Day: November 18, 2022

Sargent, Brendon T. published the artcileCobalt-Catalyzed Aminocarbonylation of Alkyl Tosylates: Stereospecific Synthesis of Amides, Name: tert-Butyl piperidin-4-ylcarbamate, the main research area is amide stereospecific synthesis cobalt catalyzed aminocarbonylation unactivated alkyl tosylate; alkyl tosylates; aminocarbonylation; cobalt; homogenous catalysis; synthetic methods.

Metal-catalyzed aminocarbonylation is a standard approach for installing amide functionality in chem. synthesis. Despite broad application of this transformation using aryl or vinyl electrophiles, there are few examples involving unactivated aliphatic substrates. Furthermore, there are no stereocontrolled aminocarbonylations of alkyl electrophiles known. Herein, we report a stereospecific aminocarbonylation of unactivated alkyl tosylates for the synthesis of enantioenriched amides. This cobalt-catalyzed transformation uses a remarkably broad range of amines and proceeds with excellent stereospecificity and chemoselectivity.

Angewandte Chemie, International Edition published new progress about Acylation. 73874-95-0 belongs to class piperidines, name is tert-Butyl piperidin-4-ylcarbamate, and the molecular formula is C10H20N2O2, Name: tert-Butyl piperidin-4-ylcarbamate.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Bae, Jinsu published the artcileSynthesis and Structure-Activity Relationship Studies of Benzimidazole-4,7-dione-Based P2X3 Receptor Antagonists as Novel Anti-Nociceptive Agents, Computed Properties of 73874-95-0, the main research area is neuropathic pain antinociceptive structure activity relationship; P2X3 receptor; adenosine 5′-triphosphate; antagonist; anti-nociceptive agents; neuropathic pain; structure−activity relationship study.

P2X3 receptors (P2X3R) are ATP-gated ion channels predominantly expressed in C- and Aδ-fiber primary afferent neurons and have been introduced as a novel therapeutic target for neurol. disorders, including neuropathic pain and chronic cough. Because of its localized distribution, antagonism of P2X3R has been thoroughly considered, and the avoidance of issues related to CNS side effects has been proven in clin. trials. In this article, benzimidazole-4,7-dione-based derivatives were introduced as a new chem. entity for the development of P2X3R antagonists. Starting from the discovery of a hit compound from the screening of 8364 random library compounds in the Korea Chem. Bank, which had an IC50 value of 1030 nM, studies of structure-activity and structure-property relationships enabled further optimization toward improving the antagonistic activities as well as the drug′s physicochem. properties, including metabolic stability. As for the results, the final optimized compound 14h was developed with an IC50 value of 375 nM at P2X3R with more than 23-fold selectivity vs. P2X2/3R, along with properties of metabolic stability and improved solubility In neuropathic pain animal models evoked by either nerve ligation or chemotherapeutics in male Sprague-Dawley rats, compound 14h showed anti-nociceptive effects through an increase in the mech. withdrawal threshold as measured by von Frey filament following i.v. administration.

Molecules published new progress about Analgesics. 73874-95-0 belongs to class piperidines, name is tert-Butyl piperidin-4-ylcarbamate, and the molecular formula is C10H20N2O2, Computed Properties of 73874-95-0.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Agarwal, Jyoti published the artcileWater-mediated, highly-efficient and improved protocol for the synthesis of vesamicol, its analogues and β-blockers through the highly-chemoselective aminolysis of epoxides, COA of Formula: C18H23NO2, the main research area is vesamicol analog green preparation diastereoselective; epoxide aryl piperidine chemoselective aminolysis water mediated.

An efficient, eco-friendly and cost-effective protocol was developed for the synthesis of vesamicol e.g., I, benzovesamicol, spirovesamicol, their analogs and drug mols. such as Naftopidil and SR 59230 A. In this reaction, water had played dual role i.e. of bifunctional catalyst and reaction medium, also no other chem. reagent/promotor was required to afford the products. Reaction follows 100% atom economy and was found to be highly chemo-selective. All studied reactions worked well to yield the corresponding products in excellent to near quant. yields without following the tedious and time consuming column chromatog. as purification step. Thus, this protocol provided the vesamicol and other products without generating any chem. waste to the environment.

ChemistrySelect published new progress about Aminolysis. 137419-24-0 belongs to class piperidines, name is tert-Butyl spiro[indene-1,4′-piperidine]-1′-carboxylate, and the molecular formula is C18H23NO2, COA of Formula: C18H23NO2.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Gawley, Robert E. published the artcileAlkylation of 2-lithio-N-methylpiperidines and -pyrrolidines: scope, limitations, and stereochemistry, Formula: C8H15NO2, the main research area is alkylation lithio piperidine pyrrolidine stereochem.

The scope and limitations of the alkylation of racemic and nonracemic 2-lithiopiperidines and 2-lithiopyrrolidines, obtained by transmetalation of the corresponding stannanes, is reported. These organolithiums react with a variety of electrophiles to afford 2-substituted pyrrolidines and piperidines in excellent yield. With primary alkyl halides the reaction proceeds with net inversion of configuration at the metal-bearing carbon in the piperidines; in the pyrrolidines there is a mixture of inversion and retention, with the former predominating. With most carbonyl electrophiles (carbon dioxide, di-Me carbonate, Me chloroformate, pivaloyl chloride, benzaldehyde, and dialkyl ketones), retention is observed in both cases. Electrophiles such as benzophenone, benzyl bromide, and tert-Bu bromoacetate afford racemic coupling products. A mechanistic interpretation is presented.

Journal of Organic Chemistry published new progress about Alkylation. 1690-74-0 belongs to class piperidines, name is Methyl 1-methylpiperidine-2-carboxylate, and the molecular formula is C8H15NO2, Formula: C8H15NO2.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Giancola, JoLynn B. published the artcileStructure-activity relationships for a series of (Bis(4-fluorophenyl)methyl)sulfinylethyl-aminopiperidines and -piperidine amines at the dopamine transporter: Bioisosteric replacement of the piperazine improves metabolic stability, Synthetic Route of 73874-95-0, the main research area is aminopiperidine piperidine amine preparation dopamine transporter SAR; Atypical dopamine uptake inhibitors; Cocaine; DAT; Modafinil; NET; Psychostimulant use disorders; SERT; Sigma receptors.

The bioisosteric substitutions of the piperazine ring were explored with a series of aminopiperidines and piperidine amines wherein compounds with either a terminal tertiary amine or amide were synthesized. Several lead compounds showed high to moderate DAT affinities and metabolic stability in rat liver microsomes. N-(2-((bis(4-fluorophenyl)methyl)sulfinyl)ethyl)-1-(4-fluorobenzyl)piperidin-4-amine (DAT Ki = 50.6 nM), I [R= F] (DAT Ki = 77.2 nM) and II [X1=X2= F] (DAT Ki = 30.0 nM) produced only minimal stimulation of ambulatory activity in mice, compared to cocaine, suggesting an atypical DAT inhibitor profile.

European Journal of Medicinal Chemistry published new progress about Alkylation. 73874-95-0 belongs to class piperidines, name is tert-Butyl piperidin-4-ylcarbamate, and the molecular formula is C10H20N2O2, Synthetic Route of 73874-95-0.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Zeng, Xiaojun published the artcileCopper-Catalyzed Decarboxylative Difluoromethylation, HPLC of Formula: 158922-07-7, the main research area is copper catalyzed decarboxylative difluoromethylation; difluoromethylation aliphatic carboxylic acid radical mechanism.

We report herein a highly efficient Cu-catalyzed protocol for the conversion of aliphatic carboxylic acids to the corresponding difluoromethylated analogs. This robust, operationally simple and scalable protocol tolerates a variety of functional groups and can convert a diverse array of acid-containing complex mols. to the alkyl-CF2H products. Mechanistic studies support the involvement of alkyl radicals.

Journal of the American Chemical Society published new progress about Alkylation. 158922-07-7 belongs to class piperidines, name is 1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-3-carboxylic acid, and the molecular formula is C21H21NO4, HPLC of Formula: 158922-07-7.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Valentukeviciene, Marina published the artcileFluoride Removal from Groundwater by Technological Process Optimization, Recommanded Product: Bis(2,2,6,6-tetramethylpiperidin-4-yl) decanedioate, the main research area is fluoride removal groundwater technol process optimization.

Fluoride removal from aqueous solutions was studied using nanofiltration and sorption techniques which have always been best key ways to deal with water contaminated by fluoride. In this presented work, we were firstly interested on fluoridated rejected water overcoming the drawback of RO membrane process of groundwater treatment plant in Baltic region (Kretinga, Lithuania). Opoka sorbent has shown effective results of fluoride sorption with efficiency higher than 77%. In order to understand the sorption phenomenon and to validate the results obtained, we have applied exptl. data on Freundlich and Langmuir isotherms which allow us to determine isotherms parameters (KF; 1/n and KL; qmax) and to confirm the experiment Because of the unacceptable tariff of drinking water treated by RO, defluoridation with nanofiltration method is proposed in this study as a solution which can replace reverse osmosis technique. For that, tests of nanofiltration for fluoride removal were carried out at laboratory scale by using nanofiltration flat sheet membranes (NF270 and NF90).

Ecological Chemistry and Engineering S published new progress about Adsorption. 52829-07-9 belongs to class piperidines, name is Bis(2,2,6,6-tetramethylpiperidin-4-yl) decanedioate, and the molecular formula is C28H52N2O4, Recommanded Product: Bis(2,2,6,6-tetramethylpiperidin-4-yl) decanedioate.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Lin, Yi-Li published the artcileUsing in situ modification to enhance organic fouling resistance and rejection of pharmaceutical and personal care products in a thin-film composite nanofiltration membrane, HPLC of Formula: 52829-07-9, the main research area is NF90 hydroxyethyl sulfopropyl methacrylate potassium personal care product antifouling; Adsorption; Antifouling; In situ modification; Modified Hermia model; Nanofiltration; Pharmaceutical and personal care products (PPCPs); Radical graft polymerization.

A com. available nanofiltration membrane, NF90, was modified using an in situ concentration polarization-enhanced radical graft polymerization method to improve the organic fouling resistance as well as the removal of pharmaceutical and personal care products (PPCPs), including ibuprofen (IBU), carbamazepine, sulfadiazine, sulfamethoxazole, sulfamethazine, and triclosan (TRI). 3-Sulfopropyl methacrylate potassium salt (SPM) and 2-hydroxyethyl methacrylate (HEMA) were used in various dosages for surface modification, and the extent of membrane modifications was quantified based on the degree of grafting. The modified NF90 exhibited a 15-40% lower flux during humic acid (HA) fouling and 25% greater NaCl rejection compared with the virgin membrane. PPCP rejection in the modified NF90 membranes before and after HA fouling was 20-45% and 5-20% greater, resp., compared with that of the virgin membrane. Both SPM and HEMA increased the hydrophilicity of NF90 by decreasing contact angles. SEM revealed lower amounts of foulants on the modified NF90 than on the virgin membrane. The main fouling mechanism for virgin NF90 was gel layer formation and those for modified NF90 were complete and intermediate blocking. Therefore, the modification of NF90 was effective for controlling organic fouling and strongly rejecting PPCPs.

Environmental Science and Pollution Research published new progress about Adsorption. 52829-07-9 belongs to class piperidines, name is Bis(2,2,6,6-tetramethylpiperidin-4-yl) decanedioate, and the molecular formula is C28H52N2O4, HPLC of Formula: 52829-07-9.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Ishida, Akiharu published the artcileDiscovery and SAR Studies of Orally Active Somatostatin Receptor Subtype-2 (SSTR2) Agonists for the Treatment of Acromegaly, Synthetic Route of 73874-95-0, the main research area is acromegaly somatostatin SSTR2 GPCR acromegaly nonpeptidic orally active SAR; GPCR; SSTR2; Somatostatin; acromegaly; nonpeptidic; orally active.

Acromegaly is a disease caused by the oversecretion of growth hormone. It is currently treated by i.v. injection with cyclic peptide drugs that activate somatostatin receptor subtype 2 (SSTR2). Here, novel nonpeptidic, small-mol., and orally active SSTR2 agonists were identified from a hit compound (13). Pharmacophore studies enabled scaffold hopping to obtain a unique 3,4,5-trisubstituted pyridine motif. Further optimization conferred potent SSTR2 agonistic activity and metabolic stability. Several compounds were evaluated and these showed good oral pharmacokinetic profiles in rats, and one representative compound (25)(I) showed highly potent inhibition of growth hormone secretion induced by growth hormone-releasing hormone in rats. Based on these results, 25 was identified as a promising lead for further optimization. A structure-activity relationship (SAR) study and the metabolic stability data for this compound are also described.

ACS Chemical Neuroscience published new progress about Acromegaly. 73874-95-0 belongs to class piperidines, name is tert-Butyl piperidin-4-ylcarbamate, and the molecular formula is C10H20N2O2, Synthetic Route of 73874-95-0.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Rus, Anika Zafiah M. published the artcileDeterioration rate of renewable polyurethanes composites prior to ultra violet irradiation exposure, Application of Bis(2,2,6,6-tetramethylpiperidin-4-yl) decanedioate, the main research area is polyurethane composite preparation UV irradiation deterioration.

Polyurethanes (PU’s) made from renewable and sustainable materials are one of the most important groups of polymers because of their versatility with wide range of grades, densities and stiffness. In this project, polymers based on renewable materials such as rapeseed (RS) and sunflower oil (SF) were synthesized and cross-linked to form polyurethanes. The effect of prolonged exposure up to 1000 h upon UVB light, in general promotes photodegradation for both RS and SF-based polyurethanes, both neat and also composites loaded with TiO2. The addition of 10% Degussa P25 TiO2 pigment, gives the greater degradation while PUs loaded with 5% Kronos 2220 show the slowest rates of degradation due to the effect of the coating of this pigment. The photostabilizer Tinuvin 770 offers high protection from UVB, thus lead the combination of Tinuvin 770 with Degussa P25 promotes the highest protection from UVB exposure. Moreover, addition of Tinuvin 770 at the stage of preparation of the PUs also greatly reduced the undesirable yellow coloration prevalent during PU synthesis.

Composites, Part B: Engineering published new progress about Absorption. 52829-07-9 belongs to class piperidines, name is Bis(2,2,6,6-tetramethylpiperidin-4-yl) decanedioate, and the molecular formula is C28H52N2O4, Application of Bis(2,2,6,6-tetramethylpiperidin-4-yl) decanedioate.

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem