Mild Organic Base-Catalyzed Primary Alcohol-Selective Aroylation Reaction Using N-Aroylcarbazoles for Underexplored Prodrugs

2020 ◽  
Author(s):  
Yasuaki Morita ◽  
Bubwoong Kang ◽  
Rubi Nakashima ◽  
Yuki Shimizu ◽  
Asumi Sakai ◽  
...  
Keyword(s):  
Primary Alcohol ◽  
Reaction System ◽  
Organic Base ◽  
Base Catalyst ◽  
Preparation Methods ◽  
General Base ◽  
Drug Molecules ◽  
Synthetic Utility ◽  
Scale Preparation ◽  
Complex Drug

<div>We report a highly primary alcohol-selective aroylation reaction using N-aroylcarbazoles (NAroCs). The aroylation</div><div>proceeded smoothly in the presence of DBU, which most likely works as a general base catalyst in the reaction system. The synthetic utility was displayed in the primary alcohol-selective aroylation of complex drug molecules and natural products to their prodrugs. Stoichiometrically generated carbazole, the starting material of NAroCs could be easily recovered. We also established safer multigram and multidecagram scale preparation methods of NAroCs, which are easy-to-handle bench-stable reagents.</div>

Mild Organic Base-Catalyzed Primary Alcohol-Selective Aroylation Reaction Using N-Aroylcarbazoles for Underexplored Prodrugs

2020 ◽  
Author(s):  
Yasuaki Morita ◽  
Bubwoong Kang ◽  
Rubi Nakashima ◽  
Yuki Shimizu ◽  
Asumi Sakai ◽  
...  
Keyword(s):  
Primary Alcohol ◽  
Reaction System ◽  
Organic Base ◽  
Base Catalyst ◽  
Preparation Methods ◽  
General Base ◽  
Drug Molecules ◽  
Synthetic Utility ◽  
Scale Preparation ◽  
Complex Drug

<div>We report a highly primary alcohol-selective aroylation reaction using N-aroylcarbazoles (NAroCs). The aroylation</div><div>proceeded smoothly in the presence of DBU, which most likely works as a general base catalyst in the reaction system. The synthetic utility was displayed in the primary alcohol-selective aroylation of complex drug molecules and natural products to their prodrugs. Stoichiometrically generated carbazole, the starting material of NAroCs could be easily recovered. We also established safer multigram and multidecagram scale preparation methods of NAroCs, which are easy-to-handle bench-stable reagents.</div>

scholarly journals Evidence for lysine 80 as general base catalyst of leucine dehydrogenase.

1993 ◽  
Vol 268 (36) ◽  
pp. 27039-27045
Author(s):  
T Sekimoto ◽  
T Matsuyama ◽  
T Fukui ◽  
K Tanizawa
Keyword(s):  
Base Catalyst ◽  
Leucine Dehydrogenase ◽  
General Base

An Overview of Nanoparticles: Current Scenario

2021 ◽  
pp. 239-246
Author(s):  
Seema U. Shinde ◽  
Nikita D. Gidde ◽  
Pradnya P. Shinde ◽  
Akshay B. Kadam
Keyword(s):  
Drug Delivery ◽  
High Stability ◽  
Hydrophobic Drug ◽  
Preparation Methods ◽  
Routes Of Administration ◽  
Drug Molecules ◽  
Conventional Drug ◽  
Current Scenario ◽  
Release Potential ◽  
Novel Drug

The simplest type of structures with sizes in the nm range will be nanoparticles. Any atom mean that is associated by intensity with other atoms within a 'limited' distance may be claimed to be a nanoparticle in principle. The creation of novel drug delivery systems using nanoparticles has seen an exponential interest in recent years. In terms of high stability, high precision, high drug carrying capability, managed release potential, the possibility of use in various routes of administration and the ability to deliver both hydrophilic and hydrophobic drug molecules, nanoparticles may offer significant advantages over conventional drug delivery. The emphasis of this study is on classification, types, synthesis, preparation methods, characterization, use, nanoparticle advantages, and health perspectives.

scholarly journals The Importance of Interfacial Tension in Emulsification: Connecting Scaling Relations Used in Large Scale Preparation with Microfluidic Measurement Methods

2020 ◽  
Vol 4 (4) ◽  
pp. 63
Author(s):  
Karin Schroën ◽  
Jolet de Ruiter ◽  
Claire Berton-Carabin
Keyword(s):  
Interfacial Tension ◽  
Large Scale ◽  
Measurement Methods ◽  
Scaling Relations ◽  
Active Components ◽  
Preparation Methods ◽  
Large Scale Preparation ◽  
Complex Process ◽  
Scale Preparation ◽  
Multi Phase

This paper starts with short descriptions of emulsion preparation methods used at large and smaller scales. We give scaling relations as they are generally used, and focus on the central role that interfacial tension plays in these relations. The actual values of the interfacial tension are far from certain given the dynamic behavior of surface-active components, and the lack of measurement methods that can be applied to conditions as they occur during large-scale preparation. Microfluidic techniques are expected to be very instrumental in closing this gap. Reduction of interfacial tension resulting from emulsifier adsorption at the oil-water interface is a complex process that consists of various steps. We discuss them here, and present methods used to probe them. Specifically, methods based on microfluidic tools are of great interest to study short droplet formation times, and also coalescence behavior of droplets. We present the newest insights in this field, which are expected to bring interfacial tension observations to a level that is of direct relevance for the large-scale preparation of emulsions, and that of other multi-phase products.

scholarly journals Nanosuspension Technologies for Delivery of Poorly Soluble Drugs

2015 ◽  
Vol 2015 ◽  
pp. 1-13 ◽  
Author(s):  
Roya Yadollahi ◽  
Krasimir Vasilev ◽  
Spomenka Simovic
Keyword(s):  
Aqueous Solubility ◽  
Drug Formulation ◽  
Preparation Methods ◽  
Administration Routes ◽  
Drug Molecules ◽  
Advanced Therapies ◽  
Poorly Soluble ◽  
Minimal Damage ◽  
Processing Techniques ◽  
Cancer Tissues

Poor aqueous solubility of some drug molecules is a major problem in drug formulation. Drug nanosuspensions emerged as one solution to delivering such hydrophobic drugs. Scaling down to nanoparticles enhances drug aqueous solubility and bioavailability by increasing drug surface area that comes into contact with biological media. Nanosuspensions that have attracted particular attention are those sterically stabilised by steric polymers such as polyethylene glycol (PEG) with a typical size range of 10–100 nm. These nanoparticles are capable of accumulating in targeted areas such as cancer tissues and infarct zones with minimal damage to healthy tissues. Nanosuspensions are often prepared by commercially available methods such as high pressure homogenization, media milling, emulsification, and melt emulsification. Solidification and surface modification methods are post-processing techniques used to add particular properties for advanced therapies. In this review, we firstly describe preparation methods for nanosuspensions. Secondly, we highlight typical characterization techniques. Finally, we describe several practical application of applications for drug delivery design and different administration routes such as parenteral, pulmonary, oral, and ocular.

Ligand-Accelerated Non-Directed C–H Cyanation of Arenes

2018 ◽  
Author(s):  
Luoyan Liu ◽  
Kap-Sun Yeung ◽  
jin-quan yu
Keyword(s):  
Natural Products ◽  
Bond Cleavage ◽  
Drug Molecules ◽  
Kinetic Isotope ◽  
Rate Limiting Step ◽  
Limiting Step ◽  
Broad Scope ◽  
Synthetic Utility ◽  
Rate Limiting

<p>We herein report the first example of a 2-pyridone accelerated non-directed C−H cyanation with an arene as the limiting reagent. This protocol is compatible with a broad scope of arenes, including advanced intermediates, drug molecules, and natural products. A kinetic isotope experiment (k<sub>H</sub>/k<sub>D</sub> = 4.40) indicates that the C–H bond cleavage is the rate-limiting step. Also, the reaction is readily scalable, further showcasing the synthetic utility of this method.<i></i></p>

The Pharmacology of Delta-9-Tetrahydrocannabinol (THC)

2018 ◽  
Author(s):  
Leslie Iversen
Keyword(s):  
Mechanism Of Action ◽  
Neurotransmitter Release ◽  
Cannabinoid Receptors ◽  
The Body ◽  
Psychoactive Substance ◽  
Plant Chemistry ◽  
Drug Molecules ◽  
History Of ◽  
The 19Th Century ◽  
Complex Drug

The 19th century was a great era for plant chemistry. Many complex drug molecules, known as alkaloids, were isolated and identified from plants. This chapter discusses the history of the discovery of delta-9-tetrahyrocannabinol (THC) as the psychoactive substance in cannabis products and also the discovery of the cannabinoid receptors CB-1 and CB-2 in the body and brain. The mechanism of action of cannabinoids on such receptors to inhibit neurotransmitter release or other actions is also discussed. In addition, various methods for the ingestion of cannabis, such as smoking and vaping, are reviewed. Synthetic agonists and antagonists at cannabinoid receptors and the proliferation of synthetic agonists as novel psychoactive agents are also discussed.

AMORPHOUS PHARMACEUTICAL SOLIDS: A REVIEW

INDIAN DRUGS ◽  
2013 ◽  
Vol 50 (07) ◽  
pp. 5-13
Author(s):  
B. V Dhokchawle ◽  
◽  
S. J. Tauro ◽  
A. B Bhandari
Keyword(s):  
Freeze Drying ◽  
Amorphous State ◽  
Vapor Sorption ◽  
Pharmaceutical Solids ◽  
Preparation Methods ◽  
Continuous Increase ◽  
Amorphous Pharmaceuticals ◽  
Drug Molecules ◽  
Sorption Method ◽  
Quench Cooling

Amorphous pharmaceutical solids have recently attracted the interest of pharmaceutical scientists because of a continuous increase in the number of developmental drug molecules that are insoluble. Amorphous state of the drug provides several pharmacokinetic advantages over the crystalline state. In this review preparation methods, characterization techniques and applications of amorphous pharmaceuticals have been discussed. Quench cooling, melt extrusion, spray drying and freeze drying are important methods for amorphization of solids. Amorphous pharmaceutical solids are characterized by diffraction technique, spectroscopy, vapor sorption method and thermal analytical methods. Stability of amorphous solids is important as their advantage of improved solubility might not be long lasting.

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