Tag: M.W=250-300

Wang, Guangjun published the artcileAn efficient synthesis of ABT-263, a novel inhibitor of antiapoptotic Bcl-2 proteins, Synthetic Route of 187669-28-9, the main research area is ABT263 Bcl2 protein inhibitor preparation.

ABT-263, a newly developed Bcl-2 inhibitor, was efficiently synthesized. The key intermediates 4-(4-{[2-(4-chlorophenyl)-5,5-dimethylcyclohex-1-enyl]methyl}piperazin-1-yl)benzoic acid and 4-fluoro-3-[(trifluoromethyl)sulfonyl]benzenesulfonamide were efficiently prepared by a 3-component Mannich reaction and by nucleophilic fluorination of 1-nitro-2-[(trifluoromethyl)sulfonyl]benzene as the key steps, resp. Our work may lay a foundation for a new process development of this promising anticancer drug candidate.

Synthesis published new progress about Bcl-2 proteins Role: NUU (Other Use, Unclassified), USES (Uses) (inhibitors of). 187669-28-9 belongs to class piperazines, name is tert-Butyl 4-(piperazin-1-yl)benzoate, and the molecular formula is C15H22N2O2, Synthetic Route of 187669-28-9.

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

Scattolin, Thomas published the artcileA Nucleophilic Deprotection of Carbamate Mediated by 2-Mercaptoethanol, HPLC of Formula: 187669-28-9, the main research area is carbamate mercaptoethanol nucleophilic deprotection; secondary amine preparation.

Carbamates, typically used for the protection of amines, including Cbz, Alloc, and Me carbamate, was readily deprotected by treatment with 2-mercaptoethanol in the presence of potassium phosphate tribasic in N,N-dimethylacetamide at 75°C. This nucleophilic deprotection protocol was superior to the standard hydrogenolysis or Lewis acid-mediated deprotection conditions for substrates bearing a functionality sensitive to these more traditional methods.

Organic Letters published new progress about Free energy. 187669-28-9 belongs to class piperazines, name is tert-Butyl 4-(piperazin-1-yl)benzoate, and the molecular formula is C15H22N2O2, HPLC of Formula: 187669-28-9.

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

Nishizawa, Akihiro; Takahira, Tsuyoshi; Yasui, Kosuke; Fujimoto, Hayato; Iwai, Tomohiro; Sawamura, Masaya; Chatani, Naoto; Tobisu, Mamoru published the artcile< Nickel-Catalyzed Decarboxylation of Aryl Carbamates for Converting Phenols into Aromatic Amines>, Computed Properties of 197638-83-8, the main research area is phenol conversion aromatic amine nickel catalyzed decarboxylation carbamate; polystyrene supported phosphine ligand nickel catalyzed decarboxylation carbamate.

Herein, we describe a new catalytic approach to accessing aromatic amines from an abundant feedstock, namely phenols. The most reliable catalytic method for converting phenols to aromatic amines uses an activating group, such as a trifluoromethane sulfonyl group. However, this activating group is eliminated as a leaving group during the amination process, resulting in significant waste. Our nickel-catalyzed decarboxylation reaction of aryl carbamates forms aromatic amines with carbon dioxide as the only byproduct. As this amination proceeds in the absence of free amines, a range of functionalities, including a formyl group, are compatible. A bisphosphine ligand immobilized on a polystyrene support (PS-DPPBz) is key to the success of this reaction, generating a catalytic species that is significantly more active than simple nonsupported variants.

Journal of the American Chemical Society published new progress about Amination (decarboxylative amination). 197638-83-8 belongs to class piperazines, and the molecular formula is C16H22N2O3, Computed Properties of 197638-83-8.

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

Bavetsias, Vassilios; Crumpler, Simon; Sun, Chongbo; Avery, Sian; Atrash, Butrus; Faisal, Amir; Moore, Andrew S.; Kosmopoulou, Magda; Brown, Nathan; Sheldrake, Peter W.; Bush, Katherine; Henley, Alan; Box, Gary; Valenti, Melanie; Brandon, Alexis de Haven; Raynaud, Florence I.; Workman, Paul; Eccles, Suzanne A.; Bayliss, Richard; Linardopoulos, Spiros; Blagg, Julian published the artcile< Optimization of Imidazo[4,5-b]pyridine-Based Kinase Inhibitors: Identification of a Dual FLT3/Aurora Kinase Inhibitor as an Orally Bioavailable Preclinical Development Candidate for the Treatment of Acute Myeloid Leukemia>, Electric Literature of 197638-83-8, the main research area is imidazopyridine FLT3 Aurora kinase inhibitor preparation orally bioavailable; antitumor activity imidazopyridine acute myeloid leukemia.

Optimization of the imidazo[4,5-b]pyridine-based series of Aurora kinase inhibitors led to the identification of 6-chloro-7-(4-(4-chlorobenzyl)piperazin-1-yl)-2-(1,3-dimethyl-1H-pyrazol-4-yl)-3H-imidazo[4,5-b]pyridine (I), a potent inhibitor of Aurora kinases (Aurora-A Kd = 7.5 nM, Aurora-B Kd = 48 nM), FLT3 kinase (Kd = 6.2 nM), and FLT3 mutants including FLT3-ITD (Kd = 38 nM) and FLT3(D835Y) (Kd = 14 nM). FLT3-ITD causes constitutive FLT3 kinase activation and is detected in 20-35% of adults and 15% of children with acute myeloid leukemia (AML), conferring a poor prognosis in both age groups. In an in vivo setting, I strongly inhibited the growth of a FLT3-ITD-pos. AML human tumor xenograft (MV4-11) following oral administration, with in vivo biomarker modulation and plasma free drug exposures consistent with dual FLT3 and Aurora kinase inhibition. Compound I, an orally bioavailable dual FLT3 and Aurora kinase inhibitor, was selected as a preclin. development candidate for the treatment of human malignancies, in particular AML, in adults and children.

Journal of Medicinal Chemistry published new progress about Acute myeloid leukemia. 197638-83-8 belongs to class piperazines, and the molecular formula is C16H22N2O3, Electric Literature of 197638-83-8.

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

Wang, Lun; Cai, Xiaoying; Shi, Mingsong; Xue, Linlin; Kuang, Shuang; Xu, Ruiling; Qi, Wenyan; Li, Yan; Ma, Xu; Zhang, Ruijia; Hong, Feng; Ye, Haoyu; Chen, Lijuan published the artcile< Identification and optimization of piperine analogues as neuroprotective agents for the treatment of Parkinson's disease via the activation of Nrf2/keap1 pathway>, Formula: C16H22N2O3, the main research area is piperine analog preparation neuroprotective Parkinsons disease treatment; MPTP; Nrf2 activation; Parkinson’s disease; Piperine analogues.

Parkinson’s disease (PD) is a slowly progressive and complex neurodegenerative disorder. Up to date, there are no approved drugs that could slow or reverse the neurodegenerative process of PD. Here, we reported the synthesis of series of piperine analogs and the evaluation of their neuroprotective effects against hydrogen peroxide (H2O2) induced damage in the neuron-like PC12 cells. Among these analogs, I exhibited the most potent protection effect and its underlying mechanism was further investigated. Further results indicated that the ROS scavenging and cytoprotection effect of I might be related to the Nrf2 activation and upregulation of related phase II antioxidant enzymes, such as HO-1 and NQO1. In in vivo study, oral administration (100 mg/kg) of I significantly attenuated PD-associated behavioral deficits in a 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)-induced mouse model of PD and protected tyrosine hydroxylase-immunopos. dopaminergic neurons. Our results provided evidence that I might be a promising candidate for Parkinson’s disease treatment.

European Journal of Medicinal Chemistry published new progress about Antiparkinsonian agents. 197638-83-8 belongs to class piperazines, and the molecular formula is C16H22N2O3, Formula: C16H22N2O3.

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

Bavetsias, Vassilios; Large, Jonathan M.; Sun, Chongbo; Bouloc, Nathalie; Kosmopoulou, Magda; Matteucci, Mizio; Wilsher, Nicola E.; Martins, Vanessa; Reynisson, Johannes; Atrash, Butrus; Faisal, Amir; Urban, Frederique; Valenti, Melanie; Brandon, Alexis de Haven; Box, Gary; Raynaud, Florence I.; Workman, Paul; Eccles, Suzanne A.; Bayliss, Richard; Blagg, Julian; Linardopoulos, Spiros; McDonald, Edward published the artcile< Imidazo[4,5-b]pyridine Derivatives As Inhibitors of Aurora Kinases: Lead Optimization Studies toward the Identification of an Orally Bioavailable Preclinical Development Candidate>, HPLC of Formula: 197638-83-8, the main research area is imidazopyridine derivative arsenic inhibitor Aurora kinase orally bioavailable development.

Lead optimization studies using an imidazo[4,5-b]pyridinylpiperazine as the starting point led to a new class of imidazo[4,5-b]pyridine-based inhibitors of Aurora kinases that possessed the 1-benzylpiperazinyl motif at the 7-position, and displayed favorable in vitro properties. Cocrystn. of Aurora-A with a morpholinylmethylphenylimidazopyridinyl chlorobenzyl piperazine (CCT137444) provided a clear understanding into the interactions of this novel class of inhibitors with the Aurora kinases. Subsequent physicochem. property refinement by the incorporation of solubilizing groups led to the identification of 3-((4-(6-bromo-2-(4-(4-methylpiperazin-1-yl)phenyl)-3H-imidazo[4,5-b]pyridin-7-yl)piperazin-1-yl)methyl)-5-methylisoxazole (CCT137690)(I) which is a potent inhibitor of Aurora kinases (Aurora-A IC50 = 0.015±0.003 μM, Aurora-B IC50 = 0.025 μM, Aurora-C IC50 = 0.019 μM). I is highly orally bioavailable, and in in vivo efficacy studies it inhibited the growth of SW620 colon carcinoma xenografts following oral administration with no observed toxicities as defined by body weight loss.

Journal of Medicinal Chemistry published new progress about Antitumor agents. 197638-83-8 belongs to class piperazines, and the molecular formula is C16H22N2O3, HPLC of Formula: 197638-83-8.

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

Allan, Pia N. M.; Ostrowska, Martyna I.; Patel, Bhaven published the artcile< Acetic Acid Catalyzed One-Pot Synthesis of Pyrrolo[1,2- a ]quinoxaline Derivatives>, Safety of 1-Boc-4-(4-Formylphenyl)piperazine, the main research area is pyrroloquinoxaline preparation; benzaldehyde pyrrolylaniline Pictet Spengler reaction acetic acid catalyst.

An efficient acetic acid catalyzed reaction has been developed for the synthesis of 4-aryl substituted pyrrolo[1,2-a]quinoxalines I (R = H, 8-Me, 7-CF3, etc.; Ar = Ph, 2-MeOC6H4, 4-MeC6H4, etc.) from readily available starting materials. A range of structures have been synthesized in very good to excellent yields. The one-pot reaction proceeds through imine formation, cyclization followed by air oxidation

Synlett published new progress about Aromatic heterocyclic amines Role: RCT (Reactant), RACT (Reactant or Reagent). 197638-83-8 belongs to class piperazines, and the molecular formula is C16H22N2O3, Safety of 1-Boc-4-(4-Formylphenyl)piperazine.

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

Chopin, Nicolas; Yanai, Hikaru; Iikawa, Shinya; Pilet, Guillaume; Bouillon, Jean-Philippe; Medebielle, Maurice published the artcile< A Rapid Entry to Diverse γ-Ylidenetetronate Derivatives through Regioselective -Bromination of Tetronic Acid Derived γ-Lactones and Metal-Catalyzed Postfunctionalization>, Product Details of C16H22N2O3, the main research area is furanone tetronate preparation crystal mol structure.

The synthesis of a series of diverse Me and benzyl γ-ylidenetetronate derivatives was accomplished through the condensation of Me and benzyl tetronates with (hetero)aryl aldehydes in a new two-step or three-step aldolization/dehydration sequence. The bromination of Me and benzyl γ-ylidenetetronates occurred under mild conditions to provide the corresponding C-3-brominated γ-unsaturated lactones. Di- and tribrominated γ-lactones were prepared under slightly different conditions. Some brominated materials were employed in representative Stille, Suzuki-Miyaura , and Sonogashira cross-coupling reactions to yield functionalized Me and benzyl γ-ylidenetetronate derivatives Compounds that resulted from the Sonogashira cross-coupling reactions were desilylated and converted into 1,2,3-triazole derivatives through a copper(I)-catalyzed 1,3-dipolar cycloaddition reaction with benzyl azide. The synthesis of the target compounds was achieved by a reaction of 4-methoxy-2(5H)-furanone (Me tetronate), 4-(phenylmethoxy)-2(5H)-furanone (benzyl tetronate) with aldehydes. The title compounds thus formed included (5Z)-4-methoxy-5-(phenylmethylene)-2(5H)-furanone and related substances.

European Journal of Organic Chemistry published new progress about Aldehydes Role: RCT (Reactant), RACT (Reactant or Reagent). 197638-83-8 belongs to class piperazines, and the molecular formula is C16H22N2O3, Product Details of C16H22N2O3.

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

Bhattacharyya, Bhaswati; Dhara, Kaliprasanna published the artcile< Highly efficient, mild, one pot synthesis of 2-substituted benzimidazoles, benzothiazoles and pyridoimidazoles promoted by N-iodosuccinimide>, Related Products of 197638-83-8, the main research area is benzimidazole benzothiazole imidazopyridine preparation.

A common and highly efficient metal-free route for the synthesis of 2-substituted benzimidazoles, benzothiazoles and pyridoimidazoles from suitable 1,2- functionalized aromatic compounds and various aromatic and aliphatic aldehydes and ferrocenecarboxaldehyde was developed using 1-iodo-2,5-pyrrolidinedione, (N-iodosuccinimide) as the oxidizing agent. The methodol. involved very short reaction time, mild reaction procedure and easy work-up as well as excellent yields of the products. The synthesis of the target compounds was achieved by a reaction of 1,2-benzenediamine, 2-aminobenzenethiol, 2,3-pyridinediamine with aldehydes, such as benzaldehyde derivatives, 4-formylbenzonitrile, 1,3-benzodioxole-5-carboxaldehyde, citronellal, (formyl)ferrocene. The title compounds thus formed included 2-phenyl-1H-benzimidazole, 2-phenylbenzothiazole, (4-methyl-1H-benzimidazol-2-yl)ferrocene, 2-phenyl-3H-imidazo[4,5-b]pyridine derivatives

Journal of the Indian Chemical Society published new progress about Aliphatic aldehydes Role: RCT (Reactant), RACT (Reactant or Reagent). 197638-83-8 belongs to class piperazines, and the molecular formula is C16H22N2O3, Related Products of 197638-83-8.

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

De-la-Torre, Pedro; Treuer, Adriana V.; Gutierrez, Margarita; Poblete, Horacio; Alzate-Morales, Jans H.; Trilleras, Jorge; Astudillo-Saavedra, Luis; Caballero, Julio published the artcile< Synthesis and in silico analysis of the quantitative structure-activity relationship of heteroaryl-acrylonitriles as AChE inhibitors>, Name: 1-Boc-4-(4-Formylphenyl)piperazine, the main research area is AChE inhibitor antiAlzheimers agent mol docking QSAR Alzheimers disease.

Alzheimer disease (AD) is a neurodegenerative disorder that causes damages in brain due to factors such as oxidative stress, low-levels of the neurotransmitter acetylcholine, β-amyloid protein aggregation, etc. It is necessary the design of novel efficient drugs for AD treatment to counteract the increase of people suffering from AD. Recently, heteroaryl-acrylonitrile derivatives have emerged as a new family of acetylcholinesterase inhibitors (AChEIs). The anal. of the structure-activity relationship of these compounds could help to elucidate the main mol. features that contribute to the activity of these compounds In this paper, we performed 3D-QSAR analyses through a Comparative Similarity Indexes Anal. (CoMSIA) to determine the key-factors for the activity of E/Z-heteroaryl-acrylonitriles reported in literature and novel derivatives that are reported in this work for the first time. The novel derivatives were synthesized in order to enlarge the library of compounds available in literature. They were synthesized via microwave-assisted Knoevenagel reaction and their biol. activities as AChE/BuChE inhibitors were explored by the Ellman’s spectrophotometric method. The best CoMSIA model included both electrostatic and hydrogen bond donor fields (CoMSIA-ED model) and provided the best statistical results with a highest Q2 value of 0.901. The model also had satisfactory predictions of external compounds Our in silico study provided a new tool for predicting the affinity of heteroaryl-acrylonitriles as AChEIs to the scientific community. It can be used for guiding the design and synthesis of novel, selective, and more potent AChEIs.

Journal of the Taiwan Institute of Chemical Engineers published new progress about Alzheimer disease. 197638-83-8 belongs to class piperazines, and the molecular formula is C16H22N2O3, Name: 1-Boc-4-(4-Formylphenyl)piperazine.

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