Category: piperidines

The author of 《Highly durable and conductive poly(arylene piperidine) with a long heterocyclic ammonium side-chain for hydroxide exchange membranes》 were Jin, Cuihong; Zhang, Shuai; Cong, Yuanyuan; Zhu, Xiuling. And the article was published in International Journal of Hydrogen Energy in 2019. Related Products of 1445-73-4 The author mentioned the following in the article:

Recently, the preparation of hydroxide exchange membranes (HEMs) without ether bonds have attracted much attention because of their high chem. stability. Hence, ether-bond free, highly durable, and conductive poly(arylene piperidine)s (PAPips) tethered with heterocyclic ammonium via hexyl spacer chains were prepared successfully for HEMs via a facile synthetic procedure. The effect of the cationic groups (quaternary ammonium, piperidinium, and morpholinium) on the properties of the corresponding PAPip-based HEMs, including the morphol., hydroxide conductivity, and alk. and chem. stability were systematically investigated. The as-designed PAPip-based membranes exhibited excellent overall performance. The membranes attached with piperidinium (IEC = 1.64 mmol g-1) exhibited a hydroxide conductivity of 0.082 S cm-1 at 80°C and exhibited significant alk. stability which maintained 80.1% of its conductivity after immersion in 1 M NaOH at 80°C for 1500 h. The as-prepared membrane also presented a peak power d. of 76 mW cm-2 at 80°C in a H2/O2 HEMFC. The resulting HEMs also showed excellent mech. properties, thermal stability, and well-defined phase separation In the experimental materials used by the author, we found 1-Methyl-4-piperidone(cas: 1445-73-4Related Products of 1445-73-4)

1-Methyl-4-piperidone(cas: 1445-73-4) 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.Related Products of 1445-73-4

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

In 2019,European Journal of Medicinal Chemistry included an article by Yao, Bin-Rong; Sun, Yue; Chen, Shuang-Long; Suo, Hao-Dong; Zhang, Yu-Long; Wei, Hao; Wang, Chun-Hua; Zhao, Feng; Cong, Wei; Xin, Wen-Yu; Hou, Gui-Ge. Related Products of 1445-73-4. The article was titled 《Dissymmetric pyridyl-substituted 3,5-bis(arylidene)-4-piperidones as anti-hepatoma agents by inhibiting NF-κB pathway activation》. The information in the text is summarized as follows:

A series of dissym. pyridyl-substituted 3,5-bis(arylidene)-4-piperidones (BAPs, I [R1 = 3-pyridinyl, 4-pyridinyl; R2 = 2-F, 4-cyano, 3,4,5-OMe, etc.] II[R3 = 3-pyridinyl, 4-pyridinyl; R4 = F, CF3; R5 = H, Cl, CF3, etc]) were designed and synthesized to get new anti-hepatoma agents with anti-inflammatory activity and hypotoxicity. Many of them exhibited potential anti-hepatoma properties against human hepatocellular carcinoma cell lines (HepG2, QGY-7703, SMMC-7721) and hypotoxicity for human normal heptical cell line (HHL-5, LO2) and prominently inhibited lipopolysaccharides (LPS) induced IL-6, TNF-α secretion to exert its anti-inflammatory effect. Combining the data of cytotoxicity, cytocompatibility and anti-inflammatory activity, II [R3 = 3-pyridinyl; R4 = R5 = CF3] may be the potential anti-hepatoma agent. II [R3 = 3-pyridinyl; R4 = R5 = CF3] effectively promoted cell apoptosis through up-regulating cleaved caspase-3 and Bax expression and down-regulating Bcl-2 expression. Furthermore, II [R3 = 3-pyridinyl; R4 = R5 = CF3]prominently inhibited NF-κB pathway activation by blocking the phosphorylation of IκBα, p65 and the nuclear translocation of NF-κB induced by TNF-α and LPS. In addition, II [R3 = 3-pyridinyl; R4 = R5 = CF3] could reasonably bind to the active site of Bcl-2 and NF-κB/p65 protein proved by Mol. docking analyses. Moreover, II [R3 = 3-pyridinyl; R4 = R5 = CF3] significantly suppressed the growth and inflammatory response of HepG2 xenografts in nude mice and was relatively nontoxic to mice. These results suggested that II [R3 = 3-pyridinyl; R4 = R5 = CF3] may be effective and hypotoxicity anti-hepatoma agent for the clin. treatment of liver cancers. In the part of experimental materials, we found many familiar compounds, such as 1-Methyl-4-piperidone(cas: 1445-73-4Related Products of 1445-73-4)

1-Methyl-4-piperidone(cas: 1445-73-4) 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 1445-73-4

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

In 2018,Bioorganic & Medicinal Chemistry Letters included an article by Rong, Rui-Xue; Wang, Shan-Shan; Liu, Xuan; Li, Ren-Feng; Wang, Ke-Rang; Cao, Zhi-Ran; Li, Xiao-Liu. Quality Control of 2-(Piperidin-4-yl)ethanol. The article was titled 《Lysosomes-targeting imaging and anticancer properties of novel bis-naphthalimide derivatives》. The information in the text is summarized as follows:

A series of novel bridged bis-naphthalimide derivatives containing saturated nitrogenous heterocycles were designed and synthesized, their cytotoxic activities against Hela, MCF-7, A549 and MGC-803 cells were investigated. Compounds NI1-NI4 (I.4HCl – IV.4HCl, resp.) modified with piperidine and piperazine exhibited good and selective cytotoxic activity, for instance, compounds NI1 (IC50 2.89 and 0.60 μM) and NI4 (2.73 and 1.60 μM) showed potent cytotoxic activity against Hela cells and MGC-803 cells, resp., better than the control drug (Amonafide). However, compounds conjugated with pyrrole derivatives showed weak cytotoxic activities against the all tested cell lines. Furthermore, their DNA binding properties, fluorescence imaging and cell cycle were investigated. Interestingly, compounds NI1 and NI4 showed fluorescence enhancement because of the strong binding with Ct-DNA, and exhibited fluorescence imaging with Hela cells on the lysosomes. In the part of experimental materials, we found many familiar compounds, such as 2-(Piperidin-4-yl)ethanol(cas: 622-26-4Quality Control of 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.Quality Control of 2-(Piperidin-4-yl)ethanol

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Li, Zhuoqian; Li, Kai; Ma, Shuanglong; Dang, Bingjun; Li, Yi; Fu, Haichao; Du, Jinge; Meng, Qingxiang published an article on January 15 ,2021. The article was titled 《Activation of peroxymonosulfate by iron-biochar composites: Comparison of nanoscale Fe with single-atom Fe》, and you may find the article in Journal of Colloid and Interface Science.Recommanded Product: 826-36-8 The information in the text is summarized as follows:

A convenient and efficient method to fabricate isolated Fe single-atom catalysts deposited on Myriophyllum aquaticum-based biochar (ISA-Fe/MC) is reported for peroxymonosulfate-based organics degradation Firstly, the Fe nanoparticles anchored on the hierarchical porous biochar (nano-Fe/MC) can be obtained by utilizing K2FeO4 as a synchronous activation and graphitization agent. Subsequently, ISA-Fe/MC was achieved by HCl etching of nano-Fe/MC to remove the excess Fe nanoparticles. Compared with nano-Fe/MC, ISA-Fe/MC demonstrated outperformed catalytic capacity towards PMS activation for phenol degradation The combination of super high surface area, hierarchical porous structure, graphitization structure and atomically dispersed Fe species should be responsible for prominent catalytic oxidation ability and outstanding resistance to common anions and humic acid. Based on the chem. scavengers, EPR experiments and electrochem. tests, the SO•-4 dominated radical degradation pathway for nano-Fe/MC and electron transfer reigned non-radical degradation pathway for ISA-Fe/MC was revealed. In contrast to nano-Fe/MC, d. functional theory calculations demonstrated the enhanced d. of states around Fermi level in ISA-Fe/MC meaning the increased catalytic performance and more electron transfer between single-atom Fe to adjacent graphitic C and N which could serve as electron transfer channel for PMS activation. In the experimental materials used by the author, we found Triacetonamine(cas: 826-36-8Recommanded Product: 826-36-8)

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.Recommanded Product: 826-36-8

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Thu, Zaw Min; Sun, Jian; Ji, Jingwen; He, Lili; Ji, Jinbo; Iqbal, Zafar; Myo, Ko Ko; Gao, Yuanyu; Zhai, Lijuan; Mu, Yangxiu; Tang, Dong; Vidari, Giovanni; Yang, Haikang; Yang, Zhixiang published an article in 2021. The article was titled 《Synthesis and antibacterial evaluation of new monobactams》, and you may find the article in Bioorganic & Medicinal Chemistry Letters.Application of 87120-72-7 The information in the text is summarized as follows:

Monobactams play an important role in antibiotic drug discovery. Based on the structural characteristics of aztreonam and its biol. targets, six new monobactam derivatives were synthesized and their in vitro antibacterial activities were investigated. Some compounds showed higher activities against tested gram-neg. bacteria than that of parent aztreonam. Monobactam I exhibited the most potent activities, with MIC ranging from 0.25 to 2μg/mL against most bacteria. The experimental part of the paper was very detailed, including the reaction process of tert-Butyl 4-aminopiperidine-1-carboxylate(cas: 87120-72-7Application of 87120-72-7)

tert-Butyl 4-aminopiperidine-1-carboxylate(cas: 87120-72-7) belongs to anime. Many important products require amines as part of their syntheses. Methylamine is utilized in the production of the analgesic meperidine (trade name Demerol) and the photographic developer Metol (trademark), and dimethylamine is used in the synthesis of the antihistamine diphenhydramine (trade name Benadryl), the solvent dimethylformamide (DMF), and the rocket propellant 1,1-dimethylhydrazine. The synthesis of the insect repellent N,N-diethyl-m-toluamide (DEET) incorporates diethylamine while that of the synthetic fibre Kevlar requires aromatic amines.Application of 87120-72-7

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Luo, Guoshun; Lin, Xin; Li, Zhenbang; Xiao, Maoxu; Li, Xinyu; Zhang, Dayong; Xiang, Hua published an article in 2021. The article was titled 《Structure-guided modification of isoxazole-type FXR agonists: Identification of a potent and orally bioavailable FXR modulator》, and you may find the article in European Journal of Medicinal Chemistry.Name: tert-Butyl 4-hydroxypiperidine-1-carboxylate The information in the text is summarized as follows:

Farnesoid X receptor (FXR) agonists are emerging as potential therapeutics for the treatment of various metabolic diseases, as they display multiple effects on bile acid, lipid, and glucose homeostasis. Although the steroidal obeticholic acid, a full FXR agonist, was recently approved, several side effects probably due to insufficient pharmacol. selectivity impede its further clin. application. Activating FXR in a partial manner is therefore crucial in the development of novel FXR modulators. Our efforts focusing on isoxazole-type FXR agonists, common nonsteroidal agonists for FXR, led to the discovery a series of novel FXR agonists bearing aryl urea moieties through structural simplification of LJN452 (phase 2). Encouragingly, compound I was discovered as a potent FXR agonist which exhibited similar FXR agonism potency but lower maximum efficacy compared to full agonists GW4064 and LJN452 in cell-based FXR transactivation assay. Extensive in vitro evaluation further confirmed partial efficacy of I in cellular FXR-dependent gene modulation, and revealed its lipid-reducing activity. More importantly, orally administration of I in mice exhibited desirable pharmacokinetic characters resulting in promising in vivo FXR agonistic activity. The results came from multiple reactions, including the reaction of tert-Butyl 4-hydroxypiperidine-1-carboxylate(cas: 109384-19-2Name: tert-Butyl 4-hydroxypiperidine-1-carboxylate)

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.Name: tert-Butyl 4-hydroxypiperidine-1-carboxylate

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

《Amine-Responsive Disassembly of AuI-CuI Double Salts for Oxidative Carbonylation》 was published in Angewandte Chemie, International Edition in 2020. These research results belong to Cao, Yanwei; Yang, Jian-Gong; Deng, Yi; Wang, Shengchun; Liu, Qi; Shen, Chaoren; Lu, Wei; Che, Chi-Ming; Chen, Yong; He, Lin. Application In Synthesis of tert-Butyl 4-hydroxypiperidine-1-carboxylate The article mentions the following:

A sensitive amine-responsive disassembly of self-assembled AuI-CuI double salts was observed and its use for the synergistic catalysis was enlightened. Study of the disassembly of [Au(NHC)2][CuI2] revealed the contribution of Cu-assisted ligand exchange of N-heterocyclic carbene (NHC) by amine in [Au(NHC)2]+ and the capacity of [CuI2]- on the oxidative step. By integrating the implicative information coded in the responsive behavior and inherent catalytic functions of d10 metal complexes, a catalyst for the oxidative carbonylation of amines was developed. The advantages of this method were clearly reflected on mild reaction conditions and the significantly expanded scope (51 examples); both primary and steric secondary amines can be employed as substrates. The cooperative reactivity from Au and Cu centers, as an indispensable prerequisite for the excellent catalytic performance, was validated in the synthesis of (un)sym. ureas and carbamates. The results came from multiple reactions, including the reaction of tert-Butyl 4-hydroxypiperidine-1-carboxylate(cas: 109384-19-2Application In Synthesis of tert-Butyl 4-hydroxypiperidine-1-carboxylate)

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 In Synthesis of tert-Butyl 4-hydroxypiperidine-1-carboxylate

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

The author of 《Continuous-Flow Synthesis of Phenothiazine Antipsychotics: A Feasibility Study》 were Movsisyan, Marine; De Coen, Laurens M.; Heugebaert, Thomas S. A.; Verlee, Arno; Roman, Bart I.; Stevens, Christian V.. And the article was published in European Journal of Organic Chemistry in 2019. Safety of 2-(Piperidin-4-yl)ethanol The author mentioned the following in the article:

The continuous flow synthesis of a model phenothiazine I antipsychotic was reported, using 3-chloropropionyl chloride as a central building block. The basic phenothiazine-derived scaffold was (atom)-efficiently and mildly synthesized with the aim to present continuous flow technol. as a contributor to fast and efficient synthesis of challenging APIs, which were experiencing supply disruptions and global shortages. The experimental process involved the reaction of 2-(Piperidin-4-yl)ethanol(cas: 622-26-4Safety 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 FAKSafety of 2-(Piperidin-4-yl)ethanol

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

In 2016,Park, Jung Sang; Im, Weonbin; Choi, Sunghak; Park, Sook Jin; Jung, Jun Min; Baek, Ki Seon; Son, Han Pyo; Sharma, Satyasheel; Kim, In Su; Jung, Young Hoon published 《Discovery and SAR of N-(1-((substituted piperidin-4-yl)methyl)-3-methoxypiperidin-4-yl)-2-methoxybenzamide derivatives: 5-Hydroxytryptamine receptor 4 agonist as a potent prokinetic agent》.European Journal of Medicinal Chemistry published the findings.Formula: C7H15NO The information in the text is summarized as follows:

A series of novel benzamide derivatives altering the 4-fluorophenylalkyl moiety in cisapride, was synthesized as 5-HT4 receptor agonists; and SAR of these analogs was examined on in vitro and in vivo prokinetic activities. These compounds were synthesized for high 5-HT4 receptor binding affinities and low hERG affinities. Several types of analogs were obtained and screened for 5-HT4 binding, hERG blocking, agonism and gastric emptying assessment. Among the analogs, compound I showed promising results compared with the other analogs with respect to gastric emptying rates in rats and can be a clin. candidate for the development of a potent prokinetic agent to treat GI disorders. In the experiment, the researchers used many compounds, for example, 2-(Piperidin-4-yl)ethanol(cas: 622-26-4Formula: C7H15NO)

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 FAKFormula: C7H15NO

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

In 2014,Gao, Mingzhang; Wang, Min; Zheng, Qi-Huang published 《Concise and high-yield synthesis of T808 and T808P for radiosynthesis of [18F]-T808, a PET tau tracer for Alzheimer’s disease》.Bioorganic & Medicinal Chemistry Letters published the findings.COA of Formula: C7H15NO The information in the text is summarized as follows:

The authentic standard T808 and its corresponding mesylate precursor T808P were synthesized in six steps using Et vinyl ether and trichloroacetyl chloride as starting materials. The overall chem. yields of T808 and T808P were 35% and 52%, resp. [18F]-T808 was synthesized from T808P by the nucleophilic substitution with K[18F]F/Kryptofix 2.2.2 and isolated by HPLC combined with solid-phase extraction (SPE) purification in 35-45% radiochem. yield with 37-370 GBq/μmol specific activity at end of bombardment (EOB). 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: 622-26-4COA of Formula: 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.COA of Formula: C7H15NO

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem