Concise approach to γ-(het)aryl- and γ-alkenyl-γ-aminobutyric acids. Synthesis of vigabatrin.

γ-Aminobutyric acid (GABA) and GABA derivatives have attracted increased attention over the years in the fields of medicinal chemistry and chemical biology due to their interesting biological properties and synthetic relevance. Here, we report a short synthetic route to γ-(het)aryl- and γ-alkenyl-γ-aminobutyric acids, including the antiepileptic drug vigabatrin, from readily available donor-acceptor cyclopropanes and ammonia or methylamine. This protocol includes a facile synthesis of 2-oxopyrrolidine-3-carboxamides and their acid hydrolysis to γ-aryl- or γ-alkenyl-substituted GABAs, which can serve as perspective building blocks for the synthesis of various GABA-based N-heterocycles and bioactive compounds.

Synthesis of 1,5-Substituted Pyrrolidin-2-ones from Donor-Acceptor Cyclopropanes and Anilines/Benzylamines.

We developed a straightforward synthetic route to pharmacologically important 1,5-substituted pyrrolidin-2-ones from donor-acceptor cyclopropanes bearing an ester group as one of the acceptor substituents. This method includes a Lewis acid-catalyzed opening of the donor-acceptor cyclopropane with primary amines (anilines, benzylamines, etc.) to γ-amino esters, followed by in situ lactamization and dealkoxycarbonylation. The reaction has a broad scope of applicability; a variety of substituted anilines, benzylamines, and other primary amines as well as a wide range of donor-acceptor cyclopropanes bearing (hetero)aromatic or alkenyl donor groups and various acceptor substituents can be involved in this transformation. In this process, donor-acceptor cyclopropanes react as 1,4-C,C-dielectrophiles, and amines react as 1,1-dinucleophiles. The resulting di- and trisubstituted pyrrolidin-2-ones can be also used in subsequent chemistry to obtain various nitrogen-containing polycyclic compounds of interest to medicinal chemistry and pharmacology, such as benz[g]indolizidine derivatives.

Satisfaction of outpatient oncologists with their work.

Job satisfaction is a fundamental ingredient in the life quality of a modern person; for a health care worker, it determines to a large extent the quality and accessibility of health care services they provide. Our aim is identification of key reasons for low job satisfaction among outpatient oncologists at cancer care centres (CCC) and identification of the best ways to address them. 110 oncologists working in outpatient CCC in Moscow, Moscow region and Ivanovo region participated in this research. Respondents' job satisfaction was assessed using V.A. Rozanova's Job Satisfaction Assessment Questionnaire. Virtually a quarter (23.6%) of oncologists were dissatisfied with their work; male respondents and surgical employees reported significantly higher levels of dissatisfaction. Wage levels and equity, working hours, teamwork and coordination in carrying out collective tasks and managerial style were the main areas of dissatisfaction. Measures to improve the work process included enhancing the resource outfit, fair consideration of each employee's achievements when distributing incentives, clear allocation of responsibility for collective project tasks, creating opportunities for paid part-time work and arranging regular meals at the expense of the health care organisation. Raising managers' awareness of the results can contribute to improvements in oncologists' performance, work process satisfaction, productivity and performance, quality of care and access to it, as well as public satisfaction and confidence in the health-care system as a whole.