Month: November 2022

On January 6, 2022, Anderson, Kenneth C.; Hideshima, Teru; Dhe-Paganon, Sirano; Seo, Hyuk-Soo; Mizutani, Takashi; Zhang, Tinghu published a patent.Category: piperidines The title of the patent was PRPK inhibitors. And the patent contained the following:

This disclosure relates to compounds of formula (I) as defined in the Specification. This disclosure also relates to methods of synthesizing the compound of formula I and using the compounds of formula I for treating a disease (e.g., cancer). The experimental process involved the reaction of 2-(2,6-Dioxopiperidin-3-yl)-1,3-dioxoisoindoline-5-carboxylic acid(cas: 1216805-11-6).Category: piperidines

The Article related to prpk inhibitor cancer, Pharmaceuticals: Formulation and Compounding and other aspects.Category: piperidines

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On August 6, 2020, U. Dighe, Shashikant; Julia, Fabio; Luridiana, Alberto; Douglas, James J.; Leonori, Daniele published an article.HPLC of Formula: 39512-49-7 The title of the article was A photochemical dehydrogenative strategy for aniline synthesis. And the article contained the following:

Chem. reactions that reliably join two mol. fragments together (cross-couplings) are essential to the discovery and manufacture of pharmaceuticals and agrochems.1,2. The introduction of amines onto functionalized aromatics at specific and pre-determined positions (ortho vs. meta vs. para) is currently achievable only in transition-metal-catalyzed processes and requires halogen- or boron-containing substrates3-6. The introduction of these groups around the aromatic unit is dictated by the intrinsic reactivity profile of the method (electrophilic halogenation or C-H borylation) so selective targeting of all positions is often not possible. Here we report a non-canonical cross-coupling approach for the construction of anilines, exploiting saturated cyclohexanones as aryl electrophile surrogates. Condensation between amines and carbonyls, a process that frequently occurs in nature and is often used by (bio-)organic chemists7, enables a predetermined and site-selective carbon-nitrogen (C-N) bond formation, while a photoredox- and cobalt-based catalytic system progressively desaturates the cyclohexene ring en route to the aniline. Given that functionalized cyclohexanones are readily accessible with complete regiocontrol using the well established carbonyl reactivity, this approach bypasses some of the frequent selectivity issues of aromatic chem. We demonstrate the utility of this C-N coupling protocol by preparing com. medicines and by the late-stage amination-aromatization of natural products, steroids and terpene feedstocks. 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 aniline preparation photochem dehydrogenative amination, General Organic Chemistry: Synthetic Methods and other aspects.HPLC of Formula: 39512-49-7

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Kumar, Rayala Naveen; Meshram, H. M. published an article in 2016, the title of the article was ‘Claycop’ catalyzed highly efficient and chemoselective aza-Michael addition under solvent free condition.HPLC of Formula: 39512-49-7 And the article contains the following content:

A chemoselective and highly efficient addition of amines to electron deficient alkenes is described in the presence of claycop in solvent free condition. The reaction is very rapid and exhibited higher yields in comparison with slurry reaction. Claycop can be readily recovered and reused after activation. This method is suitable for a variety of amines and alkenes. Solvent free condition and recyclability of supported catalyst makes procedure more environmental friendly. 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 electron deficient alkene amine addition claycop solvent free condition, General Organic Chemistry: Synthetic Methods and other aspects.HPLC of Formula: 39512-49-7

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Rafiq, Kiran; Saify, Zafar Saied; Vaid, Faiyaz; Navaid, Farzana; Kamil, Arfa; Kausar, Rana; Ghous, Asghari published an article in 2013, the title of the article was Synthesis of 4-(4′-chlorophenyl)-4-hydroxy piperidine analogues having promising compatibility with alpha amylase enzyme.Product Details of 39512-49-7 And the article contains the following content:

A new series of 4-(4′-Chlorophenyl)-4-hydroxy piperidine derivatives I·HX [R = adamantan-1-acyl, 6-methyluracil, 3-phenoxy-1-Pr, 3-phenyl-1-propyl] were synthesized with different phenacyl halide. All synthesized compounds were screened for their in vitro antiamylatic activity by semiquant. agar plate method. The parent compound 4-(4′-Chlorophenyl)-4-hydroxy piperidine showed moderate while I·HX [R = adamantan-1-acyl, 3-phenoxy-1-Pr, 3-phenyl-1-propyl] showed good antiamylatic activity. The experimental process involved the reaction of 4-(4-Chlorophenyl)piperidin-4-ol(cas: 39512-49-7).Product Details of 39512-49-7

The Article related to chlorophenyl hydroxy piperidine preparation antiamylase, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.Product Details of 39512-49-7

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On June 30, 2016, Bradner, James; Buckley, Dennis; Winter, Georg published a patent.Application of 1216805-11-6 The title of the patent was Methods to induce targeted protein degradation through bifunctional molecules. And the patent contained the following:

The present application provides bifunctional compounds which act as protein degradation inducing moieties. The present application also relates to methods for the targeted degradation of endogenous proteins through the use of the bifunctional compounds that link a cereblon-binding moiety to a ligand that is capable of binding to the targeted protein which can be utilized in the treatment of proliferative disorders. The present application also provides methods for making compounds of the application and intermediates thereof. 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 targeted protein degradation bifunctional mol preparation, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.Application of 1216805-11-6

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On July 31, 2018, Rafiq, Kiran; Saify, Zafar Saied; Nesar, Shagufta; Faiyaz, Ambreen; Muhammad, Iyad Naeem published an article.COA of Formula: C11H14ClNO The title of the article was Some novel piperidine analogues having strong alpha glucosidase inhibition. And the article contained the following:

In the present work some hydroxy piperidine analogs have been synthesized and analyzed for their hypoglycemic effect through glucosidase inhibition owing to the structural resemblance with nojirimycin. The activity was done by spectral absorbance anal. using acarbose as standard Two analogs 1-(1”-phenoxypropyl)-4-phenyl-4-hydroxy piperidinium hydrobromide and 1-(1”-adamantan acyl)-4-(4′-bromophenyl)-4-hydroxy piperidinium hydrobromide were found to pose excellent activity having 87.4 and 54.7% inhibition resp., hence strengthening the idea of studying piperidine analogs as glucosidase inhibitors due to structural similarity with nojirimycin. 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 piperidine derivative preparation alpha glucosidase inhibitor, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.COA of Formula: C11H14ClNO

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On June 12, 2014, Frei, Beat; Gobbi, Luca; Grether, Uwe; Kimbara, Atsushi; Nettekoven, Matthias; Roever, Stephan; Rogers-Evans, Mark; Schulz-Gasch, Tanja published a patent.Safety of tert-Butyl 4-amino-4-(2-methoxy-2-oxoethyl)piperidine-1-carboxylate The title of the patent was Preparation of novel pyridine derivatives as cannabinoid receptor 2 agonists. And the patent contained the following:

The title compounds I [R1 = halo, cycloalkylalkoxy, alkylsulfonyl, etc.; R2 = halo, cycloalkyl, haloalkyl, etc.; R3 = (alkyl)(oxo)pyrrolidinyl or C(R4R5)C(R6R7)C(O)R8; R4, R5 = H, alkyl, Ph, etc.; or R4 and R5 together with the carbon atom to which they are attached form cycloalkyl, oxetanyl, thiethanyl, etc.; R6, R7 = H, alkyl; or one of R4 and R5 and one of R6 and R7, together with the carbon atoms to which they are attached, form cycloalkyl, and the other ones are both hydrogen at the same time; R8 = NH2, alkoxy, alkylamino, OH], useful as CB2 receptor agonists were prepared and formulated. E.g., a multi-step synthesis of the amide II, starting from Me 5-bromo-pyridine-2-carboxylate, was described. The exemplified compounds I showed an excellent affinity for the CB2 receptor with affinities below 10 μM (specific data given). The experimental process involved the reaction of tert-Butyl 4-amino-4-(2-methoxy-2-oxoethyl)piperidine-1-carboxylate(cas: 362703-57-9).Safety of tert-Butyl 4-amino-4-(2-methoxy-2-oxoethyl)piperidine-1-carboxylate

The Article related to pyridine amide preparation cannabinoid receptor 2 cb2 agonist, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.Safety of tert-Butyl 4-amino-4-(2-methoxy-2-oxoethyl)piperidine-1-carboxylate

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On January 27, 2022, Lee, Song Hee; Ryu, Je Ho; Ahn, Jung Min; Choi, Yu Ri; Lee, Ho Hyun; Jang, Mi Young; Woo, Yae Jin; Kim, Hanwool; Kim, Ji Young; Park, Ji Youn published a patent.Recommanded Product: 1262988-77-1 The title of the patent was Amide compound for androgen receptor degradation, and pharmaceutical use thereof. And the patent contained the following:

The present invention provides a compound I [R1 = H, alkyl, halogen, etc.; R2 = H, alkyl, halogen, etc.; X1, X3, X4 and X5 = independently CH or N; X2 = CR3 or N; R3 = H, alkyl, halogen, etc.; n = 0, 1, or 2; m = 0 or 1; L = -(CH2)q1-A1-(CH2)q2-B1-(CH2)q3-A2-(CH2)q4-B2-(CH2)q5-A3-(CH2)q6-B3-; A1, A2 and A3 = independently direct bond, -O-, -N(R4)-, etc.; R4 = H, alkyl or haloalkyl; B1, B2 and B3 = independently direct bond, cycloalkyl, heterocycle, etc.; q1-q6 = independently 0-6; E = Q1 or Q2; X6, X7, X8 and X9 = independently CH or N; Y = -C(R6)2-, -C(O)-, -C(R6)2-C(R6′)2-, etc.; Z = direct bond, -C(R6)2-, -O-, etc.; R5 and R5′ = independently H, alkyl, halogen, etc.; R6 and R6′ = independently H, alkyl, halogen, etc.] of a specific chem. structure, having androgen receptor (AR) degradation activity, or a pharmaceutically acceptable salt thereof. The present invention also provides a composition containing the compound or a pharmaceutically acceptable salt thereof. According to present invention, provided is a pharmaceutical use of the compound, the salt thereof, and the composition containing same for treating or preventing AR-related diseases. According to the present invention, further provided is a method for treating or preventing AR-related diseases, the method comprising administering, to a subject in need of treatment, an effective amount of the compound, the salt thereof, or the composition containing same. For example, compound II (preparation given) was coupled with compound III (preparation given) to provide compound IV. The experimental process involved the reaction of 1-Benzyl-4-hydroxypiperidine-4-carboxylic acid hydrochloride(cas: 1262988-77-1).Recommanded Product: 1262988-77-1

The Article related to amide compound preparation androgen receptor degradation activity, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.Recommanded Product: 1262988-77-1

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

On January 1, 2014, Hatae, Noriyuki; Nagayama, Tomoyuki; Esaki, Hiroyoshi; Kujime, Eiko; Minami, Masabumi; Ishikura, Minoru; Choshi, Tominari; Hibino, Satoshi; Okada, Chiaki; Toyota, Eiko; Nagasawa, Hideko; Iwamura, Tatsunori published an article.Application of 39512-49-7 The title of the article was Synthesis of 4-arylpiperidin-4-ol derivatives of loperamide as agents with potent antiproliferative effects against HCT-116 and HL-60 cells. And the article contained the following:

The synthesis of 4-arylpiperidin-4-ol derivatives of loperamide I [R1 = n-Pr, Ph2C(OH)CH2, R2 = 4-ClC6H4; R1 = Ph2C(OH)CH2CH2, R2 = Ph, 4-ClC6H4, 3-F3CC6H4] and N-(3-hydroxy-3,3-diphenylpropyl)piperidine was carried out by alkylation of the corresponding N-unsubstituted piperidines. The synthesized compounds were tested for their antiproliferative activity against HCT-116 cells and HL-60 cells. The N-substituents on 4-arylpiperidin-4-ol units were found to play an important role in their antiproliferative activity, and the N-diphenylpropanol analogs exhibited the most potent antiproliferative activity. The experimental process involved the reaction of 4-(4-Chlorophenyl)piperidin-4-ol(cas: 39512-49-7).Application of 39512-49-7

The Article related to piperidinol aryl preparation loperamide antiproliferative activity, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.Application of 39512-49-7

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Ibis, Cemil; Ayla, Sibel Sahinler; Bahar, Hakan; Stasevych, Maryna V.; Komarovska-Porokhnyavets, Olena; Novikov, Volodymyr published an article in 2015, the title of the article was Synthesis, Characterization, and Biological Properties of Novel Piperidinolyl-, Piperidinyl-, and Piperazinyl-Substituted Naphthoquinone Compounds and Their Reactions With Some Thiols.Electric Literature of 39512-49-7 And the article contains the following content:

Nucleophilic substitution reactions of 2,3-dichloro-1,4-naphthoquinone were studied using a variety of piperidinol, piperidine, and piperazine derivatives The N-substituted compounds were treated with some thiols and N,S-substituted compounds were formed. The structures of the new products were characterized by spectroscopic methods (1H NMR, 13C NMR, MS) and elemental anal. The novel compounds were evaluated for their antibacterial and antifungal activity. 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 naphthoquinone derivative preparation antibacterial antifungal activity, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.Electric Literature of 39512-49-7

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem