Day: October 20, 2022

Reference of 2-(Piperidin-4-yl)ethanolIn 2020 ,《Discovery of a Novel, Highly Potent, and Selective Thieno[3,2-d]pyrimidinone-Based Cdc7 Inhibitor with a Quinuclidine Moiety (TAK-931) as an Orally Active Investigational Antitumor Agent》 was published in Journal of Medicinal Chemistry. The article was written by Kurasawa, Osamu; Miyazaki, Tohru; Homma, Misaki; Oguro, Yuya; Imada, Takashi; Uchiyama, Noriko; Iwai, Kenichi; Yamamoto, Yukiko; Ohori, Momoko; Hara, Hideto; Sugimoto, Hiroshi; Iwata, Kentaro; Skene, Robert; Hoffman, Isaac; Ohashi, Akihiro; Nomura, Toshiyuki; Cho, Nobuo. The article contains the following contents:

In our pursuit of developing a novel, potent, and selective cell division cycle 7 (Cdc7) inhibitor, we optimized the previously reported thieno[3,2-d]pyrimidinone analog I showing time-dependent Cdc7 kinase inhibition and slow dissociation kinetics. These medicinal chem. efforts led to the identification of compound 3d, which exhibited potent cellular activity, excellent kinase selectivity, and antitumor efficacy in a COLO205 xenograft mouse model. However, the issue of formaldehyde adduct formation emerged during a detailed study of 3d, which was deemed an obstacle to further development. A structure-based approach to circumvent the adduct formation culminated in the discovery of compound 11b (TAK-931) possessing a quinuclidine moiety as a preclin. candidate. In this paper, the design, synthesis, and biol. evaluation of this series of compounds will be presented. In the experiment, the researchers used many compounds, for example, 2-(Piperidin-4-yl)ethanol(cas: 622-26-4Reference of 2-(Piperidin-4-yl)ethanol)

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 FAKReference of 2-(Piperidin-4-yl)ethanol

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

《A novel series of potent and selective ketone histone deacetylase inhibitors with antitumor activity in vivo》 was written by Jones, Philip; Altamura, Sergio; De Francesco, Raffaele; Gonzalez Paz, Odalys; Kinzel, Olaf; Mesiti, Giuseppe; Monteagudo, Edith; Pescatore, Giovanna; Rowley, Michael; Verdirame, Maria; Steinkuhler, Christian. Reference of 1-Methylpiperidine-2-carboxylic acid hydrochloride And the article was included in Journal of Medicinal Chemistry on April 24 ,2008. The article conveys some information:

Histone deacetylase (HDAC) inhibitors offer a promising strategy for cancer therapy, and the first generation HDAC inhibitors are currently in the clinic. Entirely novel ketone HDAC inhibitors have been developed from the cyclic tetrapeptide apicidin. These compounds show class I subtype selectivity and levels of cellular activity comparable to clin. candidates. A representative example has demonstrated tumor growth inhibition in a human colon HCT-116 carcinoma xenograft model comparable to known inhibitors. The experimental process involved the reaction of 1-Methylpiperidine-2-carboxylic acid hydrochloride(cas: 25271-35-6Reference of 1-Methylpiperidine-2-carboxylic acid hydrochloride)

1-Methylpiperidine-2-carboxylic acid hydrochloride(cas: 25271-35-6) 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.Reference of 1-Methylpiperidine-2-carboxylic acid hydrochloride

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

《Molecular Orientation and Dynamics of a Derivative of 2,2,6,6-Tetramethyl-1-Piperidinyloxyl Radical with a Large Substituent Group Dispersed in 1D-Nanochannels of 2,4,6-Tris(4-Chlorophenoxy)-1,3,5-Triazine Crystal》 was written by Kobayashi, Hirokazu; Odanaka, Yuki. Related Products of 826-36-8 And the article was included in Applied Magnetic Resonance on August 31 ,2020. The article conveys some information:

The mol. orientation and dynamics were examined for 4-acetamido-2,2,6,6-tetramethyl-1-piperidinyloxyl (4-acetamido-TEMPO) radicals, which have a larger substituent group than many other TEMPO radicals, dispersed in the one-dimensional (1D) nanochannel of 2,4,6-tris(4-chlorophenoxy)-1,3,5-triazine (CLPOT) with 4-substituted-2,2,6,6-tetramethylpiperidine (R-TEMP; R=OH or H). When TEMPOH (R=OH) was used as a spacer for dispersion in the CLPOT nanochannels, the mol. orientation of 4-acetamido-TEMPO in the CLPOT nanochannels was similar to that of other previously reported 4-substituted-TEMPO (4-X-TEMPO; X=OH, =O or OCH3) radicals. However, the activation energy for the rotational diffusion of 4-acetamido-TEMPO in the CLPOT nanochannels, estimated to be 11 kJ mol-1, was larger than that of other 4-X-TEMPO mols. (6-8 kJ mol-1). These results indicate that the mol. dynamics of 4-X-TEMPO in the CLPOT nanochannels can be controlled by the selection of a larger substituent X at the 4-position in 4-X-TEMPO (in this study, X=NHCOCH3), and also suggest an important concept for the design of new organic magnets. In addition to this study using Triacetonamine, there are many other studies that have used Triacetonamine(cas: 826-36-8Related Products of 826-36-8) was used in this study.

Triacetonamine(cas: 826-36-8) is a member of piperidine. 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. Hence, continuous efforts have been made to develop convenient methods to prepare piperidine derivatives.Related Products of 826-36-8

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

《Structure-Based Bioisosterism Yields HIV-1 NNRTIs with Improved Drug-Resistance Profiles and Favorable Pharmacokinetic Properties》 was written by Kang, Dongwei; Feng, Da; Sun, Yanying; Fang, Zengjun; Wei, Fenju; De Clercq, Erik; Pannecouque, Christophe; Liu, Xinyong; Zhan, Peng. Quality Control of tert-Butyl 4-aminopiperidine-1-carboxylateThis research focused onthiophenepyrimidine piperidine substituted preparation antiHIV activity. The article conveys some information:

The development of efficacious NNRTIs for AIDS therapy commonly encountered the rapid generation of drug-resistant mutations, which becomes a major impediment to effective anti-HIV treatment. Using a structure-based bioisosterism strategy, a series of piperidine-substituted thiophene[2,3-d]pyrimidine derivatives were designed and synthesized. Compound I yielded the greatest potency, exhibiting significantly better anti-HIV-1 activity than ETR against all of the tested NNRTI-resistant HIV-1 strains. In addition, the phenotypic (cross)resistance of I and other NRTIs to the different selected HIV-1 strains was evaluated. As expected, no phenotypic cross-resistance against the NRTIs (AZT and PMPA) was observed with the mutant Ires strain. Furthermore, I was identified with improved solubility, lower CYP liability, and hERG inhibition. Remarkably, I exhibited optimal pharmacokinetic properties in rats (F = 37.06%) and safety in mice (LD50 > 2000 mg/kg), which highlights I as a promising anti-HIV-1 drug candidate. After reading the article, we found that the author used tert-Butyl 4-aminopiperidine-1-carboxylate(cas: 87120-72-7Quality Control of tert-Butyl 4-aminopiperidine-1-carboxylate)

tert-Butyl 4-aminopiperidine-1-carboxylate(cas: 87120-72-7) 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.Quality Control of tert-Butyl 4-aminopiperidine-1-carboxylate

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Product Details of 826-36-8On May 3, 2022 ,《Marine colloids promote the adaptation of diatoms to nitrate contamination by directional electron transfer》 appeared in Environmental Science & Technology. The author of the article were Kang, Weilu; Yu, Fubo; Wang, Shuting; Hu, Xiangang. The article conveys some information:

Nitrate contamination from human activities (e.g., domestic pollution, livestock breeding, and fertilizer application) threatens marine ecosystems and net primary productivity. As the main component of primary productivity, diatoms can adapt to high nitrate environments, but the mechanism is unclear. We found that electron transfer from marine colloids to diatoms enhances nitrogen uptake and assimilation under visible-light irradiation, providing a new pathway for nitrogen adaptation. Under irradiation, marine colloids exhibit semiconductor properties (e.g., the separation of electron-hole pairs) and can trigger the generation of free electrons and singlet oxygen. They also exhibit electron acceptor and donor properties, with the former being stronger than the latter, reacting with polysaccharides in extracellular polymeric substances (EPSs) under high nitrogen stress, enhancing the elasticity and permeability of cells, and promoting nitrogen assimilation and electron transfer to marine diatom EPSs. Electron transfer promotes extracellular-to-intracellular nitrate transport by upregulating membrane nitrate transporters and nitrate reductase. The upregulation of anion transport genes and unsaturated fatty acids contributes to nitrogen assimilation. We estimate that colloids may increase the nitrate uptake efficiency of marine diatoms by 10.5-82.2%. These findings reveal a mechanism by which diatoms adapt to nitrate contamination and indicate a low-cost strategy to control marine pollution. In the part of experimental materials, we found many familiar compounds, such as Triacetonamine(cas: 826-36-8Product Details of 826-36-8)

Triacetonamine(cas: 826-36-8) is a member of piperidine. 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. Hence, continuous efforts have been made to develop convenient methods to prepare piperidine derivatives.Product Details of 826-36-8

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Mao, Shuhua; Jiang, Zhiyuan; Yuan, Jie; Wu, Tun; Zhang, Qianqian; Liu, Haisheng; Chen, Mingzhao; Liu, Qianqian; Zhang, Zhe; Wang, Pingshan published an article on January 31 ,2022. The article was titled 《(RuBpy3)2+-bisterpyridinyl triangle promoted singlet oxygen (1O2) photosensitization for fast oxidation of sulfur mustard simulant》, and you may find the article in Inorganic Chemistry Communications.COA of Formula: C9H17NO The information in the text is summarized as follows:

(RuBpy3)2+-bisterpyridine-based metallacycle T photosensitizer was prepared by a facile single-step self-assembly process. Supramol. self-assembly strategy greatly improved metallacycle T’s photosensitized ability due to its enhanced light-harvesting capability, smaller energy gap (ΔEST) between lowest excited singlet state (S1) and lowest excited triplet state (T1) along with excellent solubility which exhibiting higher efficiency for singlet oxygen (1O2) production than the ligand L and its pendant [(RuBpy3)2+·2PF6-]. In the practical photo-driven degradation of sulfur mustard simulant (2-chloroethyl Et sulfide, CEES), full conversion of toxic CEES to nontoxic CEESO was achieved by metallacycle T with an extremely fast lifetime of 90 s (half lifetime t1/2 = 25 s) and 100% selectivity (without formation of highly toxic CEESO2), while ligand L and [(RuBpy3)2+·2PF6-] needed 130 s and 330 s, resp. This study demonstrated terpyridine-based novel supermols. can serve as efficient scaffolds for effective enhancement of photosensitization. The experimental process involved the reaction of Triacetonamine(cas: 826-36-8COA of Formula: C9H17NO)

Triacetonamine(cas: 826-36-8) is a member of piperidine. 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. Hence, continuous efforts have been made to develop convenient methods to prepare piperidine derivatives.COA of Formula: C9H17NO

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Sasakura, Kazuyuki; Adachi, Makoto; Sugasawa, Tsutomu published their research in Synthetic Communications on February 29 ,1988. The article was titled 《Simple synthesis of 1-(azacycloalkyl)indoles using exclusive ortho α-chloroacetylation of N-(azacycloalkyl)anilines》.Recommanded Product: 1-(Piperidin-4-yl)-1H-indole The article contains the following contents:

Indoles I (n = 1,2; R1 = H, F; R2 = H, halo, OMe) were prepared from the resp. 2-amino-2-chloroacetophenones II (R3 = Me, PhCH2) by sequential hydride reduction, cyclization, dealkylation-acylation with ClCO2Et, and deacylation. In the part of experimental materials, we found many familiar compounds, such as 1-(Piperidin-4-yl)-1H-indole(cas: 118511-81-2Recommanded Product: 1-(Piperidin-4-yl)-1H-indole)

1-(Piperidin-4-yl)-1H-indole(cas: 118511-81-2) belongs to piperidines. Piperidine derivatives are also used in solid-phase peptide synthesis (SPPS) and many degradation reactions. Recommanded Product: 1-(Piperidin-4-yl)-1H-indole

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Wang, Xiaolei; Ding, Yingzhi; Dionysiou, Dionysios D.; Liu, Cun; Tong, Yunping; Gao, Juan; Fang, Guodong; Zhou, Dongmei published their research in Science of the Total Environment on December 20 ,2020. The article was titled 《Efficient activation of peroxymonosulfate by copper sulfide for diethyl phthalate degradation: Performance, radical generation and mechanism》.SDS of cas: 826-36-8 The article contains the following contents:

Copper-containing minerals have been extensively used in Fenton-like processes for degradation of pollutants and have exhibited great potential for environmental remediation. This work reports the first use of copper sulfide (CuS), a typical Cu-mineral, for the activation of peroxymonosulfate (PMS) for pollutant degradation; the study also elucidates the underlying mechanism of these processes. Copper sulfide effectively activated PMS to degrade di-Et phthalate (DEP). ESR, free radical quenching, XPS, X-ray diffraction analyses and DFT calculations confirmed that Ξ Cu (I)/ ΞCu (II) cycling on the surface of CuS provided the main pathway to activate PMS to produce highly oxidative species. Unlike conventional sulfate radical-based PMS activation processes, hydroxyl radical (·OH) were found to be the dominant radical in the tested CuS/PMS system, which performed more efficiently than an alternative ·OH-based oxidation system (CuS/H2O2) for DEP degradation In addition, the presence of anions such Cl- and NO-3 has limited inhibition effects on DEP degradation Overall, this study provides an efficient pathway for PMS-based environmental remediation as well as a new insight into the mechanism of PMS activation by Cu-containing minerals. In the experiment, the researchers used many compounds, for example, Triacetonamine(cas: 826-36-8SDS of cas: 826-36-8)

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.SDS of cas: 826-36-8

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

In 2016,Horikawa, Rikiya; Fujimoto, Chika; Yazaki, Ryo; Ohshima, Takashi published 《μ-Oxo-Dinuclear-Iron(III)-Catalyzed O-Selective Acylation of Aliphatic and Aromatic Amino Alcohols and Transesterification of Tertiary Alcohols》.Chemistry – A European Journal published the findings.COA of Formula: C7H15NO The information in the text is summarized as follows:

A highly chemoselective and reactive μ-oxo-dinuclear iron(III) salen catalyst for transesterification was developed. The developed iron complex catalyzed acylation of aliphatic amino alcs. with nearly perfect O-selectivity, even when using activated esters, for which chemoselectivity is more difficult to control. In addition, O-selective transesterification of aromatic amino alcs. was achieved for the first time. The high activity of the iron complex enabled the use of sterically congested tertiary alcs., including unprecedented tert-butanol. After reading the article, we found that the author used 2-(Piperidin-4-yl)ethanol(cas: 622-26-4COA of Formula: C7H15NO)

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.COA of Formula: C7H15NO

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

In 2017,Yamaki, Susumu; Koga, Yuji; Nagashima, Akira; Kondo, Mitsuhiro; Shimada, Yoshiaki; Kadono, Keitaro; Moritomo, Ayako; Yoshihara, Kosei published 《Synthesis and pharmacological evaluation of glycine amide derivatives as novel vascular adhesion protein-1 inhibitors without CYP3A4 and CYP2C19 inhibition》.Bioorganic & Medicinal Chemistry published the findings.Synthetic Route of C7H15NO The information in the text is summarized as follows:

Vascular adhesion protein-1 (VAP-1) is a promising therapeutic target for the treatment of diabetic nephropathy. Here, the authors conducted optimization studies of the authors’ lead compound 1 (I), which the authors previously reported as a novel VAP-1 inhibitor, to enhance the inhibition of human VAP-1 and to reduce CYP3A4 and CYP2C19 inhibition. As a result, the authors identified 3-chloro-4-{4-[5-(3-{[glycyl(methyl)amino]methyl}phenyl)pyrimidin-2-yl]piperazin-1-yl}benzoic acid (17h) as a novel orally active VAP-1 inhibitor, with 14-fold increased human VAP-1 inhibitory activity compared to 1, without CYP3A4 and CYP2C19 inhibition. Oral administration of 17h significantly inhibited the progression of proteinuria in streptozotocin (STZ) induced diabetic rats at 0.3 and 1 mg/kg, suggesting that this compound has potential to be a therapeutic agent for the treatment of diabetic nephropathy. 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: 622-26-4Synthetic Route of C7H15NO) 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.Synthetic Route of C7H15NO

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem