Category: piperidines

Wei, Peng’s team published research in Journal of Organic Chemistry in 70 | CAS: 4972-31-0

Journal of Organic Chemistry published new progress about 4972-31-0. 4972-31-0 belongs to piperidines, auxiliary class Piperidine,Benzene, name is 1-(Phenylsulfinyl)piperidine, and the molecular formula is C8H15NO, Product Details of C11H15NOS.

Wei, Peng published the artcileFactors Affecting Stereocontrol during Glycosidation of 2,3-Oxazolidinone-Protected 1-Tolylthio-N-acetyl-D-glucosamine, Product Details of C11H15NOS, the publication is Journal of Organic Chemistry (2005), 70(10), 4195-4198, database is CAplus and MEDLINE.

It is demonstrated that a ring-fused 2,3-oxazolidinone-protected derivative of 1-tolylthio-N-acetyl-D-glucosamine, e.g. β-I (R = SPhMe), undergoes high-yield stereoselective glycosidation under mild donor activation conditions to give the corresponding glycosides, e.g. I (R = OBn). Stereoselective formation of α-linked or β-linked glycosides is dependent on reactivity of acceptor alcs., where rate of glycosidation correlates to stereochem. outcome. Evidence for the role of glycosyl triflate intermediates and the N-acetyl substituent of the 2N,3O-oxazolidinone ring in stereochem. control is presented.

Journal of Organic Chemistry published new progress about 4972-31-0. 4972-31-0 belongs to piperidines, auxiliary class Piperidine,Benzene, name is 1-(Phenylsulfinyl)piperidine, and the molecular formula is C8H15NO, Product Details of C11H15NOS.

Referemce:
https://en.wikipedia.org/wiki/Piperidine,
Piperidine | C5H11N – PubChem

 

Yadav, Nisha’s team published research in Organic & Biomolecular Chemistry in 13 | CAS: 39546-32-2

Organic & Biomolecular Chemistry published new progress about 39546-32-2. 39546-32-2 belongs to piperidines, auxiliary class Piperidine,Amine,Amide, name is Piperidine-4-carboxamide, and the molecular formula is C10H14O2, Name: Piperidine-4-carboxamide.

Yadav, Nisha published the artcileTricyclic dihydrobenzoxazepine and tetracyclic indole derivatives can specifically target bacterial DNA ligases and can distinguish them from human DNA ligase I, Name: Piperidine-4-carboxamide, the publication is Organic & Biomolecular Chemistry (2015), 13(19), 5475-5487, database is CAplus and MEDLINE.

DNA ligases are critical components for DNA metabolism in all organisms. NAD+-dependent DNA ligases (LigA) found exclusively in bacteria and certain entomopoxviruses are drawing increasing attention as therapeutic targets as they differ in their cofactor requirement from ATP-dependent eukaryotic homologs. Due to the similarities in the cofactor binding sites of the two classes of DNA ligases, it is necessary to find determinants that can distinguish between them for the exploitation of LigA as an anti-bacterial target. In the present endeavor, we have synthesized and evaluated a series of tricyclic dihydrobenzoxazepine and tetracyclic indole derivatives, e.g. I [X = S, O, CH2; R = 1-piperidinyl,, 4-hydroxy-1-piperidinyl, 1-pyrrolidinyl, etc.], for their ability to distinguish between bacterial and human DNA ligases. The in vivo inhibition assays that employed LigA deficient E. coli GR501 and S. typhimurium LT2 bacterial strains, rescued by ATP-dependent T4 DNA ligase or Mycobacterium tuberculosis NAD+-dependent DNA ligase (Mtb LigA), resp., showed that the compounds can specifically inhibit bacterial LigA. The in vitro enzyme inhibition assays using purified MtbLigA, human DNA ligase I & T4 DNA ligase showed specific inhibition of MtbLigA at low micromolar range. Our results demonstrate that tricyclic dihydrobenzoxazepine and tetracyclic indole derivatives can distinguish between bacterial and human DNA ligases by ∼5-folds. In silico docking and enzyme inhibition assays identified that the compounds bind to the cofactor binding site and compete with the cofactor. Ethidium bromide displacement and gel-shift assays showed that the inhibitors do not exhibit any unwanted general interactions with the substrate DNA. These results set the stage for the detailed exploration of this compound class for development as antibacterials.

Organic & Biomolecular Chemistry published new progress about 39546-32-2. 39546-32-2 belongs to piperidines, auxiliary class Piperidine,Amine,Amide, name is Piperidine-4-carboxamide, and the molecular formula is C10H14O2, Name: Piperidine-4-carboxamide.

Referemce:
https://en.wikipedia.org/wiki/Piperidine,
Piperidine | C5H11N – PubChem

 

Egli, Jasmine et al. published their research in Organic Letters in 2020 | CAS: 86069-86-5

(S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5) belongs to piperidine derivatives.Piperidine is a key saturated heterocyclic scaffold found in several of the top-selling small molecule pharmaceuticals and natural alkaloids, with a diverse range of biological activities. 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.COA of Formula: C21H21NO4

Why Proline? Influence of Ring-Size on the Collagen Triple Helix was written by Egli, Jasmine;Schnitzer, Tobias;Dietschreit, Johannes C. B.;Ochsenfeld, Christian;Wennemers, Helma. And the article was included in Organic Letters in 2020.COA of Formula: C21H21NO4 The following contents are mentioned in the article:

The effect of four- and six-membered ring-size analogs (azetidine- and piperidine-2-carboxylic acid, H-Aze-OH and H-Pip-OH) of proline on the stability of the collagen triple helix was examined Computational and NMR spectroscopic studies with model compounds and thermal denaturation experiments with collagen peptides showed that the ring-size analogs destabilize the triple helix to a similar extent by either mismatching backbone dihedral angles ϕ and ψ (Pip) or by an unfavorable trans/cis amide bond ratio (Aze). This study involved multiple reactions and reactants, such as (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5COA of Formula: C21H21NO4).

(S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5) belongs to piperidine derivatives.Piperidine is a key saturated heterocyclic scaffold found in several of the top-selling small molecule pharmaceuticals and natural alkaloids, with a diverse range of biological activities. 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.COA of Formula: C21H21NO4

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

 

Bai, Guo-liang et al. published their research in Huaxue Shiji in 2012 | CAS: 86069-86-5

(S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5) belongs to piperidine derivatives.Piperidine is a key saturated heterocyclic scaffold found in several of the top-selling small molecule pharmaceuticals and natural alkaloids, with a diverse range of biological activities. Several piperidine alkaloids isolated from natural herbs, were found to exhibit antiproliferation and antimetastatic effects on various types of cancers both in vitro and in vivo for example Piperine, Evodiamine, Matrine, Berberine and Tetrandine.Recommanded Product: (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid

Design and synthesis of N’-phenylacylhydrazide safety-catch resin and its application in synthesis of p-nitroaniline chromogenic peptide substrates was written by Bai, Guo-liang;Yang, Xiao-xiao;Lin, Hao;Yang, Li-quan;Wang, De-xin. And the article was included in Huaxue Shiji in 2012.Recommanded Product: (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid The following contents are mentioned in the article:

N’-Phenylacylhydrazide safety-catch resin was synthesized by derivatizing com. available MBHA resin with N’-Boc-4-hydrazinobenzoic acid. N’-Protection form of 4-hydrazinobenzoic acid and initial amino functional resin type have been investigated to achieve higher derivation yield. Five serine protease peptidyl-pNA chromogenic substrates were synthesized with the safety-catch resin by Boc/Fmoc hybridized protocol with high yields and purity. Intermediates and product were characterized by HRMS and NMR. This study involved multiple reactions and reactants, such as (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5Recommanded Product: (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.Piperidine is a key saturated heterocyclic scaffold found in several of the top-selling small molecule pharmaceuticals and natural alkaloids, with a diverse range of biological activities. Several piperidine alkaloids isolated from natural herbs, were found to exhibit antiproliferation and antimetastatic effects on various types of cancers both in vitro and in vivo for example Piperine, Evodiamine, Matrine, Berberine and Tetrandine.Recommanded Product: (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

 

Bai, Guo-liang et al. published their research in Huaxue Shiji in 2012 | CAS: 86069-86-5

(S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5) belongs to piperidine derivatives. Piperidine is a metabolite of cadaverine, a polyamine found in the human intestine. Piperidine derivatives bearing a masked aldehyde function in the ε-position are easily transformed into quinolizidine compounds through intramolecular reductive amination.Category: piperidines

Design and synthesis of N’-phenylacylhydrazide safety-catch resin and its application in synthesis of p-nitroaniline chromogenic peptide substrates was written by Bai, Guo-liang;Yang, Xiao-xiao;Lin, Hao;Yang, Li-quan;Wang, De-xin. And the article was included in Huaxue Shiji in 2012.Category: piperidines The following contents are mentioned in the article:

N’-Phenylacylhydrazide safety-catch resin was synthesized by derivatizing com. available MBHA resin with N’-Boc-4-hydrazinobenzoic acid. N’-Protection form of 4-hydrazinobenzoic acid and initial amino functional resin type have been investigated to achieve higher derivation yield. Five serine protease peptidyl-pNA chromogenic substrates were synthesized with the safety-catch resin by Boc/Fmoc hybridized protocol with high yields and purity. Intermediates and product were characterized by HRMS and NMR. 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. Piperidine is a metabolite of cadaverine, a polyamine found in the human intestine. Piperidine derivatives bearing a masked aldehyde function in the ε-position are easily transformed into quinolizidine compounds through intramolecular reductive amination.Category: piperidines

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

 

Monteiro, Hugo J. et al. published their research in Journal of the Chemical Society, Chemical Communications in 1973 | CAS: 30727-21-0

Ethyl 2,3-dioxopiperidine-4-carboxylate (cas: 30727-21-0) 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. Several piperidine alkaloids isolated from natural herbs, were found to exhibit antiproliferation and antimetastatic effects on various types of cancers both in vitro and in vivo for example Piperine, Evodiamine, Matrine, Berberine and Tetrandine.Application In Synthesis of Ethyl 2,3-dioxopiperidine-4-carboxylate

New synthesis of the amino acid (+-)-cucurbitine was written by Monteiro, Hugo J.. And the article was included in Journal of the Chemical Society, Chemical Communications in 1973.Application In Synthesis of Ethyl 2,3-dioxopiperidine-4-carboxylate The following contents are mentioned in the article:

Bromination of Et 2,3-dioxo-4-piperidine carboxylate (I; X = H) gave 95% of the 4-bromo derivative (I; X = Br) which with NaN3 in refluxing MeO(CH2)2OMe gave 80% of the azido derivative (I; X = N3). I (X = Br, N3) in CHCl3 with AcOOH underwent ring contraction to 60-80% of the corresponding oxopyrrolidines (II; R = O). II (X = N3, R = O) with Et3O+BF4- gave the imino ether (III). Quant. B2H6 reduction of III gave 40% of the azidopyrrolidine (II; X = N3, R = H2), which underwent catalytic hydrogenation (PtO2) to give (±)-cucurbitine Et ester (II; X = NH2, R = H2) which on hydrolysis gave 70% (±)-cucurbitine. This study involved multiple reactions and reactants, such as Ethyl 2,3-dioxopiperidine-4-carboxylate (cas: 30727-21-0Application In Synthesis of Ethyl 2,3-dioxopiperidine-4-carboxylate).

Ethyl 2,3-dioxopiperidine-4-carboxylate (cas: 30727-21-0) 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. Several piperidine alkaloids isolated from natural herbs, were found to exhibit antiproliferation and antimetastatic effects on various types of cancers both in vitro and in vivo for example Piperine, Evodiamine, Matrine, Berberine and Tetrandine.Application In Synthesis of Ethyl 2,3-dioxopiperidine-4-carboxylate

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

 

Mansoor, Namia et al. published their research in World Journal of Pharmacy and Pharmaceutical Sciences in 2021 | CAS: 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. 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.Formula: C32H39NO4

Comparative analysis of montelukast, levocetirizine, cetirizine & fexofenadine was written by Mansoor, Namia;Nadig, Ramya;Munoth, Rohan;Reddy, Vasavi;Kamdi, Yadini. And the article was included in World Journal of Pharmacy and Pharmaceutical Sciences in 2021.Formula: C32H39NO4 The following contents are mentioned in the article:

This article is an examination of the Comparative Anal. of Fexofenadine, Levocetirizine, Cetirizine and Montelukast. The scientific development and subsequent continues to influence researchers all over the globe today. This article examines the research done and published by researchers and scientists. Consideration of current trends and data in scientific queries and demonstrates further aspects of Comparative Anal. of Fexofenadine, Levocetirizine, Cetirizine and Montelukast. Addnl., this article explores options for therapeutic functions of the antihistamines while diving into allergenic issues as well. 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: 83799-24-0Formula: C32H39NO4).

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.Formula: C32H39NO4

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

 

Koudih, Radouane et al. published their research in European Journal of Medicinal Chemistry in 2012 | CAS: 882033-93-4

(3S,4R)-rel-tert-Butyl 3-fluoro-4-(hydroxymethyl)piperidine-1-carboxylate (cas: 882033-93-4) belongs to piperidine derivatives.Piperidine is a key saturated heterocyclic scaffold found in several of the top-selling small molecule pharmaceuticals and natural alkaloids, with a diverse range of biological activities. 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.SDS of cas: 882033-93-4

Synthesis and in vitro characterization of trans- and cis-[18F]-4-methylbenzyl 4-[(pyrimidin-2-ylamino)methyl]-3-fluoropiperidine-1-carboxylates as new potential PET radiotracer candidates for the NR2B subtype N-methyl-D-aspartate receptor was written by Koudih, Radouane;Gilbert, Gwenaelle;Dhilly, Martine;Abbas, Ahmed;Barre, Louisa;Debruyne, Daniele;Sobrio, Franck. And the article was included in European Journal of Medicinal Chemistry in 2012.SDS of cas: 882033-93-4 The following contents are mentioned in the article:

Diastereoisomeric compounds [18F]cis- and [18F]trans-4-methylbenzyl 4-[(pyrimidin-2-ylamino)methyl]-3-fluoro-piperidine-1-carboxylates I were successfully synthesized as new subtype-selective PET radiotracers for imaging the NR2B subunit containing NMDA receptors. Rat brain section autoradiogs. demonstrated a high specific binding in NR2B/NMDA receptor rich regions for both radioligands. The measured logD7.4 values as well as Bmax/Kd ratios indicated that both radiotracers possess the adequate properties required for PET radiotracers. This study involved multiple reactions and reactants, such as (3S,4R)-rel-tert-Butyl 3-fluoro-4-(hydroxymethyl)piperidine-1-carboxylate (cas: 882033-93-4SDS of cas: 882033-93-4).

(3S,4R)-rel-tert-Butyl 3-fluoro-4-(hydroxymethyl)piperidine-1-carboxylate (cas: 882033-93-4) belongs to piperidine derivatives.Piperidine is a key saturated heterocyclic scaffold found in several of the top-selling small molecule pharmaceuticals and natural alkaloids, with a diverse range of biological activities. 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.SDS of cas: 882033-93-4

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

 

Sonoda, Junichiro et al. published their research in International Journal of Clinical Pharmacology and Therapeutics in 2021 | CAS: 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 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. Some chemotherapeutic agents have piperidine moiety within their structure, foremost among them, vinblastine and raloxifene.Formula: C32H39NO4

Impact of green tea intake on the pharmacokinetics of celiprolol in healthy subjects was written by Sonoda, Junichiro;Ogata, Kenji;Yoshikawa, Naoki;Sato, Keizo;Ikeda, Ryuji;Shimodozono, Yoshihiro. And the article was included in International Journal of Clinical Pharmacology and Therapeutics in 2021.Formula: C32H39NO4 The following contents are mentioned in the article:

To assess the effect of green tea intake on the pharmacokinetics of the β-blocker celiprolol. In an open-label crossover study, 3 healthy subjects were given water or a green tea beverage daily for 3 days. On day 4, each subject received a single oral dose of 200 mg celiprolol with water or green tea. Serum and urinary concentrations of celiprolol were measured for up to 24 h. Green tea intake decreased the area under the serum concentration-time curve and urinary excretion of celiprolol by 98.6 and 98.0%, resp. Green tea intake might have a neg. impact on the clin. effectiveness of celiprolol. 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: 83799-24-0Formula: C32H39NO4).

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 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. Some chemotherapeutic agents have piperidine moiety within their structure, foremost among them, vinblastine and raloxifene.Formula: C32H39NO4

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

 

Blizzard, Timothy A. et al. published their research in Bioorganic & Medicinal Chemistry Letters in 2014 | CAS: 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. 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.Computed Properties of C21H21NO4

Heterocyclic core analogs of a direct thrombin inhibitor was written by Blizzard, Timothy A.;Singh, Sanjay;Patil, Basanagoud;Chidurala, Naresh;Komanduri, Venukrishnan;Debnath, Samarpita;Belyakov, Sergei;Crespo, Alejandro;Struck, Alice;Kurtz, Marc;Wiltsie, Judyann;Shen, Xun;Sonatore, Lisa;Arocho, Marta;Lewis, Dale;Ogletree, Martin;Biftu, Tesfaye. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2014.Computed Properties of C21H21NO4 The following contents are mentioned in the article:

Thrombin is a serine protease that plays a key role in blood clotting. Pyrrolidine I•TFA is a potent thrombin inhibitor discovered at Merck several years ago. Seven analogs of I•TFA in which the pyrrolidine core was replaced with various heterocycles were prepared and evaluated for activity against thrombin, clotting factors VIIa, IXa, Xa, and XIIa, and trypsin. The thiomorpholine analog II•TFA was the most active, essentially matching the thrombin inhibitory activity of I•TFA with slightly improved selectivity over trypsin. This study involved multiple reactions and reactants, such as (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5Computed Properties of C21H21NO4).

(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. 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.Computed Properties of C21H21NO4

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem