Tag: 200-300

Molecular iodine-catalyzed facile procedure for N-Boc protection of amines was written by Varala, Ravi;Nuvula, Sreelatha;Adapa, Srinivas R.. And the article was included in Journal of Organic Chemistry in 2006.Application of 780705-64-8 This article mentions the following:

An efficient and practical protocol for the protection of various structurally and electronically divergent aryl and aliphatic amines using (Boc)₂O in the presence of a catalytic amount of mol. iodine under solvent-free conditions at ambient temperature is presented. In the experiment, the researchers used many compounds, for example, tert-Butyl 4-(pyrimidin-2-yl)piperazine-1-carboxylate (cas: 780705-64-8Application of 780705-64-8).

tert-Butyl 4-(pyrimidin-2-yl)piperazine-1-carboxylate (cas: 780705-64-8) belongs to piperazine derivatives. Piperazine was first introduced as an anthelmintic in 1953. Piperazine compounds mediate their anthelmintic action by generally paralyzing parasites, allowing the host body to easily remove or expel the invading organism. Intermediate for a wide range of pharmaceuticals, polymers, dyes, corrosion inhibitors, rubber accelerators and surfactants.Application of 780705-64-8

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

An improved synthesis of the 5-HT1A receptor agonist Eptapirone free base was written by Peng, Wei;Chen, Jian;Liu, Hui;Li, Xiufang;Deng, Zhiwei;Yuan, Jing;Peng, Yizhou;Yang, Yanjing;Zhong, Shian. And the article was included in Chemical Papers in 2019.HPLC of Formula: 780705-64-8 This article mentions the following:

A method to retro-synthesize eptapirone free base. The compound consists of heterocyclic aromatic portion and aliphatic portion, and the synthetic route consisted of a total of nine steps with an overall yield of 8.8% starting from the com. available materials. The key steps in the synthetic method involved: (1) using sodium hydroxide and ethylene glycol as solvent resulted in a better cyclization and yield (61.6%) of 1,2,4-triazine-3,5(2H,4H)-dione; (2) an acceptable yield (63.1%) of 4-tert-butyl(pyrimidin-2-yl)piperazine-1-carboxylate was obtained under an optimized conditions of using triethylamine as a base, ethanol as a solvent, and a reaction temperature of 50 闁硅櫣鐓?for 16 h with non-metal catalysis and less byproducts; (3) the reaction step of eptapirone could get a better yield (49.6%) with an optimized condition of potassium carbonate as a base, acetonitrile as a solvent, NaI as a catalyst, and a reaction temperature of 50 闁硅櫣鐓?for 12 h by nucleophilic substitution reaction. The main advantages of this route were an acceptable product purity, the com. availability of all starting materials and the absence of high temperature, high pressure and noble metal catalysts, which could result in more feasible com. applications. In the experiment, the researchers used many compounds, for example, tert-Butyl 4-(pyrimidin-2-yl)piperazine-1-carboxylate (cas: 780705-64-8HPLC of Formula: 780705-64-8).

tert-Butyl 4-(pyrimidin-2-yl)piperazine-1-carboxylate (cas: 780705-64-8) belongs to piperazine derivatives. Industrial applications of piperazine include the manufacture of plastics, resins, pesticides and brake fluids. Although many piperazine derivatives occur naturally, piperazine itself can be synthesized by reacting alcoholic ammonia with 1,2-dichloroethane, by the action of sodium and ethylene glycol on ethylene diamine hydrochloride, or by reduction of pyrazine with sodium in ethanol.HPLC of Formula: 780705-64-8

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

YAP-dependent proliferation by a small molecule targeting annexin A2 was written by Shalhout, Sophia Z.;Yang, Peng-Yu;Grzelak, Edyta M.;Nutsch, Kayla;Shao, Sida;Zambaldo, Claudio;Iaconelli, Jonathan;Ibrahim, Lara;Stanton, Caroline;Chadwick, Stormi R.;Chen, Emily;DeRan, Michael;Li, Sijia;Hull, Mitchell;Wu, Xu;Chatterjee, Arnab K.;Shen, Weijun;Camargo, Fernando D.;Schultz, Peter G.;Bollong, Michael J.. And the article was included in Nature Chemical Biology in 2021.Computed Properties of C12H25N3O2 This article mentions the following:

Abstract: The transcriptional coactivator Yes-associated protein 1 (YAP) orchestrates a pro-proliferative transcriptional program that controls the fate of somatic stem cells and the regenerative responses of certain tissues. As such, agents that activate YAP may hold therapeutic potential in disease states exacerbated by insufficient proliferative repair. Here we report the discovery of a small mol., termed PY-60, which robustly activates YAP transcriptional activity in vitro and promotes YAP-dependent expansion of epidermal keratinocytes in mouse following topical drug administration. Chem. proteomics revealed the relevant target of PY-60 to be annexin A2 (ANXA2), a protein that directly associates with YAP at the cell membrane in response to increased cell d. PY-60 treatment liberates ANXA2 from the membrane, ultimately promoting a phosphatase-bound, nonphosphorylated and transcriptionally active form of YAP. This work reveals ANXA2 as a previously undescribed, druggable component of the Hippo pathway and suggests a mechanistic rationale to promote regenerative repair in disease. In the experiment, the researchers used many compounds, for example, tert-Butyl 4-(3-aminopropyl)piperazine-1-carboxylate (cas: 373608-48-1Computed Properties of C12H25N3O2).

tert-Butyl 4-(3-aminopropyl)piperazine-1-carboxylate (cas: 373608-48-1) belongs to piperazine derivatives. Simple N-substituted piperazines have been found in many drug molecules. Piperazines are very broad chemical group, covering a wide range of drugs from antidepressants to antihistamines. The connecting property of all these chemicals is the presence of a piperazine functional group.Computed Properties of C12H25N3O2

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

Two Ligands Transfer from Ag to Pd: En Route to (SIPr)Pd(CF₂H)(X) and Its Application in One-Pot C-H Borylation/Difluoromethylation was written by Zhao, Haiwei;Herbert, Simon;Kinzel, Tom;Zhang, Wei;Shen, Qilong. And the article was included in Journal of Organic Chemistry in 2020.Recommanded Product: 780705-64-8 This article mentions the following:

A process for the concurrent transfer of both the NHC ligand and difluoromethyl group from [(SIPr)Ag(CF₂H)] to PdX₂ (X = Cl, OAc and OPiv) for the preparation [(SIPr)Pd(CF₂H)X] complexes is described. These complexes were air-stable and easily underwent transmetalation with aryl pinacol boronate/reductive elimination to generate ArCF₂H in high yields. Based on this discovery, the 1st 1-pot C-H borylation and difluoromethylation for the preparation of difluoromethylated (hetero)arenes was developed. In the experiment, the researchers used many compounds, for example, tert-Butyl 4-(pyrimidin-2-yl)piperazine-1-carboxylate (cas: 780705-64-8Recommanded Product: 780705-64-8).

tert-Butyl 4-(pyrimidin-2-yl)piperazine-1-carboxylate (cas: 780705-64-8) belongs to piperazine derivatives. Piperazine is a fairly basic compound and is an amine solvent. Intermediate for a wide range of pharmaceuticals, polymers, dyes, corrosion inhibitors, rubber accelerators and surfactants.Recommanded Product: 780705-64-8

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

The discovery of 6-amino nicotinamides as potent and selective histone deacetylase inhibitors was written by Hamblett, Christopher L.;Methot, Joey L.;Mampreian, Dawn M.;Sloman, David L.;Stanton, Matthew G.;Kral, Astrid M.;Fleming, Judith C.;Cruz, Jonathan C.;Chenard, Melissa;Ozerova, Nicole;Hitz, Anna M.;Wang, Hongmei;Deshmukh, Sujal V.;Nazef, Naim;Harsch, Andreas;Hughes, Bethany;Dahlberg, William K.;Szewczak, Alex A.;Middleton, Richard E.;Mosley, Ralph T.;Secrist, J. Paul;Miller, Thomas A.. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2007.Recommanded Product: 923565-99-5 This article mentions the following:

This communication highlights the development of a nicotinamide series of histone deacetylase inhibitors (e.g. I) within the benzamide structural class. Extensive exploration around the nicotinamide core led to the discovery of a class I selective HDAC inhibitor that possesses excellent intrinsic and cell-based potency, acceptable ancillary pharmacol., favorable pharmacokinetics, sustained pharmacodynamics in vitro, and achieves in vivo efficacy in an HCT116 xenograft model. In the experiment, the researchers used many compounds, for example, (R)-1-Cbz-2-methylpiperazine (cas: 923565-99-5Recommanded Product: 923565-99-5).

(R)-1-Cbz-2-methylpiperazine (cas: 923565-99-5) belongs to piperazine derivatives. Piperazine was first introduced as an anthelmintic in 1953. Piperazine compounds mediate their anthelmintic action by generally paralyzing parasites, allowing the host body to easily remove or expel the invading organism. Outside the body, piperazine has a remarkable power to dissolve uric acid and producing a soluble urate, but in clinical experience it has not proved equally successful. Recommanded Product: 923565-99-5

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

Modular click chemistry libraries for functional screens using a diazotizing reagent was written by Meng, Genyi;Guo, Taijie;Ma, Tiancheng;Zhang, Jiong;Shen, Yucheng;Sharpless, Karl Barry;Dong, Jiajia. And the article was included in Nature (London, United Kingdom) in 2019.Related Products of 373608-48-1 This article mentions the following:

Alkyl and aryl azides were prepared from the corresponding primary alkyl and aryl amines by reaction with fluorosulfonyl azide generated in situ from a fluorosulfonylimidazolium triflate and sodium azide, expanding access to azides and both to the 1,2,3-triazoles derived from them and to functional screens employing them. The method allowed the preparation of a library of >1000 azides from the corresponding amines; the azide library underwent copper-catalyzed azide-alkyne cycloaddition reactions to yield a library of >1000 1,2,3-triazoles. In the experiment, the researchers used many compounds, for example, tert-Butyl 4-(3-aminopropyl)piperazine-1-carboxylate (cas: 373608-48-1Related Products of 373608-48-1).

tert-Butyl 4-(3-aminopropyl)piperazine-1-carboxylate (cas: 373608-48-1) belongs to piperazine derivatives. Piperazine belongs to the family of medicines called anthelmintics. Two common salts in the form of which piperazine is usually prepared for pharmaceutical or veterinary purposes are the citrate, 3C4H10N2.2C6H8O7 (i.e. containing 3 molecules of piperazine to 2 molecules of citric acid), and the adipate, C4H10N2.C6H10O4 (containing 1 molecule each of piperazine and adipic acid).Related Products of 373608-48-1

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

Design, Synthesis, and Biological Evaluation of Mitochondria-Targeted Flavone-Naphthalimide-Polyamine Conjugates with Antimetastatic Activity was written by Dai, Fujun;Li, Qian;Wang, Yuxia;Ge, Chaochao;Feng, Chenyang;Xie, Songqiang;He, Haoying;Xu, Xiaojuan;Wang, Chaojie. And the article was included in Journal of Medicinal Chemistry in 2017.Synthetic Route of C12H25N3O2 This article mentions the following:

Approx. 90% of cancer-associated deaths result from disseminated tumors, indicating the ineffectiveness of current therapies and the imperative need of antimetastatic drugs. A novel pharmacophore with flavonoid and naphthalimide moieties was constructed by using a fragment-based drug design and a series of eight flavone-naphthalimide-polyamine conjugates were synthesized. In vitro evaluation revealed that compound I with a homospermidine motif displayed better cell selectivity between cancerous and normal liver cells than amonafide did. The in vivo assays on two hepatocellular carcinoma (HCC) models verified that I potently suppressed pulmonary metastasis with improved organ indexes compared to amonafide. Various experiments showed that I as a potential fluorescent chem. probe could target the mitochondria. Preliminary investigation into the mechanism of action of I indicated that it might harness a polyamine transporter for cell entrance, localize in the mitochondria, selectively cause reactive oxygen species (ROS) overproduction in hepatoma cells instead of normal liver cells, and finally lead to HCC cell apoptosis and migration inhibition via multiple ROS-mediated signaling pathways. In the experiment, the researchers used many compounds, for example, tert-Butyl 4-(3-aminopropyl)piperazine-1-carboxylate (cas: 373608-48-1Synthetic Route of C12H25N3O2).

tert-Butyl 4-(3-aminopropyl)piperazine-1-carboxylate (cas: 373608-48-1) belongs to piperazine derivatives. A form in which piperazine is commonly available industrially is as the hexahydrate, C4H10N2. 6H2O, which melts at 44 鎺矯 and boils at 125閳?30 鎺矯. Piperazine is an anthelminthic especially useful in the treatment of partial intestinal obstruction caused by Ascaris worms, which is a condition primarily seen in children. Piperazine hydrate and piperazine citrate are the main anthelminthic piperazines.Synthetic Route of C12H25N3O2

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

Synthesis of substituted 5-amino-3-aryl-4-(methoxycarbonyl)isoxazoles was written by Alyab’ev, S. B.;Kosul’nikova, T. S.;Dmitriev, D. E.;Il’in, A. P.;Kravchenko, D. V.;Filimonov, S. I.;Ivashchenko, A. V.. And the article was included in Izvestiya Vysshikh Uchebnykh Zavedenii, Khimiya i Khimicheskaya Tekhnologiya in 2007.Category: piperazines This article mentions the following:

A combinatorial library of substituted 5-amino-3-aryl-4-(methoxycarbonyl)isoxazoles was obtained by reaction of 3-aryl-4-methoxycarbonyl-5-chloroisoxazoles with primary and secondary amines in 1,4-dioxane in the presence of NEt₃ under parallel synthesis conditions. Products were obtained in yields of 21-95%. This reaction proceeds less uniformly in DMF in the presence of K₂CO₃, and, in the case of primary amines, bis(4-methoxycarbonyl-3-aryl-isoxazol-5-yl)arylamines are also formed in 20-69% yields. In the experiment, the researchers used many compounds, for example, 4-(4-Ethylpiperazin-1-ylmethyl)phenylamine (cas: 611225-86-6Category: piperazines).

4-(4-Ethylpiperazin-1-ylmethyl)phenylamine (cas: 611225-86-6) belongs to piperazine derivatives. A form in which piperazine is commonly available industrially is as the hexahydrate, C4H10N2. 6H2O, which melts at 44 鎺矯 and boils at 125閳?30 鎺矯. Piperazines are very broad chemical group, covering a wide range of drugs from antidepressants to antihistamines. The connecting property of all these chemicals is the presence of a piperazine functional group.Category: piperazines

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

Discovery of new thieno[3,2-d]pyrimidine derivatives targeting EGFR^L858R/T790M NSCLCs by the conformation constrained strategy was written by Chen, Yang;Yang, Linlin;Qiao, Hui;Cheng, Zhongyu;Xie, Jiahao;Zhou, Wenjuan;Huang, Xin;Jiang, Yaoxuan;Yu, Bin;Zhao, Wen. And the article was included in European Journal of Medicinal Chemistry in 2020.Related Products of 611225-86-6 This article mentions the following:

Studies on the third-generation of epidermal growth factor receptor tyrosine kinase inhibitors (EGFRTKIs) targeting EGFR^L858R/T790M mutant remain hotspots, specifically for non-small cell lung cancer(NSCLC) were described. In the current study, a new series of EGFR-TKIs with thieno[3,2-d]pyrimidine derivatives bearing quinolin-2(1H)-ones I (R = 4-fluoro-phenylamino, 4-(4-methyl-piperazin-1-yl)-phenylamino, 4-morpholin-4-ylmethyl-phenylamino, etc.) was designed and synthesized, through conformational constrained strategy from the third generation of EGFR-TKI olmutinib. In vitro structure-activity relationship (SAR) studies indicated that compounds I (R = 4-(4-methyl-piperazin-1-yl)-phenylamino, 4-[1,4′]bipiperidinyl-1′-yl-3-fluoro-phenylamino, 4-(4-methyl-piperazin-1-ylmethyl)-phenylamino, 4-(4-ethyl-piperazin-1-ylmethyl)-phenylamino, 4-(2-(dimethylamino)ethylamino)-3-fluorophenylamino) exhibited good selective inhibition to EGFR^L858R/T790M (IC₅₀ 閳?250 nM) over wild type EGFR (IC₅₀ > 10000 nM). The observed selectivity of compounds I (R = 4-[1,4′]bipiperidinyl-1′-yl-3-fluoro-phenylamino, 4-(2-(dimethylamino)ethylamino)-3-fluorophenylamino) (A) was also proved by the computational mol. docking and the cellular thermal shift assay. These compounds I had good growth inhibitory effect on the four tested cancer cell lines. Specifically, I (R = 4-(2-(dimethylamino)ethylamino)-3-fluorophenylamino) could significantly inhibit the colony formation, wound healing and the expression of p-EGFR and its downstream p-ERK in EGFR^L858R/T790M H1975 lung cancer cells. The above finding results suggest that the thieno[3,2-d]pyrimidine compounds, especially compounds A, can selectively target the mutant EGFR^L858R/T790M in vitro and at cellular level and may serve as the lead compounds for generating new series of the third generation EGFR-TKIs. In the experiment, the researchers used many compounds, for example, 4-(4-Ethylpiperazin-1-ylmethyl)phenylamine (cas: 611225-86-6Related Products of 611225-86-6).

4-(4-Ethylpiperazin-1-ylmethyl)phenylamine (cas: 611225-86-6) belongs to piperazine derivatives. Piperazine belongs to the family of medicines called anthelmintics. Piperazine and its salts did not induce point mutations in a bacterial test. A series of mutagenicity studies in cells, both in vitro and in vivo, has been completed and showed no evidence of mutagenic effect.Related Products of 611225-86-6

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

Iridium-Catalyzed C-H Borylation of Heteroarenes: Scope, Regioselectivity, Application to Late-Stage Functionalization, and Mechanism was written by Larsen, Matthew A.;Hartwig, John F.. And the article was included in Journal of the American Chemical Society in 2014.SDS of cas: 780705-64-8 This article mentions the following:

A study on the iridium-catalyzed C-H borylation of heteroarenes is reported. Several heteroarenes containing multiple heteroatoms were amenable to C-H borylation catalyzed by the combination of an iridium(I) precursor and tetramethylphenanthroline. The investigations of the scope of the reaction led to the development of powerful rules for predicting the regioselectivity of borylation, foremost of which is that borylation occurs distal to nitrogen atoms. One-pot functionalizations are reported of the heteroaryl boronate esters formed in situ, demonstrating the usefulness of the reported methodol. for the synthesis of complex heteroaryl structures. Application of this methodol. to the synthesis and late-stage functionalization of biol. active compounds is also demonstrated. Mechanistic studies show that basic heteroarenes can bind to the catalyst and alter the resting state from the olefin-bound complex observed during arene borylation to a species containing a bound heteroarene, leading to catalyst deactivation. Studies on the origins of the observed regioselectivity show that borylation occurs distal to N-H bonds due to rapid N-H borylation, creating an unfavorable steric environment for borylation adjacent to these bonds. Computational studies and mechanistic studies show that the lack of observable borylation of C-H bonds adjacent to basic nitrogen is not the result of coordination to a bulky Lewis acid prior to C-H activation, but the combination of a higher-energy pathway for the borylation of these bonds relative to other C-H bonds and the instability of the products formed from borylation adjacent to basic nitrogen. In the experiment, the researchers used many compounds, for example, tert-Butyl 4-(pyrimidin-2-yl)piperazine-1-carboxylate (cas: 780705-64-8SDS of cas: 780705-64-8).

tert-Butyl 4-(pyrimidin-2-yl)piperazine-1-carboxylate (cas: 780705-64-8) belongs to piperazine derivatives. A form in which piperazine is commonly available industrially is as the hexahydrate, C4H10N2. 6H2O, which melts at 44 掳C and boils at 125鈥?30 掳C. Piperazine and its salts did not induce point mutations in a bacterial test. A series of mutagenicity studies in cells, both in vitro and in vivo, has been completed and showed no evidence of mutagenic effect.SDS of cas: 780705-64-8

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