Category: 109384-19-2

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

Recommanded Product: 109384-19-2In 2020 ,《Discovery of Bispecific Antagonists of Retinol Binding Protein 4 That Stabilize Transthyretin Tetramers: Scaffolding Hopping, Optimization, and Preclinical Pharmacological Evaluation as a Potential Therapy for Two Common Age-Related Comorbidities》 appeared in Journal of Medicinal Chemistry. The author of the article were Cioffi, Christopher L.; Muthuraman, Parthasarathy; Raja, Arun; Varadi, Andras; Racz, Boglarka; Petrukhin, Konstantin. The article conveys some information:

Accumulation of cytotoxic lipofuscin bisretinoids may contribute to atrophic age-related macular degeneration (AMD) pathogenesis. Retinal bisretinoid synthesis depends on the influx of serum all-trans-retinol delivered via a tertiary retinol binding protein 4 (RBP4)-transthyretin (TTR)-retinol complex. We previously identified selective RBP4 antagonists that dissociate circulating RBP4-TTR-retinol complexes, reduce serum RBP4 levels, and inhibit bisretinoid synthesis in models of enhanced retinal lipofuscinogenesis. However, the release of TTR by selective RBP4 antagonists may be associated with TTR tetramer destabilization and, potentially, TTR amyloid formation. We describe herein the identification of bispecific RBP4 antagonist-TTR tetramer kinetic stabilizers. Standout analog I possesses suitable potency for both targets, significantly lowers mouse plasma RBP4 levels, and prevents TTR aggregation in a gel-based assay. This new class of bispecific compounds may be especially important as a therapy for dry AMD patients who have another common age-related comorbidity, senile systemic amyloidosis, a nongenetic disease associated with wild-type TTR misfolding.tert-Butyl 4-hydroxypiperidine-1-carboxylate(cas: 109384-19-2Recommanded Product: 109384-19-2) 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.Recommanded Product: 109384-19-2

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Antien, Kevin; Geraci, Andrea; Parmentier, Michael; Baudoin, Olivier published their research in Angewandte Chemie, International Edition in 2021. The article was titled 《A New Dioxazolone for the Synthesis of 1,2-Aminoalcohols via Iridium(III)-Catalyzed C(sp3)-H Amidation》.Product Details of 109384-19-2 The article contains the following contents:

Vicinal aminoalcs. are widespread structural motifs in bioactive mols. The development of a new dioxazolone reagent containing a p-nitrophenyldifluoromethyl group, which 1. displays a good safety profile; 2. shows a remarkably high reactivity in the oxime-directed iridium(III)-catalyzed amidation of unactivated C(sp3)-H bonds; 3. leads to amide products which can be hydrolyzed under mild conditions has been reported. The amidation reaction is mild, general and compatible with both primary C-H bonds of tertiary and secondary alcs., as well as secondary C-H bonds of cyclic secondary alcs. This method provides an easy access to free 1,2-aminoalcs. after efficient and mild cleavage of the oxime directing group and activated amide. In the part of experimental materials, we found many familiar compounds, such as tert-Butyl 4-hydroxypiperidine-1-carboxylate(cas: 109384-19-2Product Details 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.Product Details of 109384-19-2

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Yan, Jiangkun; Gu, Yanting; Sun, Yixiang; Zhang, Ziheng; Zhang, Xiangyu; Wang, Xinran; Wu, Tianxiao; Zhao, Dongmei; Cheng, Maosheng published their research in Archiv der Pharmazie (Weinheim, Germany) in 2021. The article was titled 《Design, synthesis, and biological evaluation of 5-aminotetrahydroquinoline-based LSD1 inhibitors acting on Asp375》.Recommanded Product: 109384-19-2 The article contains the following contents:

The abnormal expression of lysine-specific histone demethylase 1 (LSD1) is associated with different cancer types, and LSD1 inhibitory activity seems to have high therapeutic potential in cancer treatment. Here, we report the design, synthesis, and biochem. evaluation of novel 5-aminotetrahydroquinoline-based LSD1 inhibitors such as I. Among them, eight of the compounds showed preferable inhibitory effects on LSD1, with IC50 = 0.19-0.82μM. Several potent compounds were selected to evaluate their antiproliferative activity on A549 cells and MCF-7 cells with a high expression of LSD1. The potential binding modes of the compounds were revealed through mol. docking to rationalize the potency of compounds toward LSD1. Our data recognized that the 5-aminotetrahydroquinoline scaffold may serve as a starting point for developing potent LSD1 inhibitors for cancer therapy. In the experiment, the researchers used tert-Butyl 4-hydroxypiperidine-1-carboxylate(cas: 109384-19-2Recommanded Product: 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.Recommanded Product: 109384-19-2

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Kang, Zhenghui; Chang, Wenju; Tian, Xue; Fu, Xiang; Zhao, Wenxuan; Xu, Xinfang; Liang, Yong; Hu, Wenhao published their research in Journal of the American Chemical Society in 2021. The article was titled 《Ternary Catalysis Enabled Three-Component Asymmetric Allylic Alkylation as a Concise Track to Chiral α,α-Disubstituted Ketones》.Formula: C10H19NO3 The article contains the following contents:

Herein, a three-component asym. allylation of α-diazo carbonyl compounds with alcs. and allyl carbonates was disclosed by employing a ternary cooperative catalysis of achiral Pd-complex, Rh2(OAc)4, and chiral phosphoric acid CPA. This method represents the first example of three-component asym. allylic alkylation through an SN1-type trapping process, which involves a convergent assembly of two active intermediates, Pd-allyl species and enol derived from onium ylides, providing an expeditious access to chiral α,α-disubstituted ketones in good to high yields with high to excellent enantioselectivity. Combined exptl. and computational studies have shed light on the mechanism of this novel three-component reaction, including the critical role of Xantphos ligand and the origin of enantioselectivity. The experimental part of the paper was very detailed, including the reaction process of tert-Butyl 4-hydroxypiperidine-1-carboxylate(cas: 109384-19-2Formula: 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.Formula: C10H19NO3

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Zhai, Wenqiang; Lu, Yongping; Zhu, Yabo; Zhou, Mengguang; Ye, Cheng; Shi, Zheng-Zheng; Qian, Wenjian; Hu, Taishan; Chen, Lei published an article in 2021. The article was titled 《Discovery and optimization of a potent and selective indazolamine series of IRAK4 inhibitors》, and you may find the article in Bioorganic & Medicinal Chemistry Letters.Category: piperidines The information in the text is summarized as follows:

IRAK4 is a key mediator of innate immunity. There is a high interest in identifying novel IRAK4 inhibitors for the treatment of inflammatory autoimmune diseases. We describe here a highly potent and selective IRAK4 inhibitor HS271 (I) that exhibited superior enzymic and cellular activities, as well as excellent pharmacokinetic properties. HS271 displayed robust in vivo anti-inflammatory efficacy as evaluated in rat models of LPS induced TNFα production and collagen-induced arthritis. In the experiment, the researchers used many compounds, for example, tert-Butyl 4-hydroxypiperidine-1-carboxylate(cas: 109384-19-2Category: piperidines)

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.Category: piperidines

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Feng, Baicheng; Dong, Jingjing; Wang, Tielin; Lu, Jianqiang; Jin, Yan published an article in 2021. The article was titled 《Synthesis and characterization of N-(4-(piperidin-4-ylsulfonyl)phenyl)5-vinylpyrimidin-2-amine》, and you may find the article in Indian Journal of Heterocyclic Chemistry.Reference of tert-Butyl 4-hydroxypiperidine-1-carboxylate The information in the text is summarized as follows:

Target product N-(4-(piperidin-4-ylsulfonyl)phenyl)5-vinylpyrimidin-2- amine was synthesized using 6-oxopyran-3-carbaldehyde and 4-hydroxypiperidine as starting materials by a series of nucleophilic substitution and oxidation Different acid-binding agents were discussed to explore the effect on the yield of tert-Bu 4-((4-((5-vinylpyrimidin-2-yl)amino)phenyl)sulfonyl)piperidine-1- carboxylate. The structures of products were characterized by 1H NMR and mass spectra. In the part of experimental materials, we found many familiar compounds, such as tert-Butyl 4-hydroxypiperidine-1-carboxylate(cas: 109384-19-2Reference 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.Reference of tert-Butyl 4-hydroxypiperidine-1-carboxylate

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Zhang, Zhenhua; Gorski, Bartosz; Leonori, Daniele published an article in 2022. The article was titled 《Merging Halogen-Atom Transfer (XAT) and Copper Catalysis for the Modular Suzuki-Miyaura-Type Cross-Coupling of Alkyl Iodides and Organoborons》, and you may find the article in Journal of the American Chemical Society.Application of 109384-19-2 The information in the text is summarized as follows:

A mechanistically distinct approach to achieve Suzuki-Miyaura-type cross-couplings between alkyl iodides and aryl organoborons was reported. This process required a copper catalyst but, in contrast with previous approaches based on palladium and nickel systems, does not utilizes the metal for the activation of the alkyl electrophile. Instead, this strategy exploited the halogen-atom transfer ability of α-aminoalkyl radicals to convert secondary alkyl iodides into the corresponding alkyl radicals that then were coupled with aryl, vinyl, alkynyl, benzyl and allyl boronate species. These novel coupling reactions feature simple set up and conditions (1 h at room temperature) and facilitate access to privileged motifs targeted by the pharmaceutical sector. 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: 109384-19-2Application of 109384-19-2) 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.Application of 109384-19-2

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Sakai, Holt A.; MacMillan, David W. C. published an article in 2022. The article was titled 《Nontraditional Fragment Couplings of Alcohols and Carboxylic Acids: C(sp3)-C(sp3) Cross-Coupling via Radical Sorting》, and you may find the article in Journal of the American Chemical Society.Recommanded Product: 109384-19-2 The information in the text is summarized as follows:

In this report, the C(sp3)-C(sp3) cross-coupling of alcs. and carboxylic acids through the dual combination of N-heterocyclic carbene (NHC)-mediated deoxygenation and hypervalent iodine-mediated decarboxylation were described. This mild and practical Ni-catalyzed radical-coupling protocol was employed to prepare a wide array of alkyl-alkyl cross-coupled products, including highly congested quaternary carbon centers from the corresponding tertiary alcs. or tertiary carboxylic acids. Synthetic applications of this methodol. to alc. C1-alkylation and formal homologation, as well as to the late-stage functionalization of drugs, natural products, and biomols. were demonstrated.tert-Butyl 4-hydroxypiperidine-1-carboxylate(cas: 109384-19-2Recommanded Product: 109384-19-2) 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.Recommanded Product: 109384-19-2

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem