Month: October 2022

On April 23, 2020, Blake, James F.; Boys, Mark Laurence; Chicarelli, Mark Joseph; Cook, Adam; Elsayed, Mohamed S. A.; Fell, Jay B.; Fischer, John P.; Hinklin, Ronald Jay; McNulty, Oren T.; Mejia, Macedonio J.; Rodriguez, Martha E.; Wong, Christina E. published a patent.HPLC of Formula: 362703-57-9 The title of the patent was Preparation of pyridopyrazines and related derivatives as SHP2 protein tyrosine phosphatase inhibitors. And the patent contained the following:

The invention is related to the preparation of compounds I [X1-3independently = CH, N; L1 = a bond, S, CH2, O, NH; R1 = (un)substituted Ph, heteroaryl, bicyclic hetero/aryl, bicyclic heterocyclyl; R2 = ; R48 = H, Me, 4-amino-4-methylpiperidin-1-yl, 1,7-diazaspiro[3.5]nonan-7-yl, 4-amino-3-methyl-2-oxa-8-azaspiro[4.5]decan-8-yl, etc.] , their stereoisomers, tautomers and pharmaceutically acceptable salts, that inhibit SHP2 protein tyrosine phosphatase and are useful for treating hyperproliferative and neoplastic diseases. Methods of using compounds I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathol. conditions are disclosed. Thus, reaction of 6-chloropyrido[2,3-b]pyrazin-2-yl trifluoromethanesulfonate (preparation given) with tert-Bu (4-methylpiperidin-4-yl)carbamate, treatment of tert-Bu [1-(6-chloropyrido[2,3-b]pyrazin-2-yl)-4-methylpiperidin-4-yl]carbamate with 2-amino-3-chloropyridine-4-thiol (preparation given) and cleavage of the tert-butoxycarbonyl group gave II. Certain exemplary compounds were assayed for their SHP2 inhibition activity in an enzymic assay; II showed an iC50 of 33 nM. A cell- based assay was used to determine the effect of SHP2 inhibitors on downstream signaling by assaying ERK1/2 phosphorylation. 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 pyridopyrazine preparation shp2 protein tyrosine phosphatase inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.HPLC of Formula: 362703-57-9

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On September 30, 2021, Araujo, Erika; Sparks, Steven M.; Berlin, Michael; Zhang, Wei; Wang, Jing published a patent.Reference of tert-Butyl 3-(piperidin-4-yl)azetidine-1-carboxylate The title of the patent was Indazole based compounds and associated methods of use. And the patent contained the following:

Bifunctional compounds (e.g., I), which find utility as modulators of leucine-rich repeat kinase 2 (LRRK2), are described herein. In particular, the hetero-bifunctional compounds of the present disclosure contain on one end a moiety that binds to the cereblon E3 ubiquitin ligase and on the other end a moiety which binds LRRK2, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The hetero-bifunctional compounds of the present disclosure exhibit a broad range of pharmacol. activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aberrant regulation of the target protein are treated or prevented with compounds and compositions of the present disclosure. The experimental process involved the reaction of tert-Butyl 3-(piperidin-4-yl)azetidine-1-carboxylate(cas: 1251006-64-0).Reference of tert-Butyl 3-(piperidin-4-yl)azetidine-1-carboxylate

The Article related to indazole hetero bifunctional leucine rich repeat kinase inhibitor preparation, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Reference of tert-Butyl 3-(piperidin-4-yl)azetidine-1-carboxylate

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On August 26, 2021, Palmer, Wylie Solang; Wu, Jeffrey; Zipfel, Sheila; Ozboya, Kerem; Weiss, Dahlia published a patent.Quality Control of 2-(2,6-Dioxopiperidin-3-yl)-1,3-dioxoisoindoline-5-carboxylic acid The title of the patent was Preparation of bifunctional degraders of interleukin-1 receptor-associated kinases and therapeutic use thereof. And the patent contained the following:

The present disclosure provides bifunctional compounds I [R1 = (un)substituted C1-10 alkyl, C3-10 cycloalkyl, or 3-12 membered heterocyclyl; L = L1L2L3L4L5, each L1-L5 being independently: (a) (un)substituted C3-12 cycloalkyl, (b) (un)substituted C6-12 aryl, (c) (un)substituted 3-12 membered heterocyclyl, etc.; LHM = a ligase harness moiety] or pharmaceutically acceptable salts as IRAK4 degraders via ubiquitin proteasome pathway, and method for treating diseases modulated by IRAK4. E.g., a multi-step synthesis of II, starting from Me 4,6-dichloropyridine-3-carboxylate and tetrahydropyran-4-amine hydrochloride, was described. IRAK4 degradation of exemplified compounds I were measured in multiple runs using HTRF assay and HiBit assay (data given). Pharmaceutical composition comprising I was disclosed. The experimental process involved the reaction of 2-(2,6-Dioxopiperidin-3-yl)-1,3-dioxoisoindoline-5-carboxylic acid(cas: 1216805-11-6).Quality Control of 2-(2,6-Dioxopiperidin-3-yl)-1,3-dioxoisoindoline-5-carboxylic acid

The Article related to interleukin1 receptor associated kinase irak4 bifunctional degrader pyrrolopyridazinecarbonitrile preparation, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Quality Control of 2-(2,6-Dioxopiperidin-3-yl)-1,3-dioxoisoindoline-5-carboxylic acid

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

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

Liu, Kai; Zhang, Datong; Chojnacki, Jeremy; Du, Yuhong; Fu, Haian; Grant, Steven; Zhang, Shijun published an article in 2013, the title of the article was Design and biological characterization of hybrid compounds of curcumin and thalidomide for multiple myeloma.Application In Synthesis of 2-(2,6-Dioxopiperidin-3-yl)-1,3-dioxoisoindoline-5-carboxylic acid And the article contains the following content:

In our efforts to develop effective treatment agents for human multiple myeloma (MM), a series of hybrid mols. based on the structures of thalidomide (I) and curcumin (II) were designed, synthesized, and biol. characterized in human multiple myeloma MM1S, RPMI8226, U266 cells, and human lung cancer A549 cells. The biol. results showed that two hybrid compounds, III and IV, exhibited significantly improved lethal effects towards all three human MM cell models compared to I or II alone, as well as the combination of I and II. Furthermore, mechanistic studies in U266 cells demonstrated that III and IV can induce the production of reactive oxygen species (ROS) and cause G1/S arrest, thus leading to apoptosis and cell death. Addnl., they exhibited inhibitory effects on NFκB activation in A549 cells. Collectively, the results obtained from these hybrid compounds strongly encourage their further optimization as new leads to develop effective treatment agents for human MM. The experimental process involved the reaction of 2-(2,6-Dioxopiperidin-3-yl)-1,3-dioxoisoindoline-5-carboxylic acid(cas: 1216805-11-6).Application In Synthesis of 2-(2,6-Dioxopiperidin-3-yl)-1,3-dioxoisoindoline-5-carboxylic acid

The Article related to curcumin thalidomide hybrid preparation multiple myeloma treatment, Biomolecules and Their Synthetic Analogs: Others, Including Purines, Pyrimidine Nucleic Acid Bases, Flavins, Lignans and other aspects.Application In Synthesis of 2-(2,6-Dioxopiperidin-3-yl)-1,3-dioxoisoindoline-5-carboxylic acid

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

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 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