Day: January 6, 2023

Catalytic Oxygenative Allylic Transposition of Alkenes into Enones with an Azaadamantane-Type Oxoammonium Salt Catalyst was written by Nagasawa, Shota;Sasano, Yusuke;Iwabuchi, Yoshiharu. And the article was included in Chemistry – A European Journal in 2017.Category: piperidines This article mentions the following:

The first catalytic oxygenative allylic transposition of unactivated alkenes, e.g., Me₂C:CH₂(CH₂)₃OCOPh, into enones, e.g., H₂C:C(Me)CO(CH₂)₃OCOPh, has been developed using an oxoammonium salt, azaadamantane I, as the catalyst. This reaction converts various tri- and trans-disubstituted alkenes into their corresponding enones with transposition of their double bonds at ambient temperature in good yields. The use of a less-hindered azaadamantane-type oxoammonium salt as the catalyst and a combination of two distinct stoichiometric oxidants, namely, iodobenzene diacetate and magnesium monoperoxyphthalate hexahydrate (MMPP·6H₂O) are essential to facilitate the enone formation efficiently. In the experiment, the researchers used many compounds, for example, 1-Tosylpiperidin-4-one (cas: 33439-27-9Category: piperidines).

1-Tosylpiperidin-4-one (cas: 33439-27-9) 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 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

Rapid Synthesis of Polycyclic Aromatic Compounds by Iodocyclization of Ynamides was written by Okitsu, Takashi;Itoh, Maho;Inui, Ayaka;Muta, Emiko;Nakamoto, Ryota;Adachi, Yuta;Wada, Akimori;Hatano, Manabu. And the article was included in Asian Journal of Organic Chemistry in 2022.Application In Synthesis of 1-Tosylpiperidin-4-one This article mentions the following:

The iodocyclization of ene-ynamides, e.g., N-((2-(Cyclohept-1-en-1-yl)phenyl)ethynyl)-N,4-dimethylbenzenesulfonamide leading to naphthalenes, e.g., I and phenanthrenes, e.g., II has been described. These reactions were completed within 3 s by using I(coll)₂PF₆ as an iodonium reagent, and cyclized products were obtained in good to high yields. This method is the most rapid synthesis known to date of polycyclic aromatic compounds In the experiment, the researchers used many compounds, for example, 1-Tosylpiperidin-4-one (cas: 33439-27-9Application In Synthesis of 1-Tosylpiperidin-4-one).

1-Tosylpiperidin-4-one (cas: 33439-27-9) 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 1-Tosylpiperidin-4-one

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Ligand and Target Discovery by Fragment-Based Screening in Human Cells was written by Parker, Christopher G.;Galmozzi, Andrea;Wang, Yujia;Correia, Bruno E.;Sasaki, Kenji;Joslyn, Christopher M.;Kim, Arthur S.;Cavallaro, Cullen L.;Lawrence, R. Michael;Johnson, Stephen R.;Narvaiza, Inigo;Saez, Enrique;Cravatt, Benjamin F.. And the article was included in Cell (Cambridge, MA, United States) in 2017.Safety of 4-(2-Methoxyphenyl)piperidine This article mentions the following:

Advances in the synthesis and screening of small-mol. libraries have accelerated the discovery of chem. probes for studying biol. processes. Still, only a small fraction of the human proteome has chem. ligands. Here, we describe a platform that marries fragment-based ligand discovery with quant. chem. proteomics to map thousands of reversible small mol.-protein interactions directly in human cells, many of which can be site-specifically determined We show that fragment hits can be advanced to furnish selective ligands that affect the activity of proteins heretofore lacking chem. probes. We further combine fragment-based chem. proteomics with phenotypic screening to identify small mols. that promote adipocyte differentiation by engaging the poorly characterized membrane protein PGRMC2. Fragment-based screening in human cells thus provides an extensive proteome-wide map of protein ligandability and facilitates the coordinated discovery of bioactive small mols. and their mol. targets. In the experiment, the researchers used many compounds, for example, 4-(2-Methoxyphenyl)piperidine (cas: 58333-75-8Safety of 4-(2-Methoxyphenyl)piperidine).

4-(2-Methoxyphenyl)piperidine (cas: 58333-75-8) 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. 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.Safety of 4-(2-Methoxyphenyl)piperidine

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

6-Amino-4-(pyrimidin-4-yl)pyridones: Novel glycogen synthase kinase-3β inhibitors was written by Coffman, Karen;Brodney, Michael;Cook, James;Lanyon, Lorraine;Pandit, Jayvardhan;Sakya, Subas;Schachter, Joel;Tseng-Lovering, Elaine;Wessel, Matthew. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2011.Name: 4-(2-Methoxyphenyl)piperidine This article mentions the following:

The synthesis and structure-activity relationships for a novel series of 6-amino-4-(pyrimidin-4-yl)pyridones e. g., I derived from a high throughput screening hit are discussed. Optimization of lead matter afforded compounds with good potency, selectivity and central nervous system (CNS) exposure. In the experiment, the researchers used many compounds, for example, 4-(2-Methoxyphenyl)piperidine (cas: 58333-75-8Name: 4-(2-Methoxyphenyl)piperidine).

4-(2-Methoxyphenyl)piperidine (cas: 58333-75-8) belongs to piperidine derivatives. Piperidine is a metabolite of cadaverine, a polyamine found in the human intestine. 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.Name: 4-(2-Methoxyphenyl)piperidine

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Towards metabolically stable 5-HT₇ receptor ligands: a study on 1-arylpiperazine derivatives and related isosters was written by Lacivita, Enza;De Giorgio, Paola;Patarnello, Daniela;Niso, Mauro;Colabufo, Nicola A.;Berardi, Francesco;Perrone, Roberto;Satala, Grzegorz;Duszynska, Beata;Bojarski, Andrzej J.;Leopoldo, Marcello. And the article was included in Experimental Brain Research in 2013.Safety of 4-(2-Methoxyphenyl)piperidine This article mentions the following:

Serotonin 7 (5-hydroxytryptamine7 or 5-HT₇) is the most recently identified serotonin receptor. It is involved in mood disorders and is studied as a target for antidepressants. Here, we report on the structural manipulation of the 5-HT₇ receptor ligand 4-[2-(3-methoxyphenyl)ethyl]-1-(2-methoxyphenyl)piperazine (1a) aimed at obtaining 5-HT₇ receptor ligands endowed with good in vitro metabolic stability. A set of N-[3-methoxyphenyl)ethyl-substituted] 1-arylpiperazine, 4-arylpiperidine and 1-aryl-4-aminopiperidine was synthesized and tested in radioligand binding assays at human cloned 5-HT₇ and 5-HT_1A receptors. In vitro metabolic stability of the target compounds was assessed after incubation with rat hepatic S9 microsomal fraction. Among the new compounds, 1-(2-biphenyl)-4-[2-(3-methoxyphenyl)ethyl]piperazine (1d) and 4-(2-biphenyl)-1-[2-(3-methoxyphenyl)ethyl]piperidine (2d) showed a good compromise between affinity at 5-HT₇ receptor (K_i = 7.5 nM and 13 nM, resp.) and in vitro metabolic stability (26 and 65 % recovery of parent compound, resp.) but were poorly selective over 5-HT_1A receptor. In the experiment, the researchers used many compounds, for example, 4-(2-Methoxyphenyl)piperidine (cas: 58333-75-8Safety of 4-(2-Methoxyphenyl)piperidine).

4-(2-Methoxyphenyl)piperidine (cas: 58333-75-8) 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.Safety of 4-(2-Methoxyphenyl)piperidine

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem