote from the cinchona scaffold might be useful information for the design of new enantioselective receptors and organocatalysts. This study involved multiple reactions and reactants, such as (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5Category: piperidines).

(S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5) belongs to piperidine derivatives. The piperidine structural motif is present in numerous natural alkaloids. These include piperine, which gives black pepper its spicy taste. Piperidine prefers a chair conformation, similar to cyclohexane. Unlike cyclohexane, piperidine has two distinguishable chair conformations: one with the N–H bond in an axial position, and the other in an equatorial position.Category: piperidines

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Chromatographic enantiomer separation using 9-amino-9-(deoxy)-epiquinine-derived chiral selectors: control of chiral recognition via introduction of additional stereogenic centers was written by Maier, Norbert M.;Greco, Elisa;Petrovaj, Jan;Lindner, Wolfgang. And the article was included in Acta Chimica Slovenica in 2012.Application of 86069-86-5 The following contents are mentioned in the article:

Three new cinchona-type chiral selectors were prepared by attaching N-pivaloyl-glycine, N-pivaloyl-(S)-valine and N-pivaloyl-(R)-valine segments to the C9-amino function of 9-amino-9-(deoxy)-epiquinine (eAQN), and immobilized to silica to provide the corresponding chiral stationary phases (CSPs). Evaluation of the chromatog. enantioseparation characteristics of these CSPs with a broad assortment of N-carbamoyl protected amino acids under polar organic mobile phase conditions revealed modest chiral recognition capabilities for N-Fmoc-, N-Cbz- and N-Boc-derivatives The enantioselective analyte binding to these CSPs is strictly controlled by the absolute stereochem. of the amino acid functionalities attached to the C9-amino group of the eAQN framework. Specifically, the CSP derived from (S)-valine-based selector exhibits preferential binding of N-carbamoyl-(S)-amino acids, while the CSPs featuring (R)-valine- and the glycine-derived selectors show opposite enantioselective binding preference. The observed impact of analyte structure on enantioselectivity and the specific preferences in enantioselective binding point to chiral recognition mechanisms capitalizing on intermol. ion pairing, hydrogen bonding and subtle steric interactions, with the latter making the crucial contributions to stereodiscrimination. The finding that the chiral recognition characteristics of epiquinine can be readily controlled via incorporation of addnl. stereogenic centers remote from the cinchona scaffold might be useful information for the design of new enantioselective receptors and organocatalysts. This study involved multiple reactions and reactants, such as (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5Application of 86069-86-5).

(S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5) belongs to piperidine derivatives. The piperidine ring can be found not only in more than half of the currently known structures of alkaloids, but also in many natural or synthetic compounds with interesting biological activities. The piperidine and polyhydroxylated indolizidine derivatives have shown to be promising α-glucosidase inhibitors. The former are analogs of DNJ with an improved α-glucosidase inhibitory profile than that of DNJ. Boisson et al.Application of 86069-86-5

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Radiolabelling of 1,4-disubstituted 3-[¹⁸F]fluoropiperidines and its application to new radiotracers for NR2B NMDA receptor visualization was written by Koudih, Radouane;Gilbert, Gwenaelle;Dhilly, Martine;Abbas, Ahmed;Barre, Louisa;Debruyne, Daniele;Sobrio, Franck. And the article was included in Organic & Biomolecular Chemistry in 2012.Safety of (3S,4R)-rel-tert-Butyl 3-fluoro-4-(hydroxymethyl)piperidine-1-carboxylate The following contents are mentioned in the article:

In order to develop a novel and useful building block for the development of radiotracers for positron emission tomog. (PET), we studied the radiolabelling of 1,4-disubstituted 3-[¹⁸F]fluoropiperidines. Indeed, 3-fluoropiperidine became a useful building block in medicinal chem. for the pharmacomodulation of piperidine-containing compounds The radiofluorination was studied on substituted piperidines with electron-donating and electron-withdrawing N-substituents. In the instance of electron-donating N-substituents such as benzyl or Bu, configuration retention and satisfactory fluoride-18 incorporation yields up to 80% were observed In the case of electron-withdrawing N-substituents leading to carbamate or amide functions, the incorporation yields depend on the 4-susbtitutent (2 to 63%). The radiolabelling of this building block was applied to the automated radiosynthesis of NR2B NMDA receptor antagonists and effected by a com. available radiochem. module. The in vivo evaluation of three radiotracers demonstrated minimal brain uptakes incompatible with the imaging of NR2B NMDA receptors in the living brain. Nevertheless, moderate radiometabolism was observed and, in particular, no radiodefluorination was observed which demonstrates the stability of the 3-position of the fluorine-18 atom. In conclusion, the 1,4-disubstituted 3-[¹⁸F]fluoropiperidine moiety could be of value in the development of other radiotracers for PET even if the evaluation of the NR2B NMDA receptor antagonists failed to demonstrate satisfactory properties for PET imaging of this receptor. This study involved multiple reactions and reactants, such as (3S,4R)-rel-tert-Butyl 3-fluoro-4-(hydroxymethyl)piperidine-1-carboxylate (cas: 882033-93-4Safety of (3S,4R)-rel-tert-Butyl 3-fluoro-4-(hydroxymethyl)piperidine-1-carboxylate).

(3S,4R)-rel-tert-Butyl 3-fluoro-4-(hydroxymethyl)piperidine-1-carboxylate (cas: 882033-93-4) belongs to piperidine derivatives. The piperidine moiety constitutes an important building block for the synthesis of a variety of bioactive natural products, alkaloids and other drugs. The piperidine and polyhydroxylated indolizidine derivatives have shown to be promising α-glucosidase inhibitors. The former are analogs of DNJ with an improved α-glucosidase inhibitory profile than that of DNJ. Boisson et al.Safety of (3S,4R)-rel-tert-Butyl 3-fluoro-4-(hydroxymethyl)piperidine-1-carboxylate

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem