Category: 135616-36-3

Synthetic Route of 135616-36-3, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.135616-36-3, Name is (S,S)-(+)-N,N’-Bis(3,5-di-tert-butylsalicylidene)-1,2-cyclohexanediamine, molecular formula is C36H54N2O2. In a Article£¬once mentioned of 135616-36-3

Synthesis and in Vivo Evaluation of a Novel PET Radiotracer for Imaging of Synaptic Vesicle Glycoprotein 2A (SV2A) in Nonhuman Primates

Structural disruption and alterations of synapses are associated with many brain disorders including Alzheimer’s disease, epilepsy, depression, and schizophrenia. We have previously developed the PET radiotracer 11C-UCB-J for imaging and quantification of synaptic vesicle glycoprotein 2A (SV2A) and synaptic density in nonhuman primates and humans. Here we report the synthesis of a novel radiotracer 18F-SDM-8 and its in vivo evaluation in rhesus monkeys. The in vitro binding assay of SDM-8 showed high SV2A binding affinity (Ki = 0.58 nM). 18F-SDM-8 was prepared in high molar activity (241.7 MBq/nmol) and radiochemical purity (>98%). In the brain, 18F-SDM-8 displayed very high uptake with peak standardized uptake value (SVU) greater than 8 and fast and reversible kinetics. A displacement study with levetiracetam and blocking studies with UCB-J and levetiracetam demonstrated its binding reversibility and specificity toward SV2A. Regional binding potential values were calculated and ranged from 0.8 in the brainstem to 4.5 in the cingulate cortex. By comparing to 11C-UCB-J, 18F-SDM-8 displayed the same attractive imaging properties: very high brain uptake, appropriate tissue kinetics, and high levels of specific binding. Given the longer half-life of F-18 and the feasibility for central production and multisite distribution, 18F-SDM-8 holds promise as an excellent radiotracer for SV2A and as a biomarker for synaptic density measurement in neurodegenerative diseases and psychiatric disorders.

The reactant in an enzyme-catalyzed reaction is called a substrate. Enzyme inhibitors cause a decrease in the reaction rate of an enzyme-catalyzed reaction.I hope my blog about 135616-36-3 is helpful to your research. Synthetic Route of 135616-36-3

Reference£º
Metal catalyst and ligand design,
Ligand Template Strategies for Catalyst Encapsulation – NCBI

Synthetic Route of 135616-36-3, Chemistry is the experimental science by definition. We want to make observations to prove hypothesis. For this purpose, we perform experiments in the lab. 135616-36-3, Name is (S,S)-(+)-N,N’-Bis(3,5-di-tert-butylsalicylidene)-1,2-cyclohexanediamine,introducing its new discovery.

Synthesis and in vivo evaluation of [18F]UCB-J for PET imaging of synaptic vesicle glycoprotein 2A (SV2A)

Purpose: Synaptic abnormalities have been implicated in a variety of neuropsychiatric disorders, including epilepsy, Alzheimer?s disease, and schizophrenia. Hence, PET imaging of the synaptic vesicle glycoprotein 2A (SV2A) may be a valuable in vivo biomarker for neurologic and psychiatric diseases. We previously developed [11C]UCB-J, a PET radiotracer with high affinity and selectivity toward SV2A; however, the short radioactive half-life (20 min for 11C) places some limitations on its broader application. Herein, we report the first synthesis of the longer-lived 18F-labeled counterpart (half-life: 110 min), [18F]UCB-J, and its evaluation in nonhuman primates. Methods: [18F]UCB-J was synthesized from the iodonium precursors. PET imaging experiments with [18F]UCB-J were conducted in rhesus monkeys to assess the pharmacokinetic and in vivo binding properties. Arterial samples were taken for analysis of radioactive metabolites and generation of input functions. Regional time?activity curves were analyzed using the one-tissue compartment model to derive regional distribution volumes and binding potentials for comparison with [11C]UCB-J. Results: [18F]UCB-J was prepared in high radiochemical and enantiomeric purity, but low radiochemical yield. Evaluation in nonhuman primates indicated that the radiotracer displayed pharmacokinetic and imaging characteristics similar to those of [11C]UCB-J, with moderate metabolism rate, high brain uptake, fast and reversible binding kinetics, and high specific binding signals. Conclusion: We have accomplished the first synthesis of the novel SV2A radiotracer [18F]UCB-J. [18F]UCB-J is demonstrated to be an excellent imaging agent and may prove to be useful for imaging and quantification of SV2A expression, and synaptic density, in humans.

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Reference£º
Metal catalyst and ligand design,
Ligand Template Strategies for Catalyst Encapsulation – NCBI

135616-36-3, (S,S)-(+)-N,N’-Bis(3,5-di-tert-butylsalicylidene)-1,2-cyclohexanediamine is a catalyst-ligand compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

8,0 g (0,015 mol) (S, S)-2, 2 – [1, 2-CYCLOHEXANDIYL) bis (nitrilomethylidyn)] bis [4,6-di- tert.-butyl)-phenol] werden in 200 ml Ethanol vorgelegt und mit 2,5 g (0,01 mol) Vanadylsulfat-Pentahydrat versetzt. Nach zwei Stunden unter Rueckfluss wird das Loesungsmittel abdestilliert, der Rueckstand in 400 ML Dichlormethan aufgenommen und die Loesung mit 200 ml Wasser gewaschen. Nach Phasentrennung, Trocknen der Loesung mit Natriumsulfat und Abdestillieren des Loesungsmittels erhaelt man 8,2 g gruenes, amorphes Pulver. Zusammensetzung des Gemischs nach HPLC (Gew. -%) : Komponente (I) : (X) : (III) =85% : 15% : 0%. [alpha D20 = +200 (c = 0,01, Chloroform)., 135616-36-3

As the paragraph descriping shows that 135616-36-3 is playing an increasingly important role.

Reference£º
Patent; CLARIANT GMBH; WO2004/55028; (2004); A1;,
Metal catalyst and ligand design
Ligand Template Strategies for Catalyst Encapsulation – NCBI

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.135616-36-3,(S,S)-(+)-N,N’-Bis(3,5-di-tert-butylsalicylidene)-1,2-cyclohexanediamine,as a common compound, the synthetic route is as follows.

Reference Example 1 [(R,R)-N,N’-bis(3,5-di-tert-butylsalicylidene)-1,2-cyclohexanediamine] (hereinafter, referred to as L3 when it is a ligand of a complex) (10.9 g, 20.0 mmol) was dissolved in dichloromethane (80mL), the solution was added to a methanol solution (80 mL) of cobalt acetate tetrahydrate (5.98 g, 24.0 mmol), the mixture was stirred at room temperature for 15 minutes, and as a result, a red solid was precipitated. After stirred at 0 C. for 30 minutes, the red solid was collected and dried to obtain Co(L3) (11.6 g, red solid) (yield: 96%)., 135616-36-3

The synthetic route of 135616-36-3 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Japan Science and Technology Agency; Takasago International Corporation; US2006/173210; (2006); A1;,
Metal catalyst and ligand design
Ligand Template Strategies for Catalyst Encapsulation – NCBI