Day: October 14, 2022

Salvino, Joseph M.; Kumar, N. Vasant; Orton, Edward; Airey, John; Kiesow, Terence; Crawford, Kenneth; Mathew, Rose; Krolikowski, Paul; Drew, Mark; Engers, Darren; Krolinkowski, David; Herpin, Tim; Gardyan, Michael; McGeehan, Gerald; Labaudiniere, Richard published their research in Journal of Combinatorial Chemistry on December 31 ,2000. The article was titled 《Polymer-Supported Tetrafluorophenol: A New Activated Resin for Chemical Library Synthesis》.COA of Formula: C13H16N2O The article contains the following contents:

A new tetrafluorophenol activated resin that facilitates the use of 19F NMR to quantitate loading is presented. This new resin provides a useful tool for acylation, and a novel activated polymeric sulfonate ester to generate sulfonamides. This activated resin reacts with a wide scope of N-nucleophiles including primary and secondary amines, and anilines. This new activated resin methodol. provides a powerful tool for pure single-compound library synthesis. In addition to this study using 3-(Piperidin-4-yl)indolin-2-one, there are many other studies that have used 3-(Piperidin-4-yl)indolin-2-one(cas: 72831-89-1COA of Formula: C13H16N2O) was used in this study.

3-(Piperidin-4-yl)indolin-2-one(cas: 72831-89-1) belongs to piperidines. Piperidine derivatives are also used in solid-phase peptide synthesis (SPPS) and many degradation reactions. COA of Formula: C13H16N2O

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Wu, Chun-Feng; Wang, Qing-Chen; Chen, Rui; Zhou, Hai-Ling; Wu, Ting-Ting; Du, Yao; Zhang, Na-Na; Zhang, Hui-Min; Fan, Zu-Yan; Wang, Li-Li; Hu, Chu-Jiao; Sang, Zhi-Pei; Li, Hong-Liang; Wang, Ling; Tang, Lei; Zhang, Ji-Quan published an article on February 5 ,2022. The article was titled 《Synthesis and bioevaluation of diaryl urea derivatives as potential antitumor agents for the treatment of human colorectal cancer》, and you may find the article in European Journal of Medicinal Chemistry.Related Products of 39546-32-2 The information in the text is summarized as follows:

The development of inhibitors targeting the PI3K-Akt-mTOR signaling pathway has been greatly hindered by the on-target AEs, such as hyperglycemia and hepatotoxicities. In this study, a series of diaryl urea derivatives has been designed and synthesized based on clin. candidate gedatolisib, and most of the newly synthesized derivatives showed kinase inhibitory and antiproliferative activities within nanomolar and submicromolar level, resp. The terminal L-proline amide substituted derivative I showed 8.6-fold more potent PI3Kα inhibitory activity (0.7 nM) and 4.6-fold more potent antiproliferative effect against HCT116 cell lines (0.11μM) compared with control gedatolisib. The potential antitumor mechanism and efficacy of I in HCT116 xenograft models have also been evaluated, and found I showed comparable in vivo antitumor activity with gedatolisib. The safety investigations revealed that compound I exhibited more safer profiles in the selectivity of liver cells (selectivity index: >6.6 vs 1.85) and blood glucose regulation than gedatolisib. In addition, the in vitro stability assays also indicated that developed compound I possessed good metabolic stabilities. The experimental process involved the reaction of Piperidine-4-carboxamide(cas: 39546-32-2Related Products of 39546-32-2)

Piperidine-4-carboxamide(cas: 39546-32-2) belongs to anime. Halogenation, in which one or more hydrogen atoms of an amine is replaced by a halogen atom, occurs with chlorine, bromine, and iodine, as well as with some other reagents, notably hypochlorous acid (HClO). With primary amines the reaction proceeds in two stages, producing N-chloro- and N,N-dichloro-amines, RNHCl and RNCl2, respectively. With tertiary amines, an alkyl group may be displaced by a halogen.Related Products of 39546-32-2

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

In 2019,Angewandte Chemie, International Edition included an article by Wu, Jingjing; Baer, Robin M.; Guo, Lin; Noble, Adam; Aggarwal, Varinder K.. Related Products of 109384-19-2. The article was titled 《Photoinduced Deoxygenative Borylations of Aliphatic Alcohols》. The information in the text is summarized as follows:

A photochem. method for converting aliphatic alcs. into boronic esters is described. Preactivation of the alc. as a 2-iodophenyl-thionocarbonate enables a novel Barton-McCombie-type radical deoxygenation that proceeds efficiently with visible light irradiation and without the requirement for a photocatalyst, a radical initiator, or Sn or Si hydrides. The resultant alkyl radical is intercepted by bis(catecholato)diboron, furnishing boronic esters from a diverse range of structurally complex alcs. In the part of experimental materials, we found many familiar compounds, such as tert-Butyl 4-hydroxypiperidine-1-carboxylate(cas: 109384-19-2Related Products 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.Related Products of 109384-19-2

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

In 2019,Bioorganic & Medicinal Chemistry Letters included an article by Wang, Jiming; Zhang, Xiangyu; Yan, Jiangkun; Li, Wei; Jiang, Qinwen; Wang, Xinran; Zhao, Dongmei; Cheng, Maosheng. Electric Literature of C10H19NO3. The article was titled 《Design, synthesis and biological evaluation of curcumin analogues as novel LSD1 inhibitors》. The information in the text is summarized as follows:

Histone lysine-specific demethylase 1 (LSD1) was the first discovered histone demethylase. Inactivating LSD1 or downregulating its expression inhibits cancer-cell development, and thus, it is an attractive mol. target for the development of novel cancer therapeutics. In this study, we worked on the structural optimization of natural products and identified 30 novel LSD1 inhibitors. Utilizing a structure-based drug design strategy, we designed and synthesized a series of curcumin analogs that were shown to be potent LSD1 inhibitors in the enzyme assay. Compound WB07 (I) displayed the most potent LSD1 inhibitory activity, with an IC50 value of 0.8μM. Moreover, WA20 (II) showed an anticlonogenic effect on A549 cells with an IC50 value of 4.4μM. Mol. docking simulations were also carried out, and the results indicated that the inhibitors bound to the protein active site located around the key residues of Asp555 and Asp556. These findings suggested that compounds II and I are the first curcumin analog-based LSD1 inhibitors with remarkable A549 suppressive activity, providing a novel scaffold for the development of LSD1 inhibitors. In the experiment, the researchers used many compounds, for example, tert-Butyl 4-hydroxypiperidine-1-carboxylate(cas: 109384-19-2Electric Literature 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.Electric Literature of C10H19NO3

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

《New access to pyrano[2,3-c]pyrazole-3-carboxylates via domino four-component reaction and their antimicrobial activity》 was written by Maarop, Muhammad Siddiq; Rashid, Fatin Nur Ain Abdul; Mohammat, Mohd Fazli; Shaameri, Zurina; Johari, Saiful Azmi; Isa, Mazurah Mohamed; Low, Anis Muhammad. SDS of cas: 1445-73-4 And the article was included in Indonesian Journal of Chemistry in 2020. The article conveys some information:

A library of some novel classes of pyrano[2,3-c]pyrazole-3-carboxylates I [R = Et, i-Pr, Ph, etc.] was synthesized by employing uncatalyzed domino four-component reaction using diethyloxaloacetate, hydrazine hydrate, aldehydes and malononitrile in refluxing of ethanol-acetic acid solvent systems. Series of domino reactions involving of pyrazolone formation, Michael addition, and Thorpe-Ziegler cyclization reaction managed to produce the cyclized products I from moderate to excellent yield. This protocol provided a reliable, general and salient procedure for the title compound I using a one-pot approach. Preliminary biol. screening unveiled limited potentials of this class of compounds I for antimicrobial lead compound due to its limited solubility properties. The experimental process involved the reaction of 1-Methyl-4-piperidone(cas: 1445-73-4SDS of cas: 1445-73-4)

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.SDS of cas: 1445-73-4

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

《A divergent procedure for multicomponent synthesis of novel ferrocenyl derivatives of dicyanoanilines and cyanopyridines》 was written by Mojtahedi, Mohammad M.; Hosseinkhany, Samaneh; Abaee, M. Saeed; Mesbah, A. Wahid. Quality Control of 1-Methyl-4-piperidone And the article was included in Applied Organometallic Chemistry in 2020. The article conveys some information:

A divergent procedure was developed for multicomponent reaction of ferrocenecarboxaldehyde with malononitrile and various cyclic ketones. Ultrasonic irradiation of 1.0:1.0:2.0 ethanolic mixtures of the reactants produced dicyanoanilines, e.g. I, chemoselectively in high yields, while equimolar mixtures of the same reactants in refluxing EtOH solely resulted in four-component formation of cyanopyridines, e.g. II. Both series of products are obtained directly by spontaneous precipitation in the reaction mixtures avoiding cumbersome and expensive chromatog. separations In the experimental materials used by the author, we found 1-Methyl-4-piperidone(cas: 1445-73-4Quality Control 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.Quality Control of 1-Methyl-4-piperidone

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

《Efficacy and Tolerability of Pyrazolo[1,5-a]pyrimidine RET Kinase Inhibitors for the Treatment of Lung Adenocarcinoma》 was written by Mathison, Casey J. N.; Chianelli, Donatella; Rucker, Paul V.; Nelson, John; Roland, Jason; Huang, Zhihong; Yang, Yang; Jiang, Jiqing; Xie, Yun Feng; Epple, Robert; Bursulaya, Badry; Lee, Christian; Gao, Mu-Yun; Shaffer, Jennifer; Briones, Sergio; Sarkisova, Yelena; Galkin, Anna; Li, Lintong; Li, Nanxin; Li, Chun; Hua, Su; Kasibhatla, Shailaja; Kinyamu-Akunda, Jacqueline; Kikkawa, Rie; Molteni, Valentina; Tellew, John E.. Safety of tert-Butyl 4-hydroxypiperidine-1-carboxylate And the article was included in ACS Medicinal Chemistry Letters in 2020. The article conveys some information:

RET (REarranged during Transfection) kinase gain-of-function aberrancies have been identified as potential oncogenic drivers in lung adenocarcinoma, along with several other cancer types, prompting the discovery and assessment of selective inhibitors. Internal mining and anal. of relevant kinase data informed the decision to investigate a pyrazolo[1,5-a]pyrimidine scaffold, where subsequent optimization led to the identification of compound WF-47-JS03 (1), a potent RET kinase inhibitor with >500-fold selectivity against KDR (Kinase insert Domain Receptor) in cellular assays. In subsequent mouse in vivo studies, compound 1 demonstrated effective brain penetration and was found to induce strong regression of RET-driven tumor xenografts at a well-tolerated dose (10 mg/kg, po, qd). Higher doses of 1, however, were poorly tolerated in mice, similar to other pyrazolo[1,5-a]pyrimidine compounds at or near the efficacious dose, and indicative of the narrow therapeutic windows seen with this scaffold. The experimental part of the paper was very detailed, including the reaction process of 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

Zhang, Minkui; Tang, Li; Jiang, Liu; Wei, Jun; Hu, Yongzhou; Sheng, Rong published their research in European Journal of Medicinal Chemistry in 2021. The article was titled 《Identification of N-phenyl-3-methoxy-4-pyridinones as orally bioavailable H3 receptor antagonists and β-amyloid aggregation inhibitors for the treatment of Alzheimer’s disease》.Name: tert-Butyl 4-hydroxypiperidine-1-carboxylate The article contains the following contents:

Based on our previous work, a series of N-phenyl-3-methoxy-4-pyridinone derivatives were designed as orally bioavailable dual functional agents for therapy of Alzheimer’s disease, through introducing alkyloxy moiety into 4-pyridinone ring to avoid the possible phase II metabolism of 3-hydroxy-4-pyridinone in lead compound 3-hydroxy-2-methyl-1-(4-(3-(pyrrolidin-1-yl)propoxy)phenyl)-pyridin-4(1H)-one (4). In vitro studies indicated that most of these compounds exhibit excellent H3 receptor antagonistic activities and potent self-induced Aβ1-40/Aβ1-42 aggregation inhibitory activities. In particular, 3-methoxy-1-(4-(3-(pyrrolidin-1-yl)propoxy)phenyl)-pyridin-4(1H)-one (7i) demonstrated IC50 value of 0.52 nM in H3R antagonism and good selectivity over other histamine receptor subtypes. The transmission electron microscopy (TEM) images showed that compound 7i can inhibit self-mediated Aβ1-40/Aβ1-42 aggregation efficiently. As expected, it exhibited desirable pharmacokinetic properties in plasma and good BBB permeability. Furthermore, compound 7i can efficiently block (R)-α-methylhistamine- induced dipsogenia and reverse scopolamine-induced learning deficits of rats. All above results indicated that compound 7i was a promising orally bioavailable dual functional agents with potential use in the treatment of Alzheimer’s disease. 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: 109384-19-2Name: tert-Butyl 4-hydroxypiperidine-1-carboxylate) 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.Name: tert-Butyl 4-hydroxypiperidine-1-carboxylate

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Renk, Dana R.; Skraban, Marcel; Bier, Dirk; Schulze, Annette; Wabbals, Erika; Wedekind, Franziska; Neumaier, Felix; Neumaier, Bernd; Holschbach, Marcus published an article in 2021. The article was titled 《Design, synthesis and biological evaluation of Tozadenant analogues as adenosine A2A receptor ligands》, and you may find the article in European Journal of Medicinal Chemistry.Synthetic Route of C10H19NO3 The information in the text is summarized as follows:

With the aim to obtain potent adenosine A2A receptor (A2AR) ligands, a series of eighteen derivatives of 4-hydroxy-N-(4-methoxy-7-morpholin-4-yl-1,3-benzo[d]thiazol-2-yl)-4-methylpiperidine-1-carboxamide were designed and synthesized. The target compounds were obtained by a chem. building block principle that involved reaction of the appropriate aminobenzothiazole Ph carbamates with either com. available or readily synthesized functionalized piperidines. Ki values for human A2AR ranged from 2.4 to 38 nM, with more than 120-fold selectivity over A1 receptors for all evaluated compounds except 4-Fluoro-4-(hydroxymethyl)-N-(4-methoxy-7-morpholinobenzo[d]thiazol-2-yl)piperidine-1-carboxamide which had a Ki of 361 nM and 18-fold selectivity. The most potent fluorine-containing derivatives exhibited Ki values of 4.9 nM, 3.6 nM and 2.8 nM for the human A2AR. Interestingly, the corresponding values for rat A2AR were found to be four to five times higher. Their binding to A2AR was further confirmed by radiolabeling with 18F and in vitro autoradiog. in rat brain slices, which showed almost exclusive striatal binding and complete displacement by the A2AR antagonist ZM 241385. Authors conclude that these compounds represent potential candidates for the visualization of the A2A receptor and open pathways to novel therapeutic treatments of neurodegenerative disorders or cancer. In the experimental materials used by the author, we found 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

Wang, Liujiao; You, Rixin; Ling, Yuxuan; Xie, Yu; Mei, Cenyu; Li, Ziming; Wang, Fanghui published an article in 2021. The article was titled 《Covalent cross-linked anion exchange membrane based on poly(biphenyl piperidine) and poly(styrene-b-(ethylene-co-butylene)-b-styrene): preparation and properties》, and you may find the article in Polymer-Plastics Technology and Materials.Computed Properties of C6H11NO The information in the text is summarized as follows:

Poly(biphenyl piperidine) and polystyrene-b-poly(ethylene-co-butylene)-b-polystyrene were cross-linked to form a polymer backbone, piperidine as the ionic conducting group to improve the chem. stability of the anion exchange membrane. Results indicate that the cross-linked membranes could still retain more than 95% of ion conductivity after being soaked in 1-M KOH solution at 80°C for 800 h, indicating that this cross-linked membrane exhibits good alk. stability. The optimized microphase separation morphol. could promote the ion transport (81.68 mS/cm, 80°C). The cross-linked structure helped to restrain the swelling behavior. The membrane became flexible after crosslinking, which is beneficial to the fuel-cell assembly. In the part of experimental materials, we found many familiar compounds, such as 1-Methyl-4-piperidone(cas: 1445-73-4Computed Properties of C6H11NO)

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.Computed Properties of C6H11NO

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem