Category: 109384-19-2

Quality Control of tert-Butyl 4-hydroxypiperidine-1-carboxylateIn 2021 ,《Development of autotaxin inhibitors: A series of tetrazole cinnamides》 was published in Bioorganic & Medicinal Chemistry Letters. The article was written by Thomson, Christopher G.; Le Grand, Darren; Dowling, Mark; Beattie, David; Elphick, Lucy; Faller, Michael; Freeman, Mark; Hardaker, Elizabeth; Head, Victoria; Hemmig, Rene; Hill, Johan; Lister, Andrew; Pascoe, David; Rieffel, Sebastien; Shrestha, Binesh; Steward, Oliver; Zink, Florence. The article contains the following contents:

A series of inhibitors of autotaxin (ATX) have been developed from a high throughput screening hit, 1a (I), which shows an alternative binding mode to known catalytic site inhibitors. Selectivity over the hERG channel and microsomal clearance were dependent on the lipophilicity of the compounds, and this was optimized by reduction of clogD while maintaining high affinity ATX inhibition. Compound 15a (II) shows good oral exposure, and concentration dependent inhibition of formation of LPA in vivo, as shown in pharmacokinetic-pharmacodynamic (PK/PD) experimentstert-Butyl 4-hydroxypiperidine-1-carboxylate(cas: 109384-19-2Quality Control of 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.Quality Control of tert-Butyl 4-hydroxypiperidine-1-carboxylate

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

《Diverse functionalization of strong alkyl C-H bonds by undirected borylation》 was published in Science (Washington, DC, United States) in 2020. These research results belong to Oeschger, Raphael; Su, Bo; Yu, Isaac; Ehinger, Christian; Romero, Erik; He, Sam; Hartwig, John. COA of Formula: C10H19NO3 The article mentions the following:

In the presence of a catalyst generated from [Ir(cod)(OMe)]2 and 2-methyl-1,10-phenanthroline, alkanes (including alcs., ethers, and protected amines) and cycloalkanes, cyclic ethers, and protected nitrogen heterocycles underwent undirected and regioselective borylation with B2(pin)2 (at primary C-H bonds in alkanes with unblocked primary C-H bonds, at secondary C-H bonds in cycloalkanes, and at secondary bonds β to heteroatoms in cyclic ethers and nitrogen heterocycles) in cyclooctane to yield alkyl, cycloalkyl, and heterocyclyl boronates. The product boronates were used in a variety of post-functionalization reactions; the method allows functionalization of organic mols. at positions inaccessible by previous methods. The mechanism and kinetics of the borylation was studied through kinetic isotope effect experiments using deuterated substrates and partially deuterated methylphenanthrolines and by determination of the kinetics of borylation of various substrates using 1,10-phenanthroline ligands. The results came from multiple reactions, including the reaction of tert-Butyl 4-hydroxypiperidine-1-carboxylate(cas: 109384-19-2COA of Formula: 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.COA of Formula: C10H19NO3

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Bessieres, Maxime; Plebanek, Elzbieta; Chatterjee, Payel; Shrivastava-Ranjan, Punya; Flint, Mike; Spiropoulou, Christina F.; Warszycki, Dawid; Bojarski, Andrzej J.; Roy, Vincent; Agrofoglio, Luigi A. published an article in 2021. The article was titled 《Design, synthesis and biological evaluation of 2-substituted-6-[(4-substituted-1-piperidyl)methyl]-1H-benzimidazoles as inhibitors of ebola virus infection》, and you may find the article in European Journal of Medicinal Chemistry.Recommanded Product: tert-Butyl 4-hydroxypiperidine-1-carboxylate The information in the text is summarized as follows:

Novel 2-substituted-6-[(4-substituted-1-piperidyl)methyl]-1H-benzimidazoles were designed and synthesized as Ebola virus inhibitors. The proposed structures of the new prepared benzimidazole-piperidine hybrids were confirmed based on their spectral data and CHN analyses. The target compounds were screened in vitro for their anti-Ebola activity. Among tested mols., compounds 26a (EC50 = 0.93μM, SI = 10) and 25a (EC50 = 0.64μM, SI = 20) were as potent as and more selective than Toremifene reference drug (EC50 = 0.38μM, SI = 7) against cell line. Probably the mechanism by which 25a and 26a block EBOV infection is through the inhibition of viral entry at the level of NPC1. Also, a docking study revealed that several of the NPC1 amino acids that participate in binding to GP are involved in the binding of the most active compounds 25a and 26a. Finally, in silico ADME prediction indicates that 26a is an idealy drug-like candidate. The authors’ results could enable the development of small mol. drug capable of inhibiting Ebola virus, especially at the viral entry step. In the experiment, the researchers used tert-Butyl 4-hydroxypiperidine-1-carboxylate(cas: 109384-19-2Recommanded Product: 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.Recommanded Product: tert-Butyl 4-hydroxypiperidine-1-carboxylate

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

In 2022,Yen-Pon, Expedite; Li, Longbo; Levitre, Guillaume; Majhi, Jadab; McClain, Edward J.; Voight, Eric A.; Crane, Erika A.; Molander, Gary A. published an article in Journal of the American Chemical Society. The title of the article was 《On-DNA Hydroalkylation to Introduce Diverse Bicyclo[1.1.1]pentanes and Abundant Alkyls via Halogen Atom Transfer》.Name: tert-Butyl 4-hydroxypiperidine-1-carboxylate The author mentioned the following in the article:

A Giese addition to install highly functionalized bicyclo[1.1.1]pentanes (BCPs) using tricyclo[1.1.1.01,3]pentane (TCP) as a radical linchpin, as well as other diverse alkyl groups, on-DNA from the corresponding organohalides as non-stabilized radical precursors was reported. Telescoped procedures allow extension of the substrate pool by at least an order of magnitude to ubiquitous alcs. and carboxylic acids, allowing us to “”upcycle”” these abundant feedstocks to afford non-traditional libraries with different physicochem. properties for the small-mol. products (i.e., non-peptide libraries with acids). This approach is amenable to library production, as a DNA damage assessment revealed good PCR amplifiability and only 6% mutated sequences for a full-length DNA tag. 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

In 2022,Nakagawa, Masanari; Matsuki, Yuki; Nagao, Kazunori; Ohmiya, Hirohisa published an article in Journal of the American Chemical Society. The title of the article was 《A Triple Photoredox/Cobalt/Bronsted Acid Catalysis Enabling Markovnikov Hydroalkoxylation of Unactivated Alkenes》.Application of 109384-19-2 The author mentioned the following in the article:

Authors demonstrate Markovnikov hydroalkoxylation of unactivated alkenes using alcs. through a triple catalysis consisting of photoredox, cobalt, and Bronsted acid catalysts under visible light irradiation The triple catalysis realizes three key elementary steps in a single catalytic cycle: (1) Co(III) hydride generation by photochem. reduction of Co(II) followed by protonation, (2) metal hydride hydrogen atom transfer (MHAT) of alkenes by Co(III) hydride, and (3) oxidation of the alkyl Co(III) complex to alkyl Co(IV). The precise control of protons and electrons by the three catalysts allows the elimination of strong acids and external reductants/oxidants that are required in the conventional methods. After reading the article, we found that the author 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

The author of 《One-pot synthesis of novel tert-butyl-4-substituted phenyl-1H-1,2,3-triazolo piperazine/piperidine carboxylates, potential GPR119 agonists》 were Bashetti, Nagaraju; Shanmukha Kumar, J. V.; Seelam, Naresh Varma; Prasanna, B.; Mintz, Akiva; Damuka, Naresh; Devanathan, Sriram; Solingapuram Sai, Kiran Kumar. And the article was published in Bioorganic & Medicinal Chemistry Letters in 2019. Reference of tert-Butyl 4-hydroxypiperidine-1-carboxylate The author mentioned the following in the article:

We have synthesized a new series of 1,2,3-triazolo piperazine and piperidine carboxylate derivatives using a simple and one-pot click chem. with significantly reduced reaction times (∼5 min) and enhanced reaction yields (∼95-98%). The fourteen novel compounds thus synthesized were tested for ability to target GPR119, a G-protein coupled target receptor that plays critical role in regulation of type-2 diabetes mellitus. Four analogs demonstrated similar or better EC50 values over previously reported AR231453 activity towards GPR119. The experimental process involved the reaction of 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

The author of 《An optimised series of substituted N-phenylpyrrolamides as DNA gyrase B inhibitors》 were Tiz, Davide Benedetto; Skok, Ziga; Durcik, Martina; Tomasic, Tihomir; Masic, Lucija Peterlin; Ilas, Janez; Zega, Anamarija; Draskovits, Gabor; Revesz, Tamas; Nyerges, Akos; Pal, Csaba; Cruz, Cristina D.; Tammela, Paivi; Zigon, Dusan; Kikelj, Danijel; Zidar, Nace. And the article was published in European Journal of Medicinal Chemistry in 2019. Application of 109384-19-2 The author mentioned the following in the article:

ATP competitive inhibitors of DNA gyrase and topoisomerase IV have great therapeutic potential, but none of the described synthetic compounds has so far reached the market. To optimize the activities and physicochem. properties of the authors’ previously reported N-phenylpyrrolamide inhibitors, the authors have synthesized an improved, chem. variegated selection of compounds and evaluated them against DNA gyrase and topoisomerase IV enzymes, and against selected Gram-pos. and Gram-neg. bacteria. The most potent compound displayed IC50 values of 6.9 nM against Escherichia coli DNA gyrase and 960 nM against Staphylococcus aureus topoisomerase IV. Several compounds displayed min. inhibitory concentrations (MICs) against Gram-pos. strains in the 1-50 μM range, one of which inhibited the growth of Enterococcus faecalis, Enterococcus faecium, S. aureus and Streptococcus pyogenes with MIC values of 1.56 μM, 1.56 μM, 0.78 μM and 0.72 μM, resp. This compound has been investigated further on methicillin-resistant S. aureus (MRSA) and on ciprofloxacin non-susceptible and extremely drug resistant strain of S. aureus (MRSA VISA). It exhibited the MIC value of 2.5 μM on both strains, and MIC value of 32 μM against MRSA in the presence of inactivated human blood serum. Further studies are needed to confirm its mode of action. The results came from multiple reactions, including the reaction of 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

Reference of tert-Butyl 4-hydroxypiperidine-1-carboxylateIn 2021 ,《A knowledge-based, structural-aided discovery of a novel class of 2-phenylimidazo[1,2-a]pyridine-6-carboxamide H-PGDS inhibitors》 was published in Bioorganic & Medicinal Chemistry Letters. The article was written by Schulte, Christie A.; Deaton, David N.; Diaz, Elsie; Do, Young; Gampe, Robert T.; Guss, Jeffrey H.; Hancock, Ashley P.; Hobbs, Heather; Hodgson, Simon T.; Holt, Jason; Jeune, Michael R.; Kahler, Kirsten M.; Kramer, H. Fritz; Le, Joelle; Mortenson, Paul N.; Musetti, Caterina; Nolte, Robert T.; Orband-Miller, Lisa A.; Peckham, Gregory E.; Petrov, Kim G.; Pietrak, Beth L.; Poole, Chuck; Price, Daniel J.; Saxty, Gordon; Shillings, Anthony; Smalley, Terrence L. Jr.; Somers, Don O.; Stewart, Eugene L.; Stuart, J. Darren; Thomson, Stephen A.. The article contains the following contents:

A knowledge-based, structural-aided discovery of a novel class of 1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine and 2-phenylimidazo[1,2-a]pyridine-6-carboxamide H-PGDS inhibitors was described. 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: 109384-19-2Reference of 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.Reference of tert-Butyl 4-hydroxypiperidine-1-carboxylate

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

In 2022,Tolentino, Kirsten T.; Mashinson, Viktoriya; Vadukoot, Anish K.; Hopkins, Corey R. published an article in Bioorganic & Medicinal Chemistry Letters. The title of the article was 《Discovery and characterization of benzyloxy piperidine based dopamine 4 receptor antagonists》.Application of 109384-19-2 The author mentioned the following in the article:

The dopamine receptor 4 (D4R) is highly expressed in both motor, associative and limbic subdivisions of the cortico-basal ganglia network. Due to the distribution in the brain, there is mounting evidence pointing to a role for the D4R in the modulation of this network and its subsequent involvement in L-DOPA induced dyskinesias in Parkinson′s disease. As part of our continued effort in the discovery of novel D4R antagonists, we report the discovery and characterization of a new 3- or 4-benzyloxypiperidine scaffold as D4R antagonists. We report several D4R selective compounds (>30-fold vs. other dopamine receptor subtypes) with improved in vitro and in vivo stability over previously reported D4R antagonists.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

Related Products of 109384-19-2In 2021 ,《Polyplex-Loaded Hydrogels for Local Gene Delivery to Human Dermal Fibroblasts》 appeared in ACS Biomaterials Science & Engineering. The author of the article were Duran-Mota, Jose Antonio; Yani, Julia Quintanas; Almquist, Benjamin D.; Borros, Salvador; Oliva, Nuria. The article conveys some information:

Impaired cutaneous healing leading to chronic wounds affects between 2 and 6% of the total population in most developed countries and it places a substantial burden on healthcare budgets. Current treatments involving antibiotic dressings and mech. debridement are often not effective, causing severe pain, emotional distress, and social isolation in patients for years or even decades, ultimately resulting in limb amputation. Alternatively, gene therapy (such as mRNA therapies) has emerged as a viable option to promote wound healing through modulation of gene expression. However, protecting the genetic cargo from degradation and efficient transfection into primary cells remain significant challenges in the push to clin. translation. Another limiting aspect of current therapies is the lack of sustained release of drugs to match the therapeutic window. Herein, we have developed an injectable, biodegradable and cytocompatible hydrogel-based wound dressing that delivers poly(β-amino ester)s (pBAEs) nanoparticles in a sustained manner over a range of therapeutic windows. We also demonstrate that pBAE nanoparticles, successfully used in previous in vivo studies, protect the mRNA load and efficiently transfect human dermal fibroblasts upon sustained release from the hydrogel wound dressing. This prototype wound dressing technol. can enable the development of novel gene therapies for the treatment of chronic wounds. 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