Silica Chloride Nano Particle Catalyzed Synthesis of 2,2\u27-(arylmethylene)bis(5,5-dimethylcyclohexane-1,3-dione) Derivatives

Silica chloride nano particle (nano SiO2–Cl), has been found to be heterogeneous catalyst for fa-cile and simple condensation of dimedone with aromatic aldehydes into 2,2\u27-(arylmethylene)bis(5,5-dimethylcyclohexane-1,3-dione) derivatives in dry CH2Cl2. (doi: 10.5562/cca1721

An Overview on Veterinary Drug Residues in Food Products and Guidelines for their Production and Use

Veterinary pharmaceuticals have a significant role in animal and human health, therefore, production monitoring and quality control of these pharmaceuticals are of special importance. This work presents an overview on veterinary drug residues in food products and the environment and also discusses the main topics of the guidelines of veterinary pharmaceuticals production, quality control, and usage. This review is composed of more than 100 references and reports the findings of 44 studies conducted on drugs residuals of veterinary food products produced in Iran

Synthesis of 2-(2-Fluorophenyl)-2-methylamino-Cyclohexanone as a New Ketamine Derivative

<div><p></p><p>The main goal of this article is to the present research on the development of ketamine derivatives. The target molecule was a fluoroderivative of ketamine, for which a multistep synthesis has been reported. This novel ketamine derivative, 2-(2-fluorophenyl)-2-methylamino-cyclohexanone, has been called fluoroketamine by our research group. The starting fluorobenzonitrile was reacted with the appropriate Grignard reagent followed by the bromination reaction to obtain α-bromocyclopentyl-(2-fluorophenyl)-ketone. The reaction of the obtained ketone with methylamine at −40 °C then resulted in the formation of α-hydroxycyclopentyl-(2-flourophenyl)-N-methylamine. Finally, the five-memberd ring cyclopentanol was expanded to the cyclohexylketone by a thermal rearrangement reaction. The HCl salt of the target molecule, which is soluble in water, was obtained by the acidification of the free fluoroketamine with HCl. Preliminary animal tests on mice have shown that the resulting fluoroketamine has some advantages over ketamine in terms of the effective dose and the recovery time.</p> </div

Design, Synthesis and Radiolabeling of Peptide GPRPILE with 18FDG as Fibrin Imaging Agent for Thrombosis Detection

Background: The radionuclide of choice for routine clinical PET imaging is 18-F. As direct fluorination of peptides with 18-F is not possible, indirect methods using fluorinated prosthetic groups have been&nbsp;developed. Due to the availability of 18FDG in most PET centers, there is potential for 18FDG as a fluorinated prosthetic group. In this study, the linear peptide GPRPILE with an aminooxy group was designed,&nbsp;synthesized and radiolabeled with 18FDG as fibrin imaging agent. Material and Methods: Docking studies were conducted done using AutoDock 4.1 and HEX software programs. Aoe-GPRPILE peptide was designed, synthesized through Fmoc method and radiolabeled with 18FDG. The radiochemical purity, stability of radiolabeled and cold peptide in PBS and human plasma was determined using chromatographic methods. The solubility ratio of the radiolabeled peptide in lipid to water (LogP) was determined. Results: Docking and pharmacophore studies using HEX software revealed high affinity of designed&nbsp;peptide to fibrin (E Total=-0.01). The identity and structure of peptide were determined by LC-Mass. Peptide was stable over 24 hr in human plasma and PBS buffer. The optimum conditions of radiolabeling were 0.2 mg peptide, 1 mCi 18FDG, 90&deg;C for 30 min, pH=5. The radiochemical purity was over 95%. The stability of radiolabeled peptide in human plasma for 2 hr was over 95%. The partition coefficient (LogP) was 1.5. Conclusion: 18FDG has a high potential to be used as a prosthetic group for radiolabeling of peptides with 18-F. In this study, peptide Aoe-GPRPILE with aminooxy was synthesized and labeled with 18FDG with high yield and radiochemical purity. Aminooxy is conjugated to peptide sequence as a prosthetic group in the last step with minimal effect on peptide properties and selectively forms stable oxime bond with the aldehyde group of 18FDG

Reinvestigation of the Two-step Synthesis of Sevoflurane

Abstract Improvements in the two-step synthesis of 1,1,1,3,3,3-hexafluoro-2-(fluoromehoxy)propane (Sevoflurane) that result in the product cost reduction, safety level enhancement and positive environmental impacts are described. This process consists of chloromethylation reaction of 1,1,1,3,3,3-hexafluoro-2-propanol (HFIP) followed by a halogen-exchange fluorination. This is the first synthesis of Sevoflurane in Iran which was successfully scaled up. During this work, several improvements have been achieved by optimization of the reaction time, the amount of consumed starting materials and solvents and work up procedure while keeping the yield and purity intact. The reaction time of the first step (24 h) was diminished to 4 h. 19 F NMR spectroscopy was used to investigate the rate of the reaction in the first step and to evaluate the influence of different parameters mentioned on the achieved improvements