Tag: 200-300

On March 17, 2022, Ryu, Hyung-Chul; Kim, Jae-Sun; Lim, Jee-Woong; Lee, Ju Young; Choi, Kwanghyun; Rajesh, Rengasamy; Chang, Duk-Ho; Gwon, Hyeok Jun; Kang, Hyo Jin published a patent.Safety of tert-Butyl 4-(piperidin-4-ylmethyl)piperazine-1-carboxylate The title of the patent was Preparation of pyrimidinamine derivatives for suppressing EGFR mutant cancer and pharmaceutical use thereof. And the patent contained the following:

The invention relates to pyrimidinamine derivatives of formula I, pharmaceutically acceptable salts, or pharmaceutical compositions thereof which have the activity of inhibiting and/or degrading mutant EGFR protein and are useful for the treatment or prevention of cancer with EGFR mutation, especially lung cancer. The present disclosure also provides a method for the treatment or prevention of EGFR mutation cancer, especially lung cancer, the method comprising administering an effective amount of the compound according to the present invention, a salt thereof, or a composition containing same to a subject in need of treatment. Compounds of formula I wherein R1 and R2 are independently H, (halo)alkyl, or trideuteromethyl; R3 – R6 are independently H, halo, cyano, (halo)alkyl, (halo)alkoxy, etc.; m and n are independently 0-4; A is heterocyclyl; L is a connecting group through covalent bond; B is Q1 or Q2; X is single bond, (CH2)1-6, O-(CH2)0-6, C(O)-(CH2)0-6, N(R13)-(CH2)0-6, C(O)-N(R13)-(CH2)0-6, N(R13)-C(O)-(CH2)0-6, etc.; W is C(R14)2 or C(O); R8 is H, hydroxy, halo, (halo)alkyl, or (halo)alkoxy; R9 and R10 are independently H or alkyl; R13 and R14 are independently H or alkyl; o and p are independently 1-3; Y is (halo)alkyl, aryl, etc.; Z is O or S; R11 is H, alkyl, or (CH2)1-6-C(O); R12 is H, alkyl, or cycloalkyl; are claimed. The invention compounds were evaluated for the EGFR protein degradation activity (biol. data given). The experimental process involved the reaction of tert-Butyl 4-(piperidin-4-ylmethyl)piperazine-1-carboxylate(cas: 1211568-27-2).Safety of tert-Butyl 4-(piperidin-4-ylmethyl)piperazine-1-carboxylate

The Article related to pyrimidinamine derivative preparation egfr mutant lung cancer, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Safety of tert-Butyl 4-(piperidin-4-ylmethyl)piperazine-1-carboxylate

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

On June 2, 2022, Zhang, Chen; Liao, Yuting; Ye, Fei; Tang, Pingming; Chen, Xiaogang; Lu, Yonghua; Gao, Qiu; Li, Yao; Ni, Jia; Yan, Pangke published a patent.Reference of tert-Butyl 4-(piperidin-4-ylmethyl)piperazine-1-carboxylate The title of the patent was Benzene ring derivative, and composition and pharmaceutical use thereof. And the patent contained the following:

Disclosed are a compound or a stereoisomer, deuterated compound, solvate, prodrug, metabolite, pharmaceutically acceptable salt or co-crystal thereof, and an intermediate thereof, and the use thereof in AR or AR splicing mutant-related diseases such as cancer. The experimental process involved the reaction of tert-Butyl 4-(piperidin-4-ylmethyl)piperazine-1-carboxylate(cas: 1211568-27-2).Reference of tert-Butyl 4-(piperidin-4-ylmethyl)piperazine-1-carboxylate

The Article related to benzene ring derivative preparation treatment cancer disease, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Reference of tert-Butyl 4-(piperidin-4-ylmethyl)piperazine-1-carboxylate

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

On October 8, 2020, Yang, Bin; Hayhow, Thomas George Christopher; Fallan, Charlene; Scott, James Stewart; Diene, Coura; Barlaam, Bernard Christophe; Nissink, Johannes Wilhelmus Maria published a patent.Application of 1211568-27-2 The title of the patent was Pyrimidinyltetrahydropyridoindoles as estrogen receptor degrading PROTACs and their preparation. And the patent contained the following:

The specification relates to compounds of formula I and pharmaceutically acceptable salts thereof. This specification also relates to the use of such compounds and pharmaceutically acceptable salts thereof in methods of treatment of the human or animal body, for example in prevention or treatment of cancer. This specification also relates to processes and intermediate compounds involved in the preparation of such compounds and to pharmaceutical compositions containing them. Compounds of formula I wherein A and G are independently CR5 and N; E and Q are independently CH and N; R1 and R2 are H; R1R2 can be taken together to form oxo; R3 and R4 are independently H and OMe; R5 is H, F, Cl, CN, Me and OMe; R6 and R7 are independently H, Me and F; R6R7 can be taken together to form cyclopropyl and oxetanyl; R8 is H, Me, F, CH2F, CN, etc.; Linker is (un)substituted. (un)branched, (un)cyclized, (un)saturated 6 to 15 carbon atom moiety where 1 ot 6 carbon atoms may optionally be replaced with O, N and S; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by a multistep procedure (procedure given). The invention compounds were evaluated for their estrogen binding affinity and estrogen degradation activity. From the assay, it was determined that compound II exhibited IC50 values of 3.1 nM and 1.1 nM toward ER binding and ER degradation, resp. The experimental process involved the reaction of tert-Butyl 4-(piperidin-4-ylmethyl)piperazine-1-carboxylate(cas: 1211568-27-2).Application of 1211568-27-2

The Article related to pyrimidinylpyridoindole preparation er degrading protac, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Application of 1211568-27-2

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

On March 15, 2007, Silverman, Lisa S.; Caldwell, John P.; Greenlee, William J.; Kiselgof, Eugenia; Matasi, Julius J.; Tulshian, Deen B.; Arik, Leyla; Foster, Carolyn; Bertorelli, Rosalia; Monopoli, Angela; Ongini, Ennio published an article.Formula: C12H16N2O2 The title of the article was 3H-[1,2,4]-Triazolo[5,1-i]purin-5-amine derivatives as adenosine A2A antagonists. And the article contained the following:

A novel series of 3-substituted-8-aryl-[1,2,4]triazolo[5,1-i]purin-5-amine analogs related to Sch 58261 was synthesized in order to identify potent adenosine A2A receptor antagonists with improved selectivity over the A1 receptor, physiochem. properties, and pharmacokinetic profiles as compared to those of Sch 58261. As a result of structural modifications, numerous analogs with excellent in vitro binding affinities and selectivities were identified. Moreover, compound I (R = MeOCH2CH2O) displayed both superior in vitro and highly promising in vivo profiles. The experimental process involved the reaction of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone(cas: 67914-60-7).Formula: C12H16N2O2

The Article related to triazolopurinamine preparation adenosine a2a antagonist, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Formula: C12H16N2O2

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

On April 22, 2021, Berlin, Michael; Dong, Hanqing; Sherman, Dan; Snyder, Lawrence; Wang, Jing; Zhang, Wei published a patent.COA of Formula: C15H29N3O2 The title of the patent was Bifunctional molecules containing an E3 ubiquitin ligase binding moiety linked to a BCL6 targeting moiety and their preparation. And the patent contained the following:

Bifunctional compounds of formula I, which find utility as modulators of B-cell lymphoma 6 protein (BCL6; target protein), are described herein. Bifunctional compounds of formula I wherein ULM is a small E3 ubiquitin ligase binding moiety that bonds Von Hippel-Lindau, cereblon; PTM is a small mol. comprising a B-cell lymphoma 6 protein targeting moiety; L is a bond and a chem. linker; pharmaceutically acceptable salts, enantiomers, stereoisomers, solvates, and polymorphs thereof, are claimed. The bifunctional compounds of the disclosure exhibit a broad range of pharmacol. activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the disclosure. Example compound II was prepared by a general procedure (procedure given). The invention compounds were evaluated for their BCL6 protein degradation activity (some data given). The experimental process involved the reaction of tert-Butyl 4-(piperidin-4-ylmethyl)piperazine-1-carboxylate(cas: 1211568-27-2).COA of Formula: C15H29N3O2

The Article related to bifunctional mol preparation bcl6 protein degrader, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.COA of Formula: C15H29N3O2

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

On November 20, 2019, Daneshyar, Anahita; Nematollahi, Davood; Varmaghani, Fahimeh; Goljani, Hamed; Alizadeh, Hojjat published an article.Reference of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone The title of the article was Electrochemical synthesis of a new phosphonium betaine. Kinetic evaluation and antibacterial susceptibility. And the article contained the following:

Cyclic voltammetry, controlled-potential coulometry, chronoamperometry, chronocoulometry and chronopotentiometry methods were used for the electrochem. study of 1-acetyl-4-(4-hydroxyphenyl)piperazine (APIP) in the presence of PPh3 (TPP) as a nucleophile. Electrochem. generated APIPox can serve as a Michael acceptor for nucleophilic attack by TPP to yield a new phosphonium betaine (APTP). The authors prepared a new product in good yield and purity by reaction of TPP with APIPox in an undivided cell equipped with C anode. Based on an EC mechanism, the observed homogeneous rate constant (kobs) of the Michael addition reaction of APIPox with TPP were estimated by comparing the exptl. cyclic voltammograms with the digital simulated results. Also, electrochem. oxidation of APIP was studied both exptl. and theor. to provide insight into the influence of natural charge and thermodn. stability parameters on the type of chem. reaction which follows APIPox. The synthesized compound was evaluated for in vitro antibacterial. The experimental process involved the reaction of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone(cas: 67914-60-7).Reference of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone

The Article related to electrochem synthesis phosphonium betaine kinetics antibacterial susceptibility, antibacterial agents, chronoamperometry, chronopotentiometry, coulometry, cyclic voltammetry, glassy carbon electrodes, ir spectra, lumo (molecular orbital), mass spectra, nmr (nuclear magnetic resonance), reaction mechanism and other aspects.Reference of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Amani, Amene; Khazalpour, Sadegh; Nematollahi, Davood published an article in 2013, the title of the article was Electrochemical oxidation of acetaminophen and 4-(piperazin-1-yl)phenols in the presence of 4-hydroxy-1-methyl-2(1H)-quinolone.Electric Literature of 67914-60-7 And the article contains the following content:

A facile and 1-pot electrochem. method for the synthesis of mono and disubstituted 1,4-benzoquinones generated from the electrochem. oxidation of 1-(4-(4-hydroxyphenyl)piperazin-1-yl)ethanone (1a), 4-(piperazin-1-yl)phenol (1b) and acetaminophen (8) in the presence of 4-hydroxy-1-methyl-2(1H)-quinolone (3) as nucleophile is reported. The electrochem. generated electrophiles derived from the oxidation of 1a, 1b and 8 participate in Michael-addition reactions with 3. The authors report the synthesis of mono and diquinolone substituted of 1,4-benzoquinone in good yields based on controlled potential condition at C electrode in a divided cell. The experimental process involved the reaction of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone(cas: 67914-60-7).Electric Literature of 67914-60-7

The Article related to electrochem oxidation acetaminophen piperazinylphenol hydroxymethylquinolone, cyclic voltammetry, deprotonation (in electrochem. oxidation), electrochemical oxidation, glassy carbon electrodes, hydrolysis, michael reaction (electrochem.), nmr (nuclear magnetic resonance), reaction mechanism and other aspects.Electric Literature of 67914-60-7

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Beiginejad, Hadi; Nematollahi, Davood; Varmaghani, Fahimeh; Bayat, Mehdi published an article in 2013, the title of the article was Efficient factors on the hydrolysis reaction rate of some para-aminophenol derivatives in acidic pHs.Reference of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone And the article contains the following content:

Electrochem. oxidation of some p-aminophenol derivatives (1-5) in acidic solutions was studied both exptl. and theor. to provide insight into the influence of some factors on the hydrolysis reaction rate. The result of this work shows that the electrogenerated p-quinoneimines participate in the hydrolysis reaction and are converted to the p-benzoquinone. The hydrolysis reaction rate strongly depends on the structure of the p-aminophenols and solution’s pH. The observed homogeneous rate constants of hydrolysis (kobshyd) of p-quinoneimines were determined using digital simulation technique. The effect of different parameters such as: change of Gibbs free energy (ΔG) of the electrochem. oxidation of para-aminophenol derivatives (1-5), charge of reaction site, N-C4 bond order (Wiberg Bond Indexes, WBIs) and the nature of substituted group, on the hydrolysis rate constant were also studied. All calculations were performed using D. Functional Theory (DFT) both BP86 and B3LYP levels of theory and 6-311G (p,d) basis set. The N-C4 bond order and charge on the reaction site play significant roles in hydrolysis reaction’s rate. The experimental process involved the reaction of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone(cas: 67914-60-7).Reference of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone

The Article related to hydrolysis electrochem oxidation aminophenol derivative acidic medium, Electrochemistry: Electrodes, Electrode Reactions, and Electrode Potentials and other aspects.Reference of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

On October 31, 2016, Bayrak, Riza; Akcay, Hakki Turker; Biyiklioglu, Zekeriya; Degirmencioglu, Ismail published an article.Quality Control of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone The title of the article was Substituted phthalocyanines and their electropolymerization properties. And the article contained the following:

New metal-free and metallo-phthalocyanine complexes (Co, TiO) were synthesized using a piperazine-substituted phthalonitrile derivative All proposed structures were supported by instrumental methods. Electrochem. studies of H2-Pc, TiIVOPc, and CoIIPc were examined using cyclic voltammetry (CV) and square-wave voltammetry (SWV) techniques. Voltammetric analyses of phthalocyanines supported the proposed structure of the synthesized complexes. All studied phthalocyanines were oxidatively electropolymerized on the working electrode during the repetitive anodic potential scans. The experimental process involved the reaction of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone(cas: 67914-60-7).Quality Control of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone

The Article related to phthalocyanine electropolymerization oxidation reduction property, Electrochemistry: Electrodes, Electrode Reactions, and Electrode Potentials and other aspects.Quality Control of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Amani, Amene; Khazalpour, Sadegh; Nematollahi, Davood published an article in 2012, the title of the article was Electrochemical oxidation of 4-(piperazin-1-yl)phenols in the presence of indole derivatives: The unique regioselectivity in the synthesis of highly conjugated bisindolyl-p-quinone derivatives.Recommanded Product: 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone And the article contains the following content:

The electrochem. oxidation of 4-(piperazin-1-yl)phenols were studied in the presence of indole derivatives as nucleophiles in H2O/MeCN mixture by cyclic voltammetry and controlled-potential coulometry. The reaction mechanism is believed to be oxidation of 4-(piperazin-1-yl)phenols, Michael addition reaction, oxidation of the formed adduct, another Michael addition reaction, oxidation of new adduct and hydrolysis (ECECEC). Bisindolyl-p-quinones were synthesized through the regioselective addition of indoles to electrochem. generated quinone imines in good yields at C electrode in a divided cell. The experimental process involved the reaction of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone(cas: 67914-60-7).Recommanded Product: 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone

The Article related to electrooxidation piperazinylphenol indole derivative regioselectivity electrosynthesis conjugated bisindolyl quinone, Electrochemistry: Nonindustrial Electrochemical Syntheses and Preparations and other aspects.Recommanded Product: 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics