Category: piperidines

On September 8, 2017, Himmelsbach, Frank; Blum, Andreas; Peters, Stefan published a patent.Recommanded Product: tert-Butyl 3-(piperidin-4-yl)azetidine-1-carboxylate The title of the patent was Preparation of pyridinylmethyl carbamimidoylcarbamate derivatives as AOC3 inhibitors. And the patent contained the following:

The invention relates to new heteroaryl derivatives I [X1 = N and CH; X2 = N and CF (with the proviso that at least one of X1 and X2 is N); A = II-IV (R4 = (un)substituted azetidinyl, pyrrolidinyl, piperidinyl, piperazinyl, etc.)] or a pharmaceutically acceptable salt thereof, to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them. Over one-hundred compounds I were prepared General procedures for preparation of compounds I were provided. For example, compound I was prepared, starting from (2,3-difluoro-4-pyridyl)methanol and 3-phenylazetidine. Exemplified compounds I were tested for their pharmacol. activity in the AOC3 assay (IC50 values were given). The experimental process involved the reaction of tert-Butyl 3-(piperidin-4-yl)azetidine-1-carboxylate(cas: 1251006-64-0).Recommanded Product: tert-Butyl 3-(piperidin-4-yl)azetidine-1-carboxylate

The Article related to pyridinylmethyl carbamimidoylcarbamate preparation aoc3 vascular adhesion protein 1 inhibitor, heteroaryl carbamimidoylcarbamate preparation aoc3 vascular adhesion protein 1 inhibitor and other aspects.Recommanded Product: tert-Butyl 3-(piperidin-4-yl)azetidine-1-carboxylate

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On May 8, 2020, Ji, Changjin; Liu, Na; Tu, Jie; Li, Zhuang; Han, Guiyan; Li, Jian; Sheng, Chunquan published an article.Quality Control of 4-(4-Chlorophenyl)piperidin-4-ol The title of the article was Drug Repurposing of Haloperidol: Discovery of New Benzocyclane Derivatives as Potent Antifungal Agents against Cryptococcosis and Candidiasis. And the article contained the following:

Despite the high morbidity and mortality of invasive fungal infections (IFIs), effective and safe antifungal agents are rather limited. Starting from antifungal lead compound haloperidol that was identified by drug repurposing, a series of novel benzocyclane derivatives were designed, synthesized, and assayed. Several compounds showed improved antifungal potency and broader antifungal spectra. Particularly, compound B10 showed good inhibitory activities against a variety of fungal pathogens and was proven to be an inhibitor of several virulence factors important for drug resistance. In the in vivo cryptococcosis and candidiasis models, compound B10 could effectively reduce the brain fungal burden of Cryptococcus neoformans and synergize with fluconazole to treat resistant Candida albicans infections. Preliminary antifungal mechanism studies revealed that compound B10 regained cell membrane damage and down-regulated the overexpression of ERG11 and MDR1 genes when used in combination with fluconazole. Taken together, haloperidol derivative B10 represents a promising lead compound for the development of a new generation of antifungal agents. The experimental process involved the reaction of 4-(4-Chlorophenyl)piperidin-4-ol(cas: 39512-49-7).Quality Control of 4-(4-Chlorophenyl)piperidin-4-ol

The Article related to antifungal haloperidol drug repurposing cryptococcus drug resistance candida, candida albicans, cryptococcus neoformans, antifungal, drug repurposing, drug resistance, haloperidol and other aspects.Quality Control of 4-(4-Chlorophenyl)piperidin-4-ol

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On September 21, 2018, Mowrey, Dale R.; Reif, James J.; Milkiewicz, Karen L.; Allwein, Shawn P. published an article.Related Products of 883984-95-0 The title of the article was Development of a Novel Process for the Kilogram-Scale Synthesis of Spiro[1H-pyrido[2,3-d][1,3]oxazine-4,4′-piperidine]-2-one. And the article contained the following:

The dihydrochloride of spiro[1H-pyrido[2,3-d][1,3]oxazine-4,4′-piperidine]-2-one I·2 HCl was prepared on kilogram scale by base-mediated Boc protection of 3-bromo-2-pyridinamine, metalation with i-PrMgCl and spirocyclization with 1-Boc-4-piperidinone, and Boc deprotection with aqueous HCl in isopropanol. A two-batch kilo lab campaign generated I·2 HCl in >99% HPLC area purity and in 77% overall yield. The experimental process involved the reaction of Benzyl 7′-chloro-2′-oxo-1′,2′-dihydrospiro[piperidine-4,4′-pyrido[2,3-d][1,3]oxazine]-1-carboxylate(cas: 883984-95-0).Related Products of 883984-95-0

The Article related to spiropyridooxazinepiperidinone kilogram scale preparation, butoxycarbonylation bromopyridinamine metalation spirocyclization butoxycarbonylpiperidone neutralization kilogram scale and other aspects.Related Products of 883984-95-0

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On September 1, 2020, Donoghue, Craig; Cubillos-Rojas, Monica; Gutierrez-Prat, Nuria; Sanchez-Zarzalejo, Carolina; Verdaguer, Xavier; Riera, Antoni; Nebreda, Angel R. published an article.Application of 1216805-11-6 The title of the article was Optimal linker length for small molecule PROTACs that selectively target p38α and p38β for degradation. And the article contained the following:

We report the design of hetero-bifunctional small mols. that selectively target p38α and p38β for degradation These proteolysis targeted chimeras (PROTACs) are based on an ATP competitive inhibitor of p38α and p38β, which is linked to thalidomide analogs to recruit the Cereblon E3 ubiquitin ligase complex. Compound synthesis was facilitated by the use of a copper catalyzed “click” reaction. We show that optimization of the linker length and composition is crucial for the degradation-inducing activity of these PROTACs. We provide evidence that these chem. compounds can induce degradation of p38α and p38β but no other related kinases at nanomolar concentrations in several mammalian cell lines. Accordingly, the PROTACs inhibit stress and cytokine-induced p38α signaling. Our compounds contribute to understanding the development of PROTACs, and provide a useful tool to investigate functions of the p38 MAPK pathway and its involvement in diseases. The experimental process involved the reaction of 2-(2,6-Dioxopiperidin-3-yl)-1,3-dioxoisoindoline-5-carboxylic acid(cas: 1216805-11-6).Application of 1216805-11-6

The Article related to preparation protacs targeting p38 alpha beta proteolysis, azide-alkyne click reaction, cereblon, protac linker optimization, protein degradation, thalidomide derivative, p38 mapk and other aspects.Application of 1216805-11-6

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On August 15, 2014, Salama, Ismail; Loeber, Stefan; Huebner, Harald; Gmeiner, Peter published an article.COA of Formula: C11H14ClNO The title of the article was Synthesis and binding profile of haloperidol-based bivalent ligands targeting dopamine D2-like receptors. And the article contained the following:

Homodimers of dopamine D2-like receptors are suggested to be of particular importance in the pathophysiol. of schizophrenia and, thus, serve as promising targets for the discovery of atypical antipsychotics. This study describes the development of a series of novel bivalent mols. with a pharmacophore derived from the dopamine receptor antagonist haloperidol. These dimers were investigated in comparison to their monomeric analogs for their D2long, D2short, D3, and D4 receptor binding and the ability to bridge two neighboring receptor protomers. Radioligand binding studies provided diagnostic insights when Hill slopes close to two for the bivalent ligand 13 incorporating 22 spacer atoms and a comparative anal. with monovalent control ligands indicated a bivalent binding mode with a simultaneous occupancy of two neighboring binding sites. The experimental process involved the reaction of 4-(4-Chlorophenyl)piperidin-4-ol(cas: 39512-49-7).COA of Formula: C11H14ClNO

The Article related to preparation haloperidol bivalent ligand dopamine d2 receptor antipsychotic, binding affinity, bivalent ligands, d(2) receptor, d(3) receptor, d(4) receptor, dopamine, gpcr dimers and other aspects.COA of Formula: C11H14ClNO

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

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

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 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 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