Day: October 20, 2022

In 2019,Inorganica Chimica Acta included an article by Prishchenko, Andrey A.; Alekseyev, Roman S.; Livantsov, Mikhail V.; Novikova, Olga P.; Livantsova, Ludmila I.; Petrosyan, Valery S.. Safety of 1-Methyl-4-piperidone. The article was titled 《Bis(trimethylsiloxy)phosphine as key synthon for synthesis of new aminomethylphosphinic acids with N-alkyl 4-hydroxypiperidines moieties》. The information in the text is summarized as follows:

The convenient synthesis of new aminomethylphosphinic acids and their derivatives containing N-alkyl 4-hydroxypiperidines moieties was developed. The addition of bis(trimethylsiloxy)phosphine to N-alkyl 4-piperidones proceeds under mild conditions to give PH-phosphinates as key compounds for preparation of trimethylsilyl esters of above acids via interaction with various aminals. The further treatment of phosphinic acids trimethylsilyl esters with the methanol resulted in the water-soluble corresponding acids. The structures of aminomethylphosphinic acids and their precursors 1-3 with substituted piperidine moieties were confirmed by the 1H, 13C, 31P NMR spectra. In the experimental materials used by the author, we found 1-Methyl-4-piperidone(cas: 1445-73-4Safety of 1-Methyl-4-piperidone)

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

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

《Novel colchicine conjugate with unusual effect on the microtubules of cancer cells》 was published in Pure and Applied Chemistry in 2020. These research results belong to Zefirova, Olga N.; Nurieva, Evgenia V.; Wobith, Birgit; Schulz, Svetlana; Zefirov, Nikolay A.; Kuznetsov, Sergei A.. Synthetic Route of C10H19NO3 The article mentions the following:

Colchicine derivative bearing substituted bispidine moiety, namely N-{7-(3,7-Di-(tert-butoxycarbonyl)-1,5-dimethyl-3,7-diazabicyclo[3.3.1]nonan-9-yl)-oxy-7-oxoheptanoyl}-N-deacetylcolchicine, was synthesized and tested for its effect on the net of microtubules (MT) in lung cancer cells A549. The compound induced not only MT depolymerization but stimulated the formation of small tubulin aggregates and long tubulin fibrils localized mainly around nuclei. The assemblies were morphol. different from tubulin clusters induced by structurally related anticancer agent tubuloclustin. The biotests data demonstrate that the depolymerization takes place for both pure tubulin and tubulin in cellulo, while fibrils are formed only in the cells. The research data of structure-activity relationship for several similar colchicine derivatives synthesized in the work give evidence for the proposition that the initial conjugate may interact not only with tubulin and MT in the cells, but also with MT-associated proteins, involved in the process of tubulin polymerization The ability to affect simultaneously MAP – tubulin interactions opens attractive prospects in the design of novel anticancer agents. The experimental process involved the reaction of tert-Butyl 4-hydroxypiperidine-1-carboxylate(cas: 109384-19-2Synthetic Route of C10H19NO3)

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.Synthetic Route of C10H19NO3

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

《Design, synthesis, and structure activity relationship (SAR) studies of novel imidazo[1,2-a]pyridine derivatives as Nek2 inhibitors》 was written by Wang, Haili; Chen, Yunzhong; Gu, Xiaofan; Xi, Jianbei; Ren, Ziwei; Wang, Shuting; Duan, Yanhong; Li, Hongyu; Zhu, Tong; Du, Yijie; Zhang, Xiongwen; Ma, Mingliang. Formula: C10H19NO3 And the article was included in Bioorganic & Medicinal Chemistry in 2020. The article conveys some information:

Herein, a series of imidazo[1,2-a]pyridines, e.g., I, Nek2 inhibitors were designed, synthesized and their biol. activities were investigated. Besides, structure activity relationship anal. of these compounds were performed in the MGC-803 cell. The screening results are promising, and tert-Bu 3-((4-(3-(5-carbamoyl-4-(1-(2-(trifluoromethyl)phenyl)ethoxy)thiophen-2-yl) imidazo[1,2-a] pyridine-7-yl)-1H-pyrazol-1-yl)methyl)azetidine-1-carboxylate showed good proliferation inhibitory activity with an IC50 of 38 nM. The results would be helpful to design and develop more effective Nek2 inhibitors for the treatment of gastric cancer. In addition to this study using tert-Butyl 4-hydroxypiperidine-1-carboxylate, there are many other studies that have used tert-Butyl 4-hydroxypiperidine-1-carboxylate(cas: 109384-19-2Formula: C10H19NO3) was used in this study.

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.Formula: C10H19NO3

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

《Poly(meta/para-terphenylene-methyl piperidinium)-based anion exchange membranes: the effect of backbone structure in AEMFC application》 was written by Mayadevi, T. S.; Sung, Seounghwa; Varghese, Listo; Kim, Tae-Hyun. Synthetic Route of C6H11NO And the article was included in Membranes (Basel, Switzerland) in 2020. The article conveys some information:

A series of poly( meta/para-terphenylene-Me piperidinium)-based anion exchange membranes devoid of benzylic sites or aryl ether bonds, that are vulnerable to degradation by hydroxide ions, are synthesized and investigated for their application as novel anion exchange membranes. The copolymers are composed of both linear para-terphenyl units and kink-structured meta-terphenyl units. The meta-connectivity in terphenyl units permits the polymer backbones to fold back, maximizing the interactions among the hydrocarbon polymer chains and enhancing the peripheral formation of ion aggregates, due to the free volume generated by the kink structure. The effects of the copolymer composition between para-terphenyl and meta-terphenyl on the morphol. and the electrochem. and physicochem. properties of the corresponding polymer membranes are investigated. In the experiment, the researchers used 1-Methyl-4-piperidone(cas: 1445-73-4Synthetic Route of C6H11NO)

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.Synthetic Route of C6H11NO

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Klug, Dana M.; Mavrogiannaki, Eftychia M.; Forbes, Katherine C.; Silva, Lisseth; Diaz-Gonzalez, Rosario; Perez-Moreno, Guiomar; Ceballos-Perez, Gloria; Garcia-Hernandez, Raquel; Bosch-Navarrete, Cristina; Cordon-Obras, Carlos; Gomez-Linan, Claudia; Saura, Andreu; Momper, Jeremiah D.; Martinez-Martinez, Maria Santos; Manzano, Pilar; Syed, Ali; El-Sakkary, Nelly; Caffrey, Conor R.; Gamarro, Francisco; Ruiz-Perez, Luis Miguel; Gonzalez Pacanowska, Dolores; Ferrins, Lori; Navarro, Miguel; Pollastri, Michael P. published an article in 2021. The article was titled 《Lead Optimization of 3,5-Disubstituted-7-Azaindoles for the Treatment of Human African Trypanosomiasis》, and you may find the article in Journal of Medicinal Chemistry.Application of 109384-19-2 The information in the text is summarized as follows:

Neglected tropical diseases such as human African trypanosomiasis (HAT) are prevalent primarily in tropical climates and among populations living in poverty. Historically, the lack of economic incentive to develop new treatments for these diseases has meant that existing therapeutics have serious shortcomings in terms of safety, efficacy, and administration, and better therapeutics are needed. We now report a series of 3,5-disubstituted-7-azaindoles identified as growth inhibitors of Trypanosoma brucei, the parasite that causes HAT, through a high-throughput screen. We describe the hit-to-lead optimization of this series and the development and preclin. investigation of 29d (I), a potent antitrypanosomal compound with promising pharmacokinetic (PK) parameters. This compound was ultimately not progressed beyond in vivo PK studies due to its inability to penetrate the blood-brain barrier (BBB), critical for stage 2 HAT treatments. In the experiment, the researchers used tert-Butyl 4-hydroxypiperidine-1-carboxylate(cas: 109384-19-2Application of 109384-19-2)

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 of 109384-19-2

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Frolov, Andriy I.; Ostapchuk, Eugeniy N.; Pashenko, Alexander E.; Chuchvera, Yaroslav O.; Rusanov, Eduard B.; Volochnyuk, Dmitriy M.; Ryabukhin, Sergey V. published an article in 2021. The article was titled 《Selective α-Methylation of Ketones》, and you may find the article in Journal of Organic Chemistry.Reference of 1-Methyl-4-piperidone The information in the text is summarized as follows:

The convenient and scalable preparative approach for the two-step α-methylation of ketones was described. The optimized protocols for regioselective preparation of enaminones with further diastereoselective and functional groups tolerant hydrogenation to α-methylketones was developed. The scope and limitations of the proposed methodol. were discussed. The advantages compared to known procedures were demonstrated. The unexpected role of acetone in the hydrogenation was suggested. The evaluation of the method for both early building block synthesis and late-stage CH-functionalization was shown. The elaborate procedures preparability and scalability were demonstrated by the synthesis of several α-Me ketones up to 100 g amount The results came from multiple reactions, including the reaction of 1-Methyl-4-piperidone(cas: 1445-73-4Reference of 1-Methyl-4-piperidone)

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.Reference of 1-Methyl-4-piperidone

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

In 2022,Zhang, Jingyu; Che, Jinxin; Luo, Xiaomin; Wu, Mingfei; Kan, Weijuan; Jin, Yuheng; Wang, Hanlin; Pang, Ao; Li, Cong; Huang, Wenhai; Zeng, Shenxin; Zhuang, Weihao; Wu, Yizhe; Xu, Yongjin; Zhou, Yubo; Li, Jia; Dong, Xiaowu published an article in Journal of Medicinal Chemistry. The title of the article was 《Structural Feature Analyzation Strategies toward Discovery of Orally Bioavailable PROTACs of Bruton’s Tyrosine Kinase for the Treatment of Lymphoma》.HPLC of Formula: 109384-19-2 The author mentioned the following in the article:

Bruton’s tyrosine kinase proteolysis-targeting chimeras (BTK-PROTACs) have emerged as a promising approach to address the limitations of BTK inhibitors. However, conducting the rational discovery of orally bioavailable BTK-PROTACs presents significant challenges. In this study, dimensionality reduction anal. and model mol. validation were utilized to identify some key structural features for improving the oral absorption of BTK-PROTACs. The results were applied to optimize the newly discovered BTK-PROTACs B1 and B2. Compound C13 (I) was discovered with improved oral bioavailability, high BTK degradation activity, and selectivity. It exhibited inhibitory effects against different hematol. cancer cells and attenuated the BTK-related signaling pathway. The oral administration of C13 effectively reduced BTK protein levels and suppressed tumor growth. This study led to the discovery of a new orally bioavailable BTK-PROTAC for the treatment of lymphoma, and we hope that the strategy will find wide utility. After reading the article, we found that the author used tert-Butyl 4-hydroxypiperidine-1-carboxylate(cas: 109384-19-2HPLC of Formula: 109384-19-2)

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.HPLC of Formula: 109384-19-2

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Electric Literature of C10H20N2O2In 2022 ,《Exploratory studies on soluble small molecule CD4 mimics as HIV entry inhibitors》 appeared in Bioorganic & Medicinal Chemistry. The author of the article were Tsuji, Kohei; Kobayakawa, Takuya; Konno, Kiju; Masuda, Ami; Takahashi, Kohei; Ohashi, Nami; Yoshimura, Kazuhisa; Kuwata, Takeo; Matsushita, Shuzo; Harada, Shigeyoshi; Tamamura, Hirokazu. The article conveys some information:

Several small mol. CD4 mimics, which inhibit the interaction of gp120 with CD4, have been developed. Original CD4 mimics such as NBD-556, which has an aromatic ring, an oxalamide linker and a piperidine moiety, possess significant anti-HIV activity but with their hydrophobic aromatic ring-containing structures are poorly soluble in water. We have developed derivatives with a halopyridinyl group in place of the Ph group, such as KKN-134, and found them to have excellent aqueous solubility Other leads that were examined are YIR-821, a compound with a cyclohexane group in a spiro attachment to a piperidine ring and a guanidino group on the piperidine nitrogen atom, and its PEGylated derivative, TKB-002. YIR-821 and TKB-002 retain potent anti-HIV activity. Here, new CD4 mimics, in which the Ph group was replaced by a halopyridinyl group with the halogen atoms in different positions, their derivatives without a cyclohexane group on the piperidine ring and their hybrid mols. with PEG units were designed and synthesized. Some of these compounds show significantly higher aqueous solubility with maintenance of certain levels of anti-HIV activity. The present data should be useful in the future design of CD4 mimic mols. The experimental process involved the reaction of tert-Butyl 4-aminopiperidine-1-carboxylate(cas: 87120-72-7Electric Literature of C10H20N2O2)

tert-Butyl 4-aminopiperidine-1-carboxylate(cas: 87120-72-7) belongs to anime. Aniline, ethanolamines, and several other amines are major industrial commodities used in making rubber, dyes, pharmaceuticals, and synthetic resins and fibres and for a host of other applications. Most of the numerous methods for the preparation of amines may be broadly divided into two groups: (1) chemical reduction (replacement of oxygen with hydrogen atoms in the molecule) of members of several other classes of organic nitrogen compounds and (2) reactions of ammonia or amines with organic compounds.Electric Literature of C10H20N2O2

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Safety of tert-Butyl 4-hydroxypiperidine-1-carboxylateIn 2021 ,《Design and Synthesis of Novel Spiro Derivatives as Potent and Reversible Monoacylglycerol Lipase (MAGL) Inhibitors: Bioisosteric Transformation from 3-Oxo-3,4-dihydro-2H-benzo[b][1,4]oxazin-6-yl Moiety》 was published in Journal of Medicinal Chemistry. The article was written by Ikeda, Shuhei; Sugiyama, Hideyuki; Tokuhara, Hidekazu; Murakami, Masataka; Nakamura, Minoru; Oguro, Yuya; Aida, Jumpei; Morishita, Nao; Sogabe, Satoshi; Dougan, Douglas R.; Gay, Sean C.; Qin, Ling; Arimura, Naoto; Takahashi, Yasuko; Sasaki, Masako; Kamada, Yusuke; Aoyama, Kazunobu; Kimoto, Kouya; Kamata, Makoto. The article contains the following contents:

The therapeutic potential of monoacylglycerol lipase (MAGL) inhibitors in central nervous system-related diseases has attracted attention worldwide. However, the availability of reversible-type inhibitor is still limited to clarify the pharmacol. effect. Herein, we report the discovery of novel spiro chem. series as potent and reversible MAGL inhibitors with a different binding mode to MAGL using Arg57 and His121. Starting from hit compound 1 and its co-crystal structure with MAGL, structure-based drug discovery (SBDD) approach enabled us to generate various spiro scaffolds like 2a (azetidine-lactam), 2b (cyclobutane-lactam), and 2d (cyclobutane-carbamate) as novel bioisosteres of 3-oxo-3,4-dihydro-2H-benzo[b][1,4]oxazin-6-yl moiety in 1 with higher lipophilic ligand efficiency (LLE). Optimization of the left hand side afforded 4f (I) as a promising reversible MAGL inhibitor, which showed potent in vitro MAGL inhibitory activity (IC50 6.2 nM), good oral absorption, blood-brain barrier penetration, and significant pharmacodynamic changes (2-arachidonoylglycerol increase and arachidonic acid decrease) at 0.3-10 mg/kg, po. in mice. In the part of experimental materials, we found many familiar compounds, such as tert-Butyl 4-hydroxypiperidine-1-carboxylate(cas: 109384-19-2Safety 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.Safety of tert-Butyl 4-hydroxypiperidine-1-carboxylate

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

《Insights on the nitrate reduction and norfloxacin oxidation over a novel nanoscale zero valent iron particle: Reactivity, products, and mechanism》 was written by Diao, Zeng-Hui; Qian, Wei; Lei, Ze-Xiang; Kong, Ling-Jun; Du, Jian-Jun; Liu, Hui; Yang, Jie-Wen; Pu, Sheng Yan. SDS of cas: 826-36-8 And the article was included in Science of the Total Environment on April 10 ,2019. The article conveys some information:

Herein, the application of a novel acid mine drainage-based nanoscale zero valent iron (AMD-based nZVI) for the remediation of nitrate and norfloxacin (NOR) was studied. Exptl. results indicated that the catalytic reactivity of AMD-based nZVI toward nitrate reduction was superior to that of iron salt-based nanoscale zero valent iron (Iron salt-based nZVI). The presence of ultrasound irradiation could significantly enhance the reactivity toward both the nitrate reduction and NOR oxidation processes. The optimal efficiencies of nitrate and NOR by AMD-based nZVI/US process could be kept 96 and 94% within 120 min, resp. Ammonia was identified as a major product in nitrate reduction process, while three oxidation products were observed in NOR degradation process. Both reduction reaction of nitrate from AMD-based nZVI and oxidation reaction of NOR from US-assisted Fenton system might be involved in AMD-based nZVI/US process. The AMD-based nZVI/US process showed a better performance on the removal of NOR compared with that of nitrate. The findings of the present work could be as a guide and show that AMD-based nZVI/US process is feasible for the remediation of both nitrate and NOR in real wastewater. After reading the article, we found that the author used Triacetonamine(cas: 826-36-8SDS of cas: 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.SDS of cas: 826-36-8

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem