Heterocyclic Building Blocks-piperidine

On May 1, 2019, Verheyen, Thomas; van Turnhout, Lars; Vandavasi, Jaya Kishore; Isbrandt, Eric S.; De Borggraeve, Wim M.; Newman, Stephen G. published an article.SDS of cas: 39512-49-7 The title of the article was Ketone Synthesis by a Nickel-Catalyzed Dehydrogenative Cross-Coupling of Primary Alcohols. And the article contained the following:

In the presence of Ni(cod)2 or Ni(OTf)2 and Triphos [MeC(CH2PPh2)3], aryl triflates underwent chemoselective dehydrogenative coupling reactions with primary alkyl and benzylic alcs. using acetone as a hydrogen acceptor to yield ketones. Nonracemic 2-methyl-1-butanol underwent cross-coupling to yield a nonracemic alkyl aryl ketone in 91:9 er. This oxidative transformation is proposed to occur by generation of aldehydes from primary alcs. in situ by either hydrogen transfer oxidation or (pseudo)dehalogenation pathways followed by Ni-catalyzed carbonyl-Heck reaction to form the ketone product. The experimental process involved the reaction of 4-(4-Chlorophenyl)piperidin-4-ol(cas: 39512-49-7).SDS of cas: 39512-49-7

The Article related to aryl ketone chemoselective preparation, nickel catalyst chemoselective dehydrogenative coupling aryl triflate primary alc, Benzene, Its Derivatives, and Condensed Benzenoid Compounds: Ketones and Derivatives, Including Quinones and Sulfur Analogs and other aspects.SDS of cas: 39512-49-7

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On March 7, 2014, Leyva-Perez, Antonio; Cabrero-Antonino, Jose R.; Rubio-Marques, Paula; Al-Resayes, Saud I.; Corma, Avelino published an article.Related Products of 39512-49-7 The title of the article was Synthesis of the ortho/meta/para Isomers of Relevant Pharmaceutical Compounds by Coupling a Sonogashira Reaction with a Regioselective Hydration. And the article contained the following:

Aryl ketones substituted in ortho, meta, and para position are prepared by a palladium-catalyzed Sonogashira reaction followed by a regioselective hydration of the so-formed alkyne with triflimidic acid or a gold catalyst, under catalytic conditions. This methodol. opens a way to obtain substituted aryl alkyl ketones from readily available starting materials, haloarenes, and terminal alkynes. The syntheses of the different regioisomers of haloperidol, melperone, pipamperone, and ibuprofen are presented. Structure-activity relationships for these compounds are studied with dopaminergic and cyclooxygenase binding assays. The experimental process involved the reaction of 4-(4-Chlorophenyl)piperidin-4-ol(cas: 39512-49-7).Related Products of 39512-49-7

The Article related to haloarene terminal alkyne sonogashira regioselective hydration, aryl ketone preparation dopaminergic receptor cyclooxygenase binding, Benzene, Its Derivatives, and Condensed Benzenoid Compounds: Ketones and Derivatives, Including Quinones and Sulfur Analogs and other aspects.Related Products of 39512-49-7

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

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