scholarly journals Scalable and selective deuteration of (hetero)arenes

2022 ◽  
Author(s):  
Wu Li ◽  
Jabor Rabeah ◽  
Florian Bourriquen ◽  
Dali Yang ◽  
Carsten Kreyenschulte ◽  
...  

AbstractIsotope labelling, particularly deuteration, is an important tool for the development of new drugs, specifically for identification and quantification of metabolites. For this purpose, many efficient methodologies have been developed that allow for the small-scale synthesis of selectively deuterated compounds. Due to the development of deuterated compounds as active drug ingredients, there is a growing interest in scalable methods for deuteration. The development of methodologies for large-scale deuterium labelling in industrial settings requires technologies that are reliable, robust and scalable. Here we show that a nanostructured iron catalyst, prepared by combining cellulose with abundant iron salts, permits the selective deuteration of (hetero)arenes including anilines, phenols, indoles and other heterocycles, using inexpensive D2O under hydrogen pressure. This methodology represents an easily scalable deuteration (demonstrated by the synthesis of deuterium-containing products on the kilogram scale) and the air- and water-stable catalyst enables efficient labelling in a straightforward manner with high quality control.

2018 ◽  
Vol 25 (1) ◽  
pp. 57-69 ◽  
Author(s):  
David Cunningham Owens

SUMMARYTardive dyskinesia is a common iatrogenic neurological and neurobehavioural syndrome associated with the use of antidopaminergic medication, especially antipsychotics. Prior to the introduction of the newer antipsychotics in the 1990s, it was one of the major areas of psychiatric research but interest waned as the new drugs were reputed to have a reduced liability to extrapyramidal adverse effects in general, a claim now discredited by numerous pragmatic research studies. Early small-scale short-term prevalence studies were presented as evidence to support the assumption that patients on the newer drugs did indeed have a lower prevalence of tardive dyskinesia but recent large-scale review of studies with patients exposed for longer suggest that things have not changed. This article presents a clinical overview of a complex and varied syndrome in terms of its phenomenology, epidemiology and risk factors; a companion article will consider treatment. This overview aims to highlight tardive dyskinesia once again, especially to practitioners who have trained in an environment where this was considered mainly in historical terms.LEARNING OBJECTIVES•Understand the complex phenomenology comprising the syndrome of tardive dyskinesia•Appreciate recent data on prevalence and incidence with the newer antipsychotics•Be aware of risk factors when recommending antipsychotic (and other antidopaminergic) drugsDECLARATION OF INTERESTNone.


2000 ◽  
Vol 45 (4) ◽  
pp. 396-398
Author(s):  
Roger Smith
Keyword(s):  

2020 ◽  
Vol 1 (1) ◽  
pp. 1-10
Author(s):  
Evi Rahmawati ◽  
Irnin Agustina Dwi Astuti ◽  
N Nurhayati

IPA Integrated is a place for students to study themselves and the surrounding environment applied in daily life. Integrated IPA Learning provides a direct experience to students through the use and development of scientific skills and attitudes. The importance of integrated IPA requires to pack learning well, integrated IPA integration with the preparation of modules combined with learning strategy can maximize the learning process in school. In SMP 209 Jakarta, the value of the integrated IPA is obtained from 34 students there are 10 students completed and 24 students are not complete because they get the value below the KKM of 68. This research is a development study with the development model of ADDIE (Analysis, Design, Development, Implementation, and Evaluation). The use of KPS-based integrated IPA modules (Science Process sSkills) on the theme of rainbow phenomenon obtained by media expert validation results with an average score of 84.38%, average material expert 82.18%, average linguist 75.37%. So the average of all aspects obtained by 80.55% is worth using and tested to students. The results of the teacher response obtained 88.69% value with excellent criteria. Student responses on a small scale acquired an average score of 85.19% with highly agreed criteria and on the large-scale student response gained a yield of 86.44% with very agreed criteria. So the module can be concluded receiving a good response by the teacher and students.


2019 ◽  
Vol 61 (1) ◽  
pp. 5-13 ◽  
Author(s):  
Loretta Lees

Abstract Gentrification is no-longer, if it ever was, a small scale process of urban transformation. Gentrification globally is more often practised as large scale urban redevelopment. It is state-led or state-induced. The results are clear – the displacement and disenfranchisement of low income groups in favour of wealthier in-movers. So, why has gentrification come to dominate policy making worldwide and what can be done about it?


2020 ◽  
Vol 9 (2) ◽  
Author(s):  
Bùi Thị Bích Lan

In Vietnam, the construction of hydropower projects has contributed significantly in the cause of industrialization and modernization of the country. The place where hydropower projects are built is mostly inhabited by ethnic minorities - communities that rely primarily on land, a very important source of livelihood security. In the context of the lack of common productive land in resettlement areas, the orientation for agricultural production is to promote indigenous knowledge combined with increasing scientific and technical application; shifting from small-scale production practices to large-scale commodity production. However, the research results of this article show that many obstacles in the transition process are being posed such as limitations on natural resources, traditional production thinking or the suitability and effectiveness of scientific - technical application models. When agricultural production does not ensure food security, a number of implications for people’s lives are increasingly evident, such as poverty, preserving cultural identity, social relations and resource protection. Since then, it has set the role of the State in researching and building appropriate agricultural production models to exploit local strengths and ensure sustainability.


Author(s):  
Christina Schindler ◽  
Hannah Baumann ◽  
Andreas Blum ◽  
Dietrich Böse ◽  
Hans-Peter Buchstaller ◽  
...  

Here we present an evaluation of the binding affinity prediction accuracy of the free energy calculation method FEP+ on internal active drug discovery projects and on a large new public benchmark set.<br>


2018 ◽  
Vol 1 (3) ◽  
pp. 156-165 ◽  
Author(s):  
Nasirudeen Abdul Fatawu

Recent floods in Ghana are largely blamed on mining activities. Not only are lives lost through these floods, farms andproperties are destroyed as a result. Water resources are diverted, polluted and impounded upon by both large-scale minersand small-scale miners. Although these activities are largely blamed on behavioural attitudes that need to be changed, thereare legal dimensions that should be addressed as well. Coincidentally, a great proportion of the water resources of Ghana arewithin these mining areas thus the continual pollution of these surface water sources is a serious threat to the environmentand the development of the country as a whole. The environmental laws need to be oriented properly with adequate sanctionsto tackle the impacts mining has on water resources. The Environmental Impact Assessment (EIA) procedure needs to bestreamlined and undertaken by the Environmental Protection Agency (EPA) and not the company itself.


2013 ◽  
Vol 14 (2) ◽  
Author(s):  
Noor Fachrizal

Biomass such as agriculture waste and urban waste are enormous potency as energy resources instead of enviromental problem. organic waste can be converted into energy in the form of liquid fuel, solid, and syngas by using of pyrolysis technique. Pyrolysis process can yield higher liquid form when the process can be drifted into fast and flash response. It can be solved by using microwave heating method. This research is started from developing an experimentation laboratory apparatus of microwave-assisted pyrolysis of biomass energy conversion system, and conducting preliminary experiments for gaining the proof that this method can be established for driving the process properly and safely. Modifying commercial oven into laboratory apparatus has been done, it works safely, and initial experiments have been carried out, process yields bio-oil and charcoal shortly, several parameters are achieved. Some further experiments are still needed for more detail parameters. Theresults may be used to design small-scale continuous model of productionsystem, which then can be developed into large-scale model that applicable for comercial use.


Water Policy ◽  
2003 ◽  
Vol 5 (3) ◽  
pp. 203-212
Author(s):  
J. Lisa Jorgensona

This paper discusses a series of discusses how web sites now report international water project information, and maps the combined donor investment in more than 6000 water projects, active since 1995. The maps show donor investment:  • has addressed water scarcity,  • has improved access to improvised water resources,  • correlates with growth in GDP,  • appears to show a correlation with growth in net private capital flow,  • does NOT appear to correlate with growth in GNI. Evaluation indicates problems in the combined water project portfolios for major donor organizations: •difficulties in grouping projects over differing Sector classifications, food security, or agriculture/irrigation is the most difficult.  • inability to map donor projects at the country or river basin level because 60% of the donor projects include no location data (town, province, watershed) in the title or abstracts available on the web sites.  • no means to identify donor projects with utilization of water resources from training or technical assistance.  • no information of the source of water (river, aquifer, rainwater catchment).  • an identifiable quantity of water (withdrawal amounts, or increased water efficiency) is not provided.  • differentiation between large scale verses small scale projects. Recommendation: Major donors need to look at how the web harvests and combines their information, and look at ways to agree on a standard template for project titles to include more essential information. The Japanese (JICA) and the Asian Development Bank provide good models.


Sign in / Sign up

Export Citation Format

Share Document