Month: October 2022

On April 3, 2020, Min, Qing-Qiang; Yang, Jia-Wen; Pang, Meng-Juan; Ao, Gui-Zhen; Liu, Feng published an article.Electric Literature of 39512-49-7 The title of the article was Copper-Catalyzed Remote C(sp3)-H Amination of Carboxamides. And the article contained the following:

Here we report a method for the site-selective intermol. C(sp3)-H amination of carboxamides by merging transition-metal catalysis and the hydrogen atom transfer strategy. The reaction proceeds through a sequence of favorable single-electron transfer, 1,5-hydrogen atom transfer, and C-N cross-coupling steps, thus allowing access to a series of desired products. This reaction could accommodate a wide diversity of nitrogen nucleophiles as well as demonstrate excellent chemoselectivity and functional group compatibility. The experimental process involved the reaction of 4-(4-Chlorophenyl)piperidin-4-ol(cas: 39512-49-7).Electric Literature of 39512-49-7

The Article related to intermol amination carboxamide metal catalysis hydrogen atom transfer, Benzene, Its Derivatives, and Condensed Benzenoid Compounds: Amides, Amidines, Imidic Esters, Hydrazides, and Hydrazonic Esters and other aspects.Electric Literature of 39512-49-7

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Kralj, Ana; Kurt, Elif; Tschammer, Nuska; Heinrich, Markus R. published an article in 2014, the title of the article was Synthesis and Biological Evaluation of Biphenyl Amides That Modulate the US28 Receptor.Recommanded Product: 4-(4-Chlorophenyl)piperidin-4-ol And the article contains the following content:

To prepare and biol. evaluate 38 new potential US28 allosteric modulators were designed and the synthesis of the target compounds was achieved by the authors by a straightforward synthetic route involving a radical arylation. The study was based on a former lead structure but with the dihydroisoquinolinone moiety replaced by substituted biphenyl compounds The investigation of structure-activity relationships among the new biphenyl-derived ligands led to a preliminary pharmacophore model and the discovery of four promising candidates with full inverse agonist properties. The title compounds thus formed included a decanamide derivative (I) and related substances. The experimental process involved the reaction of 4-(4-Chlorophenyl)piperidin-4-ol(cas: 39512-49-7).Recommanded Product: 4-(4-Chlorophenyl)piperidin-4-ol

The Article related to biaryl biphenyl amide preparation antiviral agent viral infection, us28 receptor, amides, biphenyls, human cytomegalovirus, inverse agonism, Benzene, Its Derivatives, and Condensed Benzenoid Compounds: Amides, Amidines, Imidic Esters, Hydrazides, and Hydrazonic Esters and other aspects.Recommanded Product: 4-(4-Chlorophenyl)piperidin-4-ol

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On October 29, 2020, Scully, Stephen S.; Laplaca, Derek; Pelly, Rachel; Parmar, Rubina Giare; Maetani, Micah published a patent.Application of 357935-97-8 The title of the patent was Preparation of ionizable amine lipids and lipid nanoparticles. And the patent contained the following:

Ionizable amine lipids of formula I [X1 = O, (substituted) NH, bond; X2 = alkylene; X3 = CO, bond; R1 = H, Me; R2, R3 = alkyl; R2X2N = heterocyclyl; R2R3N = heterocyclyl; Y1 = alkylene; Y2 = CH2CH=CH, CO-OCH2CH=CH, CO-O; n = 0-3; R4 = alkyl; Z1 = alkylene, bond; Z2 = CO-O, absent; R5, R6 = alkyl, alkoxy; W = methylene, bond; R7 = H, Me] are prepared which are useful for the delivery of biol. active agents, for example delivering biol. active agents to cells to prepare engineered cells. The ionizable amine lipids disclosed herein are useful as ionizable lipids in the formulation of lipid nanoparticle-based compositions Thus, II was prepared, and had editing efficiency of 23.74% at 0.1 mg/kg, 58.48% at 0.3 mg/kg and 73.6% at 1 mg/kg in mice liver. The experimental process involved the reaction of 1-Ethylpiperidin-4-amine dihydrochloride(cas: 357935-97-8).Application of 357935-97-8

The Article related to lipid nanoparticle ionizable amine lipid preparation, Biomolecules and Their Synthetic Analogs: Prostaglandins and Other Arachidonic Acid Cascade Substances, Thromboxanes, Fatty Acids and other aspects.Application of 357935-97-8

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On September 2, 2016, Zhang, Wen; Wang, Fei; McCann, Scott D.; Wang, Dinghai; Chen, Pinhong; Stahl, Shannon S.; Liu, Guosheng published an article.Electric Literature of 39512-49-7 The title of the article was Enantioselective cyanation of benzylic C-H bonds via copper-catalyzed radical relay. And the article contained the following:

Direct methods for stereoselective functionalization of sp3-hybridized carbon-hydrogen [C(sp3)-H] bonds in complex organic mols. could facilitate much more efficient preparation of therapeutics and agrochems. Here, we report a copper-catalyzed radical relay pathway for enantioselective conversion of benzylic C-H bonds into benzylic nitriles. Hydrogen-atom abstraction affords an achiral benzylic radical that undergoes asym. C(sp3)-CN bond formation upon reaction with a chiral copper catalyst. The reactions proceed efficiently at room temperature with the benzylic substrate as limiting reagent, exhibit broad substrate scope with high enantioselectivity (typically 90 to 99% enantiomeric excess), and afford products that are key precursors to important bioactive mols. Mechanistic studies provide evidence for diffusible organic radicals and highlight the difference between these reactions and C-H oxidations mediated by enzymes and other catalysts that operate via radical rebound pathways. The experimental process involved the reaction of 4-(4-Chlorophenyl)piperidin-4-ol(cas: 39512-49-7).Electric Literature of 39512-49-7

The Article related to enantioselective cyanation benzylic carbon copper catalyzed radical relay, Physical Organic Chemistry: Stereochemistry and Stereochemical Relationships, Including Conformational Inversions and Rotational Isomerization and other aspects.Electric Literature of 39512-49-7

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On June 30, 2013, Razavi, Seyyede Faeze; Khoobi, Mehdi; Nadri, Hamid; Sakhteman, Amirhossein; Moradi, Alireza; Emami, Saeed; Foroumadi, Alireza; Shafiee, Abbas published an article.HPLC of Formula: 39512-49-7 The title of the article was Synthesis and evaluation of 4-substituted coumarins as novel acetylcholinesterase inhibitors. And the article contained the following:

A series of 4-hydroxycoumarin derivatives were designed and synthesized as new acetylcholinesterase (AChE) inhibitors which could be considered for Alzheimer’s disease therapeutics. Among the 19 coumarin-derived compounds tested toward Electrophorus electricus acetylcholinesterase (eelAChE) and horse serum butyrylcholinesterase (eqBChE), N-(1-benzylpiperidin-4-yl)acetamide derivative I displayed highest AChE inhibitory activity (IC50 = 1.2 μM) and good selectivity (37 times). The docking study of the most potent compound I, indicated that Phe330 is responsible for ligand recognition and trafficking by forming π-cation interaction with benzylpiperidine moiety. Furthermore, the formation of an addnl. π-π interaction between coumarin moiety and Trp279 of peripheral anionic site could stabilize the ligand in the active site resulting in more potent inhibition of the enzyme. The experimental process involved the reaction of 4-(4-Chlorophenyl)piperidin-4-ol(cas: 39512-49-7).HPLC of Formula: 39512-49-7

The Article related to coumarin preparation acetylcholinesterase inhibitor, Heterocyclic Compounds (One Hetero Atom): Benzopyrans (Including Coumarins, Isocoumarins, Chromones, Benzopyrones, Dibenzopyrans, and Other Arenopyrans) and other aspects.HPLC of Formula: 39512-49-7

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On January 14, 2003, Thorsett, Eugene D.; Porter, Warren J.; Nissen, Jeffrey S.; Latimer, Lee H.; Audia, James E.; Droste, James published a patent.Product Details of 1055049-80-3 The title of the patent was Preparation of heterocyclic compounds and their use for inhibiting β-amyloid peptide release. And the patent contained the following:

Disclosed are modified heterocyclic di- and tripeptide analogs which inhibit β-amyloid peptide release and/or its synthesis and, accordingly, have utility in treating Alzheimer’s disease. Compounds of formula R1NHCHR2(CONHCHR6)pCONHCHR5C(:NR4)R4 [R1 = H or acyl; R2, R5, R6 = (un)substituted alk(en)(yn)yl, cycloalkyl, (hetero)aryl, heterocyclyl; p = 0 or 1; R3and R4 combine to form a heterocyclic ring, which may be substituted] are claimed. Also disclosed are pharmaceutical compositions comprising a compound which inhibits β-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer’s disease both prophylactically and therapeutically with such pharmaceutical compositions Title compounds, e.g. I, were prepared in a multistep synthesis and inhibited β-amyloid peptide production by at least 30% as compared to control. The experimental process involved the reaction of (S)-tert-Butyl (2-oxopiperidin-4-yl)carbamate(cas: 1055049-80-3).Product Details of 1055049-80-3

The Article related to heterocyclic peptide preparation inhibitor amyloid release, alzheimer treatment heterocyclic compound preparation, amyloid peptide release inhibitor heterocyclic compound and other aspects.Product Details of 1055049-80-3

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On September 3, 1998, Thorsett, Eugene D.; Porter, Warren J.; Nissen, Jeffrey S.; Latimer, Lee H.; Audia, James E.; Droste, James J. published a patent.COA of Formula: C10H18N2O3 The title of the patent was Preparation of heterocyclic compounds and their use for inhibiting β-amyloid peptide release. And the patent contained the following:

Disclosed are modified heterocyclic di- and tripeptide analogs which inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer’s disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits β-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer’s disease both prophylactically and therapeutically with such pharmaceutical compositions Title compounds, e.g. I, were prepared in a multistep synthesis and inhibited β-amyloid peptide production by at least 30% as compared to control. The experimental process involved the reaction of (S)-tert-Butyl (2-oxopiperidin-4-yl)carbamate(cas: 1055049-80-3).COA of Formula: C10H18N2O3

The Article related to heterocyclic peptide preparation inhibitor amyloid release, alzheimer treatment heterocyclic compound preparation, amyloid peptide release inhibitor heterocyclic compound and other aspects.COA of Formula: C10H18N2O3

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On February 6, 2014, Takayama, Tetsuo; Shibata, Tsuyoshi; Shiozawa, Fumiyasu; Kawabe, Kenichi; Shimizu, Yuki; Hamada, Makoto; Hiratate, Akira; Takahashi, Masato; Ushiyama, Fumihito; Oi, Takahiro; Shirasaki, Yoshihisa; Matsuda, Daisuke; Koizumi, Chie; Kato, Sota published a patent.HPLC of Formula: 362703-57-9 The title of the patent was Preparation of partially saturated nitrogen-containing heterocyclic compounds, and PHD2 inhibitors, EPO formation promoters, and antianemic agents containing the heterocyclic compounds. And the patent contained the following:

Provided is a compound which is represented by general formula (I) and has an excellent PHD2-inhibiting activity or a pharmaceutically acceptable salt thereof. (In the general formula (I), W, Y, R2, R3, R4 and Y4 are as defined in the description.). Thus, N-[[4-hydroxy-2-oxo-1-[[4′-(trifluoromethyl)biphenyl-4-yl]methyl]-9-oxa-1-azaspiro[5.5]undeca-3-en-3-yl]carbonyl]glycine (preparation given) at 1 μM inhibited 78% human PHD2 activity in NM_022051-expressing insect HighFive cells. The experimental process involved the reaction of tert-Butyl 4-amino-4-(2-methoxy-2-oxoethyl)piperidine-1-carboxylate(cas: 362703-57-9).HPLC of Formula: 362703-57-9

The Article related to preparation heterocycle phd2 inhibitor epo formation promoter antianemic, oxaazaspiroundecaenylcarbonylglycine preparation phd2 inhibitor epo formation promoter antianemic and other aspects.HPLC of Formula: 362703-57-9

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On March 12, 2021, Yang, Wanzhen; Tu, Jie; Ji, Changjin; Li, Zhuang; Han, Guiyan; Liu, Na; Li, Jian; Sheng, Chunquan published an article.Application In Synthesis of 4-(4-Chlorophenyl)piperidin-4-ol The title of the article was Discovery of Piperidol Derivatives for Combinational Treatment of Azole-Resistant Candidiasis. And the article contained the following:

Effective strategies are needed to deal with invasive fungal infections caused by drug-resistant fungi. Previously, we designed a series of antifungal benzocyclane derivatives based on the drug repurposing of haloperidol. Herein, further structural optimization and antifungal mechanism studies were performed, leading to the discovery of new piperidol derivative B2 (I) with improved synergistic antifungal potency, selectivity, and water solubility In particular, the combination of compound B2 and fluconazole showed potent in vitro and in vivo antifungal activity against azole-resistant Candida albicans. Compound B2 inhibited important virulence factors by regulating virulence-associated genes and improved the efficacy of fluconazole by down-regulating the CYP51-coding gene and efflux pump gene. Taken together, the piperidol derivative B2 represents a promising lead compound for the combinational treatment of azole-resistant candidiasis. The experimental process involved the reaction of 4-(4-Chlorophenyl)piperidin-4-ol(cas: 39512-49-7).Application In Synthesis of 4-(4-Chlorophenyl)piperidin-4-ol

The Article related to antifungal candida drug resistance virulence factor candidiasis piperidol derivative, candida albicans, antifungal, drug resistance, piperidol derivatives, virulence factors and other aspects.Application In Synthesis of 4-(4-Chlorophenyl)piperidin-4-ol

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Aguilar Troyano, Francisco Jose; Ballaschk, Frederic; Jaschinski, Marcel; Oezkaya, Yasemin; Gomez-Suarez, Adrian published an article in 2019, the title of the article was Light-Mediated Formal Radical Deoxyfluorination of Tertiary Alcohols through Selective Single-Electron Oxidation with TEDA2+..Name: 4-(4-Chlorophenyl)piperidin-4-ol And the article contains the following content:

The synthesis of tertiary alkyl fluorides through a formal radical deoxyfluorination process was described. This light-mediated, catalyst-free methodol. was fast and broadly applicable allowing for the preparation of C-F bonds from (hetero)benzylic, propargylic and non-activated tertiary alc. derivatives Preliminary mechanistic studies supported that the key step of the reaction is the single-electron oxidation of cesium oxalates-which are readily available from the corresponding tertiary alcs.-with in situ generated TEDA2+ (TEDA: N-(chloromethyl)triethylenediamine), a radical cation derived from Selectfluor. The experimental process involved the reaction of 4-(4-Chlorophenyl)piperidin-4-ol(cas: 39512-49-7).Name: 4-(4-Chlorophenyl)piperidin-4-ol

The Article related to alc tertiary selectfluor photochem radical deoxyfluorination, tertiary alkyl fluoride preparation, fluorination, mechanistic studies, organic synthesis, photochemistry, radicals and other aspects.Name: 4-(4-Chlorophenyl)piperidin-4-ol

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem