Tag: 200-300

On October 8, 2009, Chang, Edcon; Duong, Tracy; Hirano, Takehiro; Mcneill, Matthew H.; Terao, Yoshito; Vassar, Angie published a patent.Category: piperidines The title of the patent was Preparation of pyrazolo[1,5-a]pyrimidine derivatives as apoptosis signal-regulating kinase 1 inhibitors. And the patent contained the following:

The invention is related to the preparation of pyrazolo[1,5-a]pyrimidines I [R1 = H, OH, (un)substituted aryloxy, sulfonylalkyl, heteroaryl, etc.; R2 = NO2, CN, (un)substituted haloalkyl, heterobicycloalkyl, aryl, etc.; provided that R2 is not an unsubstituted n-(C1-3)alkyl; R3 = H, halo, NH2, (un)substituted azaalkyl, heteroarylalkyl, etc.] and their pharmaceutically acceptable salts as inhibitors of apoptosis signal-regulating kinase 1 (ASK1) and to their pharmaceutical compositions containing them. Thus, cyclization of 5-methyl-1H-pyrazol-3-amine with Et 3-ethoxy-3-iminopropionate hydrochloride, treatment of 5-amino-2-methylpyrazolo[1,5-a]pyrimidin-7(4H)-one with POCl3 at 95-105°, conversion of phosphorylated intermediate (no data) to 7-chloro-2-methylpyrazolo[1,5-a]pyrimidin-5-amine, acylation of the amine with 4-tert-butylbenzoyl chloride and Pd-coupling of the chloride with [3-(hydroxymethyl)phenyl]boronic acid gave pyrazolopyrimidine II. The enzyme activity of selected I against ASK1 was determined in a scintillation assay. The experimental process involved the reaction of 4-Benzenesulfonylpiperidine Hydrochloride(cas: 1172500-91-2).Category: piperidines

The Article related to pyrazolopyrimidine preparation apoptosis signal regulating kinase 1 inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Category: piperidines

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On January 31, 1986, Nemeryuk, Michal P.; Sedov, Andrej L.; Safonova, Tamara S.; Cerny, Antonin; Krepelka, Jiri published an article.Category: piperidines The title of the article was Transformations of substituted 5-aminopyrimidines under conditions of diazotization. And the article contained the following:

Diazotization of aminopyrimidines I (R = H; R1 = SMe, SCH2Ph, OMe, H, OH; R2 = OMe, Cl, OH, etc.) gave triazoles II (R3 = CO2Me, COSMe, COSCH2Ph, CONH2, etc.). Under similar conditions diaminopyrimidines I [R = NH2, R1 = SCH2C6H4R4-4 (R4 = NO2, CO2Et, CONHCHMe2, H), R2 = Me] gave pyrimidotriazine N-oxides III. The experimental process involved the reaction of 4-Chloro-6-(piperidin-1-yl)pyrimidin-5-amine(cas: 84762-70-9).Category: piperidines

The Article related to aminopyrimidine diazotization, triazole, pyrimidotriazine oxide alkylthio, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Category: piperidines

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 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

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 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

Wang, Kaikai; Zeng, Rong published an article in 2022, the title of the article was Photoinduced Fe-catalyzed bromination and iodination of unstrained cyclic alcohols.Computed Properties of 39512-49-7 And the article contains the following content:

A photoinduced iron catalysis for the efficient C-C bond cleavage and bromination or iodination of unstrained tertiary cycloalkanols, e.g., 8-phenyl-1,4-Dioxaspiro[4.5]decan-8-ol with NBS/NIS was described. The reaction features good functional group tolerance and high yields under mild conditions and provides a powerful tool for the preparation of remote halogenated alkyl ketones, e.g., 3-[2-(2-bromoethyl)-1,3-dioxolan-2-yl]-1-phenyl-1-propanone. The products can be converted via nucleophilic substitution or cross-coupling to other valuable mols., such as haloperidol, fluanisone, and azabuperone, demonstrating the synthetic value of this reaction. The experimental process involved the reaction of 4-(4-Chlorophenyl)piperidin-4-ol(cas: 39512-49-7).Computed Properties of 39512-49-7

The Article related to halo alkyl ketone preparation, cyclic alc iodosuccinimide bromosuccinimide halogenation iron photocatalyst, Benzene, Its Derivatives, and Condensed Benzenoid Compounds: Ketones and Derivatives, Including Quinones and Sulfur Analogs and other aspects.Computed Properties of 39512-49-7

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On July 17, 2020, Wang, Lu; Wang, Ting; Cheng, Gui-Juan; Li, Xiaobao; Wei, Jun-Jie; Guo, Bin; Zheng, Caijuan; Chen, Guangying; Ran, Chongzhao; Zheng, Chao published an article.Category: piperidines The title of the article was Direct C-H Arylation of Aldehydes by Merging Photocatalyzed Hydrogen Atom Transfer with Palladium Catalysis. And the article contained the following:

Herein, we report that merging palladium catalysis with hydrogen atom transfer (HAT) photocatalysis enabled direct arylations and alkenylations of aldehyde C-H bonds, facilitating visible light-catalyzed construction of a variety of ketones. Tetrabutylammonium decatungstate and anthraquinone were found to act as synergistic HAT photocatalysts. D. functional theory calculations suggested a Pd0-PdII-PdIII-PdI-Pd0 pathway and revealed that regeneration of the Pd0 catalyst and the photocatalyst occurs simultaneously in the presence of KHCO3. This regeneration features a low energy barrier, promoting efficient coupling of the palladium catalytic cycle with the photocatalytic cycle. The work reported herein suggests great promise for further applications of HAT photocatalysis in palladium-catalyzed cross-coupling and C-H functionalization reactions to be successful. The experimental process involved the reaction of 4-(4-Chlorophenyl)piperidin-4-ol(cas: 39512-49-7).Category: piperidines

The Article related to aldehyde direct arylation photocatalyzed hydrogen atom transfer palladium catalysis, Benzene, Its Derivatives, and Condensed Benzenoid Compounds: Ketones and Derivatives, Including Quinones and Sulfur Analogs and other aspects.Category: piperidines

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On February 1, 2019, Buemi, Maria Rosa; Di Fiore, Anna; De Luca, Laura; Angeli, Andrea; Mancuso, Francesca; Ferro, Stefania; Monti, Simona Maria; Buonanno, Martina; Russo, Emilio; De Sarro, Giovanbattista; De Simone, Giuseppina; Supuran, Claudiu T.; Gitto, Rosaria published an article.Safety of 4-(4-Chlorophenyl)piperidin-4-ol The title of the article was Exploring structural properties of potent human carbonic anhydrase inhibitors bearing a 4-(cycloalkylamino-1-carbonyl)benzenesulfonamide moiety. And the article contained the following:

Guided by the crystal structure of 4-(3,4-dihydroquinolin-1(2H)-ylcarbonyl)benzenesulfonamide in complex with hCA II (PDB code 4Z0Q), a novel series of cycloalkylamino-1-carbonylbenzenesulfonamides was designed and synthesized. Thus, we replaced the quinoline ring with an azepine/piperidine/piperazine nucleus and introduced further modifications on cycloalkylamine nucleus by means the installation of hydrophobic/hydrophilic functionalities able to establish addnl. contacts in the middle area of the enzyme cavity. Among the synthesized compounds, the derivatives 7a, 7b, 8b (I – III, resp.) exhibited a remarkable inhibition for hCA II and the brain-expressed hCA VII in sub-nanomolar range. The binding of these mols. to the target enzymes was characterized by means of a crystallog. anal., providing a clear snapshot of the most important interactions established by this class of inhibitors into the hCA II and hCA VII catalytic site. Notably, our results showed that the benzylpiperazine tail of compound 8b is oriented both in hCA II and in hCA VII toward a poorly explored region of the active site. These features should be further investigated for the design of new isoform selective CA inhibitors. The experimental process involved the reaction of 4-(4-Chlorophenyl)piperidin-4-ol(cas: 39512-49-7).Safety of 4-(4-Chlorophenyl)piperidin-4-ol

The Article related to cycloalkylaminocarbonylbenzenesulfonamide human carbonic anhydrase inhibitor structure, benzenesulfonamides, ca inhibitors, carbonic anhydrases, x-ray crystallography, Benzene, Its Derivatives, and Condensed Benzenoid Compounds: Sulfenic, Sulfinic, and Sulfonic Acids and Derivatives and other aspects.Safety of 4-(4-Chlorophenyl)piperidin-4-ol

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On July 18, 2018, Chen, Yiding; Murray, Philip R. D.; Davies, Alyn T.; Willis, Michael C. published an article.Recommanded Product: 39512-49-7 The title of the article was Direct Copper-Catalyzed Three-Component Synthesis of Sulfonamides. And the article contained the following:

Sulfonamides such as N-(phenylsulfonyl)morpholine were prepared in one step by coupling of aryl-, heteroaryl-, and alkenylboronic acids such as phenylboronic acid with cyclic and acyclic alkyl secondary amines such as morpholine and primary anilines and the bis(sulfur dioxide) complex of DABCO (DABSO) in the presence of Cu(OTf)2 and 4,4′-dimethoxy-2,2′-bipyridine in DMSO. The method was used on gram scale and was used to prepare sulfonamides from drugs and drug fragments. The experimental process involved the reaction of 4-(4-Chlorophenyl)piperidin-4-ol(cas: 39512-49-7).Recommanded Product: 39512-49-7

The Article related to aryl heteroaryl alkenyl sulfonamide preparation, copper catalyst coupling boronic acid amine dabso, secondary cyclic acyclic amine aniline coupling boronic acid dabso, Benzene, Its Derivatives, and Condensed Benzenoid Compounds: Sulfenic, Sulfinic, and Sulfonic Acids and Derivatives and other aspects.Recommanded Product: 39512-49-7

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem