Reversal of Diastereoselection in the Conjugate Addition of Cuprates to Unsaturated Lactams

We report that the stereochemical outcome of the conjugate addition of organocopper reagents to bicyclic α,β-unsaturated lactams derived from pyroglutaminol is determined by the nature of the aminal group. Bicyclic α,β-unsaturated lactams in which the aminal is derived from a ketone have been found to afford products of <i>syn</i> conjugate addition. By contrast, bicyclic α,β-unsaturated lactams in which the aminal is derived from an aldehyde afford products of <i>anti</i> conjugate addition. These remarkably different results obtained from very similar starting materials are unexpected

Visible-Light-Driven Photocatalytic Initiation of Radical Thiol–Ene Reactions Using Bismuth Oxide

A nontoxic and inexpensive photocatalytic initiation of anti-Markovnikov hydrothiolation of olefins using visible light is reported. This method is characterized by low catalyst loading, thereby enabling a mild and selective method for radical initiation in thiol–ene reactions between a wide scope of olefins and thiols

Access to Highly Substituted 7‑Azaindoles from 2‑Fluoropyridines via 7‑Azaindoline Intermediates

A versatile synthesis of 7-azaindoles from substituted 2-fluoropyridines is described. C3-metalation and 1,4-addition to nitroolefins provide substituted 2-fluoro-3-(2-nitroethyl)­pyridines. A facile oxidative Nef reaction/reductive amination/intramolecular S_NAr sequence furnishes 7-azaindolines. Finally, optional regioselective electrophilic C5-substitution (e.g., bromination or nitration) and subsequent in situ oxidation delivers highly functionalized 7-azaindoles in high overall efficiency

Sulfones: A New Functional Group for Modular Radical Cross-Coupling

<div>Cross-coupling chemistry comprises the vast majority of reactions employed in the synthesis of medicines, agrochemicals, and other functional materials. The interest in single-electron-induced coupling chemistry stems from the unique ability of these methods to facilitate the formation of challenging C(sp2)–C(sp3) linkages. This work introduces a new functional group, PT sulfones, for radical cross-coupling, enabling the simplified modular assembly of complex structures in an ordered, practical fashion. The scope of this method is extensively explored, and its strategic application is exemplified through the streamlined preparation of medicinally-oriented fluorine-containing scaffolds that previously required multiple steps, toxic reagents, and non-modular retrosynthetic blueprints. This work has also resulted in the development of five reagents for the rapid assembly of a vast set of structures, many of which contain challenging fluorination patterns. <br></div><div><br></div

Structure-Based Approach To Identify 5‑[4-Hydroxyphenyl]­pyrrole-2-carbonitrile Derivatives as Potent and Tissue Selective Androgen Receptor Modulators

In an effort to find new and safer treatments for osteoporosis and frailty, we describe a novel series of selective androgen receptor modulators (SARMs). Using a structure-based approach, we identified compound <b>7</b>, a potent AR (ARE EC₅₀ = 0.34 nM) and selective (N/C interaction EC₅₀ = 1206 nM) modulator. In vivo data, an AR LBD X-ray structure of <b>7</b>, and further insights from modeling studies of ligand receptor interactions are also presented

Structure-Based Approach To Identify 5‑[4-Hydroxyphenyl]­pyrrole-2-carbonitrile Derivatives as Potent and Tissue Selective Androgen Receptor Modulators

In an effort to find new and safer treatments for osteoporosis and frailty, we describe a novel series of selective androgen receptor modulators (SARMs). Using a structure-based approach, we identified compound <b>7</b>, a potent AR (ARE EC₅₀ = 0.34 nM) and selective (N/C interaction EC₅₀ = 1206 nM) modulator. In vivo data, an AR LBD X-ray structure of <b>7</b>, and further insights from modeling studies of ligand receptor interactions are also presented

The Faculty of education restaurant consumers' attitude towards the responsible treatment of food

Food waste is a burning issue all over the world. Different producers, households, shops, restaurants, schools and other food offering venues face this problem. It is important to raise the society’s awareness about the consequences of food waste. In my diploma work I tried to establish the secondary school students and the students of the Faculty of Education attitude towards food and the level of their satisfaction with the faculty restaurant food. I have researched the reasons for the food waste and gathered students’ suggestions on how to reduce its amount. In my research, I have used a descriptive method and a quantitative approach. There were 60 students of the Faculty of Education and 59 secondary school students of the Pre-school Teacher Training Secondary School participating in my research. The research showed a moderate level of student’s satisfaction with the food in the restaurant at the Faculty of Education. The main reasons in case of dissatisfaction are according to students the taste and general food quality. I discovered that one of the main reasons for food waste are large portions but the students claimed the reason for not finishing the meal was the feeling of satiety. The secondary school students usually finish their meals whereas the college students more often leave some food on their plates. They have both suggested that food waste could be reduced by giving them smaller portions which means they should be able to choose the size of the meal at the self-service counter. They also proposed that users of food services could be educated about food waste problem through various lectures and education programs. They suggested the use of available food containers for the left-overs and extra food that could be given to those who are in need. Communication between the service providers and users is also very important as it can greatly reduce the number of times when less desired foods are offered. The awareness about discarded food is increasingly rising in schools and colleges. According to the results of my research, I estimated that secondary school students and college students are both conscious of the consequences of discarded food with college students being slightly more aware of the problem. My estimation is that the amount of food waste can be reduced by careful planning and management of offered foods. Different projects that would raise the awareness about food waste among the student population are also very important