bluuebunny/crossref_metadata_2025 huggingface dataset:
Health hazards by lead exposure: evaluation using ASV and XRF
Authors: Herman D'souza Sunil , Geraldine Menezes , Scott Clark C , Venkatesh Thuppil
Published: October 2006

Globally, of many toxic heavy metals, lead is the most widely used for various purposes, resulting in a variety of health hazards due to environmental contamination. Lead in the workplace enters the workers through inhalation of lead-contaminated air, by ingestion, and sometimes through dermal exposure. Furthermore, exposure outside the workplace can occur from inhalation of lead-contaminated air, ingestion of lead-contaminated dust and soil, consumption of lead polluted water, lead adulterated food and lead supplemented medicine. In the present study, an evaluation of blood lead was carried out with the aid of a 3010 B lead analyser, based on the principle of anodic stripping voltametry (ASV), and environmental lead in paint, soil and dust samples by a field portable X-ray fluorescence (XRF) analyser. This revealed a high incidence of lead toxicity in most of the lead-based industrial workers in the four facilities tested in India and high levels of lead in the environmental samples. Developed countries have complied with the global standards for regulating environmental lead poisoning in the workplace, eliminating to some degree excessive exposure to lead. A developing country, such as India, can tackle this problem by implementing national and international policies. The US Occupational Safety and Health Administration (OSHA) and Environmental Protection Agency (EPA) regulations, which are of prime importance, or similar regulations, can be adapted for use in India and implemented to minimize lead exposure and to reduce the resultant health hazards.
Load Management from an Environmental Perspective
Authors: Abaravicius Juozas , Pyrko Jurek
Published: October 2006

The key objective of this study is to discuss the possible environmental benefits of load management and evaluate their significance, primarily focusing on CO2 emissions reduction. The analysis is carried out on two levels: National – the Swedish electricity market, and local – one electric utility in southern Sweden. The results show the importance of considering the influence of site-specific or level-specific conditions on the environmental effects of load management. On the national level, load management measures can hardly provide significant environmental benefits in Sweden, due to the high hydropower production, which is the demand following production source. Emission reductions will rather be the result of energy efficiency measures, which will lower the load demand as well as the energy demand. However, when it comes to a local (utility) level, where load management is considered as an alternative to an installation of a peak diesel power plant, the benefits are clear.
Architectural Research in Information Visualization: 10 Years after
Authors: Bermudez Julio , Agutter Jim , Foresti Stefano
Published: October 2006

As our civilization dives deeper into the information age, making sense of ever more complex and larger amounts of data becomes critical. This article reports on interdisciplinary work in Information Visualization addressing this challenge and using architectural expertise as its main engine. The goal of this research is to significantly improve real time decision making in complex data spaces while devising a new architecture that responds to complex information environments. Although we have been reporting in aspects of this work for the past 7 years, this paper covers unpublished knowledge, design methods, operational strategies, and other details that bring together all the material published by our group thus far into a comprehensive and useful whole. We conclude by presenting our latest InfoVis design work in Network Security.
The EWTD: friend or foe to quality patient care?
Authors: Brewster MBS , Potter R , Power D , Rajaratnam V , Pynsent PB
Published: October 2006

For the last few years all the hospitals in the UK have been changing junior doctors' rotas to become compliant with the European Working Time Directive (EWTD). The first stage, requiring a junior doctor to work a maximum of 58 hours per week averaged over a 6-month period, became law in August 2004. In addition to new posts for junior doctors there have been schemes to facilitate the transition, such as the Hospital at Night programme. This was designed to use the minimum safe number of doctors from appropriate specialties with supporting medical staff to cover the hospital out of hours. It was required to make the most efficient use of this team and allow the junior doctor rotas to be compliant with the appointment of as few new posts as possible.
Reflections on a year in office
Authors: Ribeiro Bernard
Published: October 2006

It is hard to believe a year has flown by, with so many challenges, some still unresolved. We started the year with four main challenges to debate with government: the SHO bulge and the workforce, independent sector treatment centres (ISTCs), the European Working Time Directive (EWTD) and surgical outcome. The questions I must ask myself are: have we made a difference and have we moved the agenda forward? In order to engage politicians in these areas it was necessary to launch a media campaign to raise awareness of the issues among our patients, the public and the profession. So what have we achieved?
Changes see society 'fit to face future'
Authors: Steers James
Published: October 2006

This year, the Society of British Neurological Surgeons (SBNS) celebrates its 80th anniversary, making it the oldest national and second-oldest neurosurgical society in the world. The society will celebrate another milestone next year, hosting its 150th scientific meeting.
Spring barley yield and nitrogen recovery after application of peat manure and pig slurry
Authors: MATTILA P. K.
Published: October 2006

The effectiveness of peat manure, manufactured of pig slurry and moderately humified Sphagnum peat (slurry:peat ca. 1:1.5 v/v), as nitrogen (N) source for spring barley was investigated in a four.year field experiment on a clay loam soil in south-western Finland. Pig slurry, NPK fertilizer and plain peat were used as references. Manures were incorporated before sowing or surface-applied after sowing in spring at an ammoniacal N rate of.54.106 kg.ha-1 with or without supplementary NPK fertilizer (40.kg N.ha-1). Soil moisture conditions were varied by different irrigation treatments. Peat manure produced 5.15% higher grain yields than pig slurry, with the largest difference after surface application. Incorporation was more important for slurry than for peat manure in increasing N uptake and yield. Soil moisture deficit in spring and early summer limited the availability of manure N. Part of the manure N that was not available in the early growing period was apparently taken up by the crop later. Consequently, N concentration tended to be higher with lower yields, and differences in the recovery of manure N were smaller than the differences in grain yield. Supplementation of manures with inorganic fertilizer N increased yield by 37%, on average, and improved the N recovery.;
Ammonia volatilization, nitrogen in soil, and growth of barley after application of peat manure and pig slurry
Authors: MATTILA P. K.
Published: October 2006

Peat is added to manure, because its low pH and capacity to adsorb ammonia (NH3) give it potential to reduce nitrogen (N) loss. Peat manure was prepared by mixing pig slurry with moderately humified Sphagnum peat. Less than 1% of applied ammoniacal N was volatilized as NH3 from peat manure and pig slurry within 8 h of surface application on clay loam soil according to JTI method. Incorporated manures showed even smaller N loss. The low volatilization was due to the adsorption of manure ammoniacal N by peat, and the infiltration of slurry into harrowed, moist clay soil. In another experiment, peat manure was applied on polypropylene fabric without soil contact. Within the first 3 days there was only 9% reduction in the ammoniacal N of peat manure, but the major part of it was lost during several weeks of dry and warm weather. Peat manure did not cause any major improvements on the growth and N uptake of spring barley in spring and early summer as compared with slurry. Moisture deficit limited the availability of ammoniacal N of manures. As compared with surface application, incorporation of manures increased nitrification of ammonium in the soil, and dry matter mass (1973%) and N uptake of barley. Supplementing manures with inorganic NPK fertilizer increased both dry matter mass (4098%) and N concentration of barley stand.;
Beitrag über einige Umesterungsreaktionen des Oxalsäurediäthylesters
Authors: Klosa Josef
Published: October 2006

Es werden einige Umesterungsreaktionen des Oxalsäurediäthylesters und die Herstellung der Ester der Phenyl‐cyan‐brenztraubensäure und der p‐Nitro‐phenyl‐cyanbrenztraubensäure beschrieben.
Die Chemie der Belladonna‐flavonoide A und B und ihr Wert für die Qualitätsbeurteilung von Belladonnaextrakten. 4. Mitt. über „Extractum Belladonnae”︁
Authors: List P. H. , Hanafi S.
Published: October 2006

Frische Tollkirschenblätter enthalten 2 bisher noch unbekannte Flavonoltriglykoside, die wir als Quercetein‐3‐rhamnoglucosido‐7‐galaktosid und Kämpferol‐3‐rhamnogalaktosido‐7‐glucosid identifizierten. Die in handelsüblichen Belladonna‐Drogen und ‐Extrakten zahlreichen weiteren Flavonoide sind Abbauprodukte der beiden Triglykoside. Durch Beobachtung der fortschreitenden Hydrolyse ließ sich die Extraktbereitung schonender gestalten.
Über die Helch‐Reaktion des Pilocarpins
Authors: Auterhoff H. , Pankow H.‐J.
Published: October 2006

Es wird gezeigt, daß die Farbreaktion nach Helch von denjenigen Basen gegeben wird die sehr gut in Wasser und in Benzol löslich und gegen Chromperoxid relativ stabil sind. Um diese Hypothese zu überprüfen, wurde Pilocarpin in das in Benzol schwer lösliche Pilocarpdiol verwandelt, das die Reaktion nicht mehr gab; Acetylierung verlieh dem Pilocarpdiol wieder Lipophilie und damit die positive Reaktivität in der Helch‐Reaktion.
Aufbau des Ferredoxins, des Wirkstoffes der Assimilations vorgänge
Authors: Bayer E. , Parr W. , Kazmaier B.
Published: October 2006

Das Eisen des Ferredoxins kann mittels α,α′‐Dipyridyl abgespalten werden. Aus dem so gewonnenen Apoferredoxin und Eisen(II)‐salz ist eine Resynthese von Ferredoxin möglich. Das Molekulargewicht von Ferredoxin beträgt 7000. Das Auftreten des Schwefelwasserstoffes wird auf eine β‐Eliminierung aus den Cysteinylresten des Peptides zurückgeführt und nicht auf die Anwesenheit von anorganischem Sulfid. Nach Vergleich mit Modellsubstanzen wird das Eisen durch die Merkaptogruppen und den Stickstoff der Cysteinylreste gebunden.
Synthese des 2,3‐Dioxochinolizins und des 2‐Äthoxalylindolizidon‐3
Authors: Winterfeld K. , Erning W.
Published: October 2006

Wurde 2‐Pyridylessigsäureäthylester (V) mit Brombrenztraubensäureäthylester (III) zur Reaktion gebracht, so entstand 1‐Carbäthoxy‐2,3‐dioxochinolizin (VI), das sich zum 2,3‐Dioxochinolizin (VII) verseifen und zum 1‐Carbäthoxy‐2,3‐dioxo‐tetrahydrochinolizin (VIII) hydrieren ließ.

Beim Versuch, 3,4‐Dioxo‐2‐carbäthoxy‐chinolizidin (XI) durch Ringschluß von 2‐Piperidyl‐α‐äthoxyalylpropionsäureäthylester (IX) zu erhalten, entstand 2‐Äthoxalyl‐indolizidon‐3 (X), dessen Struktur durch Verseifen zur Indolizidonyl‐2‐α‐oxo‐essigsäure (XII) gesichert wurde. Beim Erhitzen von IX mit Natriumäthylat in siedendem Xylol bildete sich α,β‐Dioxo‐α,β‐diindolizidonyl‐2‐äthan (XIII).
Stereochemische Untersuchungen an 1,4‐substituierten Cyclohexanderivaten. 4‐Hydroxy‐ bzw. 4‐Amino‐cyclohexen‐carbonsäure‐(1) und entsprechende Ester; 4‐Hydroxy‐1‐hydroxymethyl‐cyclohexan
Authors: Schneider Woldemar , Hüttermann A.
Published: October 2006

Für die Messung der Dipolmomente werden die in der Überschrift genannten Verbindungen als cis‐ und trans‐Isomere dargestellt. Ihre Bildung auf verschiedenen Reaktionswegen und ihre Eigenschaften werden diskutiert.
Der Einfluß der Phosphorsäureesterstruktur und des Charakters der Ionen der Metalle der IV. Nebengruppe auf die Dephosphorylierung
Authors: Trapmann H. , Devani M.
Published: October 2006

Isomere Mononucleotide liefern ein weiteres Beispiel dafür, daß die Struktur der Phosphorsäureester für eine unterschiedlich rasche Dephosphorylierung, bei Verwendung des gleichen Katalysators, mitverantwortlich ist. Eine weitere Ursache für Unterschiede in der Phosphatabspaltung ist durch die Natur der Metall‐Ionen und ihre verschiedenen Hydroxidformen gegeben; dies zeigen Ergebnisse, die mit Th‐, Hf‐, Zr‐ und Ti‐Ionen erzielt werden.
Die Einwirkung von Chlorkohlensäureäthylester auf tertiäre Amine. 4. Mitt.: Untersuchungen über den Einfluß sterischer Faktoren auf die CKE‐Spaltung
Authors: Knabe J. , Shukla U. R.
Published: October 2006

Zur Klärung der Frage, ob die verminderte Reaktivität einiger tertiärer Amine, die an sich die konstitutionellen Voraussetzungen für eine glatte CKE‐Spaltung erfüllen, lediglich auf die Abschirmung des Stickstoffs zurückzuführen ist, oder ob der glatte Verlauf eventuell auch durch die Position des freien Elektronenpaares am Stickstoff entscheidend beeinflußt wird, werden die beiden aus der Literatur bekannten diastereomeren rac. 4‐Methyltetrahydroberberine IX und X hergestellt und mit CKE umgesetzt. Sowohl IX, das ein trans‐, als auch X, das ein cis‐Chinolizidin‐Ringsystem besitzt, werden von CKE nicht angegriffen. Es ist also nicht die Stellung des einsamen Elektronenpaares am Stickstoff für den Ablauf der CKE‐Spaltung ausschlaggebend, sondern der abschirmende Effekt benachbarter Substituenten — hier der Einbau des Stickstoffs in das bizyklische Chinolizidinringsystem —, der den Angriff von CKE verhindert.
Über die Biosynthese der Alkaloide in Nuphar luteum
Authors: Schütte H. R. , Lehfeldt J.
Published: October 2006

Es wurde die Biosynthese des Thionbinupharidins in Nuphar luteum mit Hilfe radioaktiv markierter Vorstufen durchgeführt. Cadaverin‐[1,5‐14C] zeigte eine Einbaurate von 0,061% und Mevalonsäure‐[3,4‐14C] eine von 0,048%. Der Abbau durch Kuhn‐Roth‐Oxydation ergab einen spezifischen Einbau der Mevalonsäure‐[3,4‐14C], aber eine unspezifische Cadaverin‐[1,5‐14C]‐Inkorporierung.
Synthese von Glucosiden der Chinolinreihe nach dem Hilbert‐Johnson‐Verfahren. 9. Mitt. über „Glykoside von Heterocyclen”︁
Authors: Wagner G. , Schmidt R.
Published: October 2006

Nach der Hilbert‐Johnson‐Synthese wurden erhalten: aus 2‐Äthoxychinolin 2‐(Tetraacetyl‐1‐α‐D‐glucosyloxy)‐chinolin, aus 4‐Äthoxychinolin ein Gemisch der Anomere des 1‐(Tetraacetyl‐1‐D‐glucosyl)‐chinolons‐(4), aus 1‐Äthoxyisochinolin je nach den Versuchsbedingungen das α‐ bzw. β‐Anomere des 1‐(Tetraacetyl‐1‐D‐glucosyloxy)‐isochinolins und aus 2‐ bzw. 4‐Äthoxychinolin‐N‐oxid das 1‐(Tetraacetyl‐1‐β‐D‐glucosyloxy)‐chinolon‐(2) bzw. ‐(4). Aus 4‐Äthylmercaptochinolin wurde nach Umsetzung mit α‐ABG nach dem Hilbert‐Johnson‐Verfahren das 1‐(Tetraacetyl‐1‐β‐D‐glucosyl)‐4‐äthylmercapto‐chinoliniumbromid erhalten, das durch Erhitzen in Toluol in 1‐(Tetraacetyl‐1‐β‐D‐glucosyl)‐thiochinolon‐(4) und durch Behandlung mit wäßriger Bromwasserstoffsäure in das 1‐(1‐β‐D‐Glucosyl)‐4‐äthylmercapto‐chinoliniumbromid übergeführt werden konnte.
Reaktionen mit Poly‐isonitrilen. 3. Mitt.
Authors: Neidlein R.
Published: October 2006

Di‐isonitrile reagieren mit Stickstoffwasserstoffsäure und Enaminen bzw. Aldehyden zu basischen Bistetrazolen bzw. Hydroxy‐bistetrazolen. Di‐isonitrile bilden mit Ketonen und Aminosäuren als Reaktionspartner Bisazetidinone, mit Ketonen und Carbonsäuren Bis(α‐acylhydroxy)‐carbonsäureamide, sowie mit Aminen, Carbonsäuren und Carbonylverbindungen Bis(α‐acylamino)‐carbonsäureamide.
Notiz über die Darstellung von β‐Amino‐propiophenonen aus aromatischen Aminen und Phenyl‐äthinyl‐carbinol
Authors: Reisch J.
Published: October 2006

β‐Amino‐propiophenone lassen sich aus Phenyl‐äthinyl‐carbinol und aromatischen Aminen durch Erhitzen in Gegenwart basischer Katalysatoren in 30–50proz. Ausbeute gewinnen. Die Reaktion stellt ein Beispiel für die vorteilhafte Anwendung von sekundären α‐Hydroxy‐acetylenen zur intermediären Bildung sonst instabiler Vinylketone dar.
Die Bildung von Pyrrolen aus γ‐Acetylenketonen
Authors: Reisch J.
Published: October 2006

γ‐Acetylenketone bilden beim Erhitzen mit primären Aminen in Gegenwart saurer Katalysatoren Pyrrolderivate. Bei β‐Acetylenketonen hat unter den gleichen Bedingungen eine prototrope Umlagerung zu den isomeren Allenketonen den Vorrang, die eine Pyrrolbildung ausschließt.
Darstellung von Hydroxylactamen durch Quecksilber(II)‐ÄDTA‐Dehydrierung. 7. Mitt.: Abstand der Hydroxylgruppe vom Stickstoff als Voraussetzung für die Lactambildung bei Aminoalkoholen
Authors: Möhrle H.
Published: October 2006

Eine Lactambildung bei der Quecksilber(II)‐ÄDTA‐Dehydrierung kann sowohl bei N‐β‐Hydroxyäthylpiperidin‐ als auch bei N‐γ‐Hydroxypropylpiperidinderivaten beobachtet werden, nicht aber bei einer δ‐Stellung des Hydroxyls in bezug auf den Stickstoff. Dies macht einen cyclischen Übergangs‐zustand mit Fünfring‐ oder Sechsringcharakter wahrscheinlich.
Über Umsetzungsprodukte der aus rhodanierten Schiffschen Basen erhaltenen Disulfide und Sulfide. 12. Mitt.: Über organische Rhodanverbindungen
Authors: Fröhling D. , Pohloudek‐Fabini R.
Published: October 2006

Es wird über die Spaltung von Azomethindisulfiden und ‐sulfiden in ihre Aldehyd‐ und Aminkomponenten, ihre Reduktion mit Natriumborhydrid und ihr Verhalten gegenüber Raney‐Nickel berichtet. Die Reduktionen der Azomethindisulfide führten zu den gleichen Verbindungen wie die analoge Behandlung der rhodansubstituierten Schiffschen Basen. Die Azomethinsulfide, die bei der Reaktion der Schiffschen Basen und ihrer Disulfide mit Raney‐Nickel entstanden waren, wurden mit Natriumborhydrid zu den entsprechenden hydrierten Produkten umgesetzt, während die katalytische Hydrierung in Gegenwart von Raney‐Nickel als Katalysator abweichend hiervon in einigen Fällen ohne Eliminierung des Schwefels verlief.
Zur NH‐Acidität und Lactam‐Lactim‐Tautomerie 1,5,5‐trisubstituierter Barbitursäuren
Authors: Roth H. J. , Jäger K. , Brandes R.
Published: October 2006

Da sich 1,5,5‐trisubstituierte Barbitursäuren, die an N‐1 eine Methylgruppe tragen, an N‐3 aminomethylieren lassen, dagegen solche, die an N‐1 eine Aminomethylgruppe besitzen, keiner weiteren Aminomethylierung zugänglich sind, darf angenommen werden, daß bei ersteren das Lactam‐Lactim‐Gleichgewicht zugunsten der Lactamform, bei letzteren zugunsten der Lactimform verschoben ist, die durch Ausbildung einer intramolekularen Wasserstoffbrücke fixiert wird.
Natur‐ und Geschichtswissenschaft im 19. Jahrhundert
Authors: Demandt Alexander
Published: October 2006

Die engen Verbindungen zwischen Natur‐ und Geschichtswissenschaft in der Zeit der Aufklärung haben sich im 19. Jahrhundert gelockert. Die meisten Historiker seitdem verfügen über eine gute Grundausbildung in der Philologie, teilweise auch in der Jurisprudenz, besitzen aber keine vergleichbare Grundkenntnis der Naturwissenschaften. Dennoch gibt es im 19. Jahrhundert drei Versuche, Geschichtswissenschaft nach dem Vorbild der Naturwissenschaft zu betreiben. 1. In der marxistischen Historiographie werden ökonomische und soziale Prozesse in enger Analogie zu Naturvorgängen, als „naturwüchsig”︁ gesehen. 2. Darwinistische Autoren betrachten menschliches Verhalten als weitgehend durch biologische Faktoren determiniert. 3. Die sogenannten Positivisten (zum Beispiel Thomas Buckle) benutzen Statistiken und mathematische Modelle in ihren historischen Schriften. Mehrere Jahrzehnte wurden derartige Ansätze durch traditionelle (historistische) Historiker zurückgewiesen (so von Gustav Droysen) mit dem Argument, daß die Historie eine Wissenschaftsui generis sei. Schließlich aber wurden positivistische Elemente in den Historismus aufgenommen. Max Weber vor allem hat gezeigt, bis zu welchem Ausmaß historisches Verständnis sich auf Idealtypen und Regelmäßigkeiten im Ereignisverlauf stützen kann. Auf der anderen Seite betonen neuerdings Naturwissenschaftler die Rolle solcher Elemente in ihren Disziplinen, die bisher als Kennzeichen der Geisteswissenschaften gegolten haben: den Einfluß subjektiver Faktoren auf wissenschaftliche Befunde und die Bedeutung von statistischen Wahrscheinlichkeiten anstelle stringenter Gesetzesaussagen.
Beziehungen zwischen Naturwissenschaft und Jurisprudenz in der ersten Hälfte des 19. Jahrhunderts
Authors: Herberger Maximilian
Published: October 2006

A central problem for legal thinkers of the 19th century was the question, whether the treatment of the law could be conceived as a scientific activity in the true sense of the word. According to the criteria which had been proposed by Kant with regard to the natural sciences, different answers seemed to be possible. G. Hugo argued that material given by experience could not be subject of an „exact science”︁. P. J. A. Feuerbach on the contrary advocated a concept of legal thinking, in which the method of physics served as a model. These two positions indicate a certain lack of self‐confidence, as a foreign standard is accepted in determining the status of the own discipline. This situation can also be interpreted as indicator for a feeling of crisis prevailing from now on in the self‐assessment of jurisprudential activity. On this background it is possible to explain many arguments and theories in the field of jurisprudence, when the corresponding counterpoint in one of the natural sciences is taken into consideration. A characteristic example is the way, in which F. K. v. Savigny has been shaping his „organic”︁ theory of specific legal correlations according to the physiological way of analysis proposed by C. C. E. Schmid. Even a statement like the one of J. H. v. Kirchmann, in which legal activity is denied any scientific value, has to be understood in this context. For Kirchmann takes the natural sciences as uncontested scientific model and accepts in this way the parameters of evaluation set by jurists like Hugo, Feuerbach and Savigny. It has still to be evaluated, whether this stream of theory led to a „turning point”︁ in the development of 19th century legal thinking, as J. E. Kuntze put it in 1856. But already now it can be stated that the close contact between Kuntze and G. Th. Fechner has been contributing to a diagnostic sensitivity on the part of Kuntze, which makes him an observer of special insight. Thus it may well be that the considerations sketched here have been introducing a leading theme into the following theoretical discussions in the field of jurisprudence during the second half of the 19th century. This question deserves further interdisciplinary research.
Natur und Staat. oder: Was lernen wir aus den Prinzipien der Deszendenztheorie in Beziehung auf die innerpolitische Entwicklung und Gesetzgebung der Staaten?
Authors: Winau Rolf
Published: October 2006

„What do the principles of evolutionary theory teach us in respect of the inner development and legislation of commonwealths?”︁ This was the subject set by three professors, Haeckel, Conrad, and Fraas, for a competition financed by Krupp in 1900. Sixty entries were submitted, eight of which received prizes and were published in the series „Natur und Staat”︁. The present article scrutinizes in the main those entries that, unlike Wilhelm Schallmayer's Vererbung und Auslese im Leben der Völker, did not become better known by going through several printings. The studies by Heinrich Matzat, Philosophie der Anpassung, by Albert Hesse, Natur und Gesellschaft, and Arthur Ruppin, Darwinismus und Sozialwissenschaft, all of which received second prizes, come under this heading. Because they throw light on the wide range of Social Darwinism at the beginning of the 20th century, Alfred Methner's tract Organismen und Staaten and Walter Haecker's Die ererbten Anlagen und die Bemessung ihres Wertes Für das politische Leben are also commented upon. The analysis does not yield an unified picture of Social Darwinism but shows common traits like the opinion that common wealth must precede private interest, that man's decisions are determined by scientific knowledge, that the endangered hereditary potential had to be safeguarded by state intervention. The discussion about these problems began in that period and lead to a basic consensus at the time of the Weimar republic with its fatal consequences.
Politisch motivierte Emigration deutscher Ärzte
Authors: Baader Gerhard
Published: October 2006

In 1933 the nazis had immediately started to reorganize the health service and the medical profession on the basis of eugenics and efficiency. For everybody who had been engaged in the institutions of social medicine or social hygiene in the Weimar Republic the inhibition of medical practice, misery, distress, persecution, imprisonment or at the best emigration had been the consequence of it, for political and mostly also for racial reasons. But for these physicians who had to flee from Nazi‐Germany the situation in the immigration countries had not been a good one in most of the cases. Therefore it is only possible to speak ‐ if you neglect the special situation of the psychiatrists in the U.S.A. ‐ in particular cases of transfer of medical science into the immigration countries from Germany. Most of the immigrants stayed after the war in their new homelands. The loss of these progressive aspects of social hygiene caused by the emigration of these physicians 1933 and afterwards from Germany can be noticed in this field of medicine and public health service in Western Germany until now.
Zur Sozialgeschichte des chemischen Hochschulfaches im 18. Jahrhundert
Authors: Meinel Christoph
Published: October 2006

The social history of chemistry as an academic discipline is dealt with in terms of competing programs of research and institutionalization, focussing on chemistry's transition from a medical curriculum to an economic and scientific context, as exemplified by universities such as Greifswald, Halle, Göttingen, and Jena in the late eighteenth century. Special attention is given to those factors that constitute, stabilize, and, eventually, re‐formulate disciplinary identity.
HIV‐1‐infected children on HAART: Immunologic features of three different levels of viral suppression
Authors: Zaccarelli‐Filho Carlos Alberto , Ono Erika , Machado Daisy Maria , Brunialti Milena , Succi Regina Célia de Menezes , Salomão Reinaldo , Kallás Esper Georges , de Moraes‐Pinto Maria Isabel
Published: October 2006

Background:

HIV‐1‐infected children show changes of blood lymphocyte subpopulations. We have, therefore, investigated how highly active anti‐retroviral therapy (ART) alter these subsets. Blood samples were taken from 41 HIV‐1‐infected children on ART who were divided into groups showing good, partial and poor responses to ART on the basis of viral load (VL) measurement in blood. The observations were compared to those seen in 20 uninfected children.

Methods:

The samples were studied using 4‐color flow cytometry for “naïve”, central memory and effector memory cells as well as for CD38 expression as the sign of activation within both the CD4+ and the CD8+ T cell populations. HIV‐1 infected children were also evaluated for the presence and the titers of antibodies induced by vaccination against childhood infections in our patients while on HAART.

Results:

Lymphocyte counts were lower in the “poor” viral load responding (VLR) group when compared with partial and good VLRs. Poor VLRs had lower total and naïve CD4+ T cell counts. HIV‐1‐infected children from all three groups had high CD8+ T cell counts. Central memory CD4+ and CD8+ T cell percentages were particularly low in the poor VLR group while in the poor VLR group the percentages of effector memory CD4+ and CD8+ T cells were higher when compared with the control group. Higher cellular activation of CD8+ T cells was observed in HIV‐1‐infected children, particularly when analyzed for the intensity of CD38 expression in the poor VLR group. CD5 expression on B cells was higher among all HIV‐1‐infected children. Antibodies to tetanus, diphtheria, measles, rubella, and hepatitis B were present in a large proportion of children but the titers were similarly low for all three groups of HIV‐infected children.

Conclusions:

Children with different levels of viral response to HAART present immune phenotype characteristics that tend to place the children with partial and good virological responses into the same group. These children are still moderately deficient in their immune responses but show better recovery than seen with children in the poor VLR group. These observations indicate that the proportions of central memory cells among the CD4+ T cells and the intensity of the expression of CD38 activation antigen on CD8+ T cells provide more informative parameters for monitoring children on HAART than the absolute numbers of CD4+ and CD8+ T cells alone. © 2006 International Society for Analytical Cytology
Fluoxetine treatment increases trabecular bone formation in mice
Authors: Battaglino R. , Vokes M. , Schulze‐Späte U. , Sharma A. , Graves D. , Kohler T. , Müller R. , Yoganathan S. , Stashenko P.
Published: October 2006

Mounting evidence exists for the operation of a functional serotonin (5‐HT) system in osteoclasts and osteoblasts, which involves both receptor activation and 5‐HT reuptake. In previous work we showed that the serotonin transporter (5‐HTT) is expressed in osteoclasts and that its activity is required by for osteoclast differentiation in vitro. The purpose of the current study was to determine the effect of treatment with fluoxetine, a specific serotonin reuptake inhibitor, on bone metabolism in vivo. Systemic administration of fluoxetine to Swiss–Webster mice for 6 weeks resulted in increased trabecular BV and BV/TV in femurs and vertebrae as determined by micro‐computed tomography (µCT). This correlated with an increase in trabecular number, connectivity, and decreased trabecular spacing. Fluoxetine treatment also resulted in increased volume in vertebral trabecular bone. However, fluoxetine‐treated mice were not protected against bone loss after ovariectomy, suggesting that its anabolic effect requires the presence of estrogen. The effect of blocking the 5‐HTT on bone loss following an LPS‐mediated inflammatory challenge was also investigated. Subcutaneous injections of LPS over the calvariae of Swiss–Webster mice for 5 days resulted in increased numbers of osteoclasts and net bone loss, whereas new bone formation and a net gain in bone mass was seen when LPS was given together with fluoxetine. We conclude that fluoxetine treatment in vivo leads to increased bone mass under normal physiologic or inflammatory conditions, but does not prevent bone loss associated with estrogen deficiency. These data suggest that commonly used anti‐depressive agents may affect bone mass. J. Cell. Biochem. 100: 1387–1394, 2007. © 2006 Wiley‐Liss, Inc.
A convenient procedure for preparing naltrexone‐15,16‐3H2 and naloxone‐15‐3H of high specific activity
Authors: Brine George A. , Kepler John A.
Published: October 2006

Mercury(II) oxide oxidation of naltrexone (1a) and naloxone (1b) gave 15,16‐didehydronaltrexone (4a) and 15,16 didehydronaloxone (4b). Subsequent reduction of 4a with tritium gas afforded naltrexone‐15,16‐3H2 having a‐specific activity of 15.3 Ci/mmole. Subsequent equilibration of 4b with carrier free tritium oxide followed by sodium cyanoborohydride reduction yielded naloxone‐15‐3H having a specific activity of 4 Ci/mmole.
Synthese de tris‐(dimethylamino‐2,4,6) triazine‐1,3,5 14C‐2‐4‐6 (hexamethylmelamine (noyau) 14C‐2‐4‐6), un nouvel agent antitumoral
Authors: Nguyen‐Hoang‐Nam  , Hoellinger Henri , Pichat Louis
Published: October 2006

L'hexaméthylmélamine (noyau) 14C‐2‐4‐6 (HMM 14C), un nouvel agent antitumoral, a été synthétisée à partir de l'urée 14C en 2 stades. L'urée 14C est cyclisée dans l'o‐dichlorobenzène en acide cyanurique 14C‐2‐4‐6, purifié par chromatographie sur colonne d'échangeur d'ions Séphadex SP C‐25. L'amination directe de l'acide en présence de HMPT et de diméthylamine donne l'HMM 14C. Aprés purification par chromatographie sur colonne de gel de silice d'adsorption, on obtient. l'HMM 14C avec un rendement radioactif global de 18 % par rapport à l'urée 14C, activité spécifique : 32 mCi/mMole.
Preparation of 6‐3H glucocerebroside
Authors: McMaster Marvin C. , Radin Norman S.
Published: October 2006

Glucocerebroside (1–0‐β‐glucosyl ceramide) can be labeled with 3H‐borohydride at the 6‐position of the glucose moiety. The 6‐trityl ether of cerebroside is formed first, the remaining hydroxyl groups are acetylated, the trityl group is removed, and the free 6‐hydroxyl group is oxidized to an aldehyde. The carbonyl group is then reduced with borohydride and the acetyl groups are removed, regenerating the original glycolipid.
Synthesis of 7‐chloro‐1,3‐dihydro‐5‐(2‐fluorophenyl)‐1‐methyl‐2H‐1,4‐benzodiazepin‐2‐one‐5‐14C (fludiazepam‐14C)
Authors: Nakatsuka Iwao , Kawahara Kazuo , Kamada Takeshi , Shono Fumiaki , Yoshitake Akira
Published: October 2006

7‐Chloro‐1,3‐dihydro‐5‐(2‐fluorophenyl)‐1‐methyl‐2H‐1,4‐benzodiazepin‐2‐one (Fludiazepam) (I), an anti‐anxiety agent, was labelled with carbon‐14 at C‐5 position for metabolic studies. The reaction sequence for the synthesis is shown in Fig. 2. o‐Fluorobenzoic‐14C acid (IV) was prepared in 65% yield by carbonation of o‐fluorophenyllithium with carbon‐14C dioxide. The acid (IV) was condensed with N‐(4‐chlorophenyl)‐N‐ methylethylenediamine, followed by Bischler‐Napieralski cyclization of the resulting amide with phosphorus pentoxide and phosphorus oxychloride to afford 7‐chloro‐2,3‐dihydro‐5‐(2‐fluorophenyl)‐1‐methyl‐1H‐1,4‐benzodiazepine‐5‐14C (VII) in good yield. Oxidation of VII by N‐bromosuccinimide in aqueous solution of sodium bicarbonate gave Fludiazepam‐14C (I). The overall yield of I was 24% from barium carbonate‐14C.
Preparation of 14C‐Labelled Vincristine and N‐Desmethyl‐N‐formyl‐leurosine
Authors: Zóyomi Gábor , Jovánovics Karola , Dancsi Lajos
Published: October 2006

14C‐Labelled vincristine was prepared from N‐desmethyl vinblastine by formylation with 14C‐formic acid. Excess radioactive formic acid was recovered as sodium formate. 14C‐Labelled N‐desmethyl‐N‐formyl‐leurosine was prepared analogously.
The preparation and purification of 3–(4‐iodophenoxy)‐1‐isopropylamino‐2‐propanol‐125I, a beta adrenergic antagonist
Authors: Bobik A. , Woodcock E. A. , Johnston C. I. , Funder W. J.
Published: October 2006

The preparation of an iodine‐125 labelled beta adrenergic ligand, 3–(4‐iodophenoxy)‐1‐isopropylamino‐2‐propanol, suitable for β‐adrenergic receptor membrane binding studies is described. Several preparations have been carried out with radiochemical yields of 20–30%. Specific activities in the order of 150 Ci/mmol are readily obtained.
Synthesis of trideuterated testosterone labeled selectively at the C‐19 angular methyl group
Authors: Baba S. , Shinohara Y. , Kasuya Y.
Published: October 2006

A synthetic procedure for testosterone‐19, 19, 19‐d3 is described. Deuterium labeling of the C‐19 position was achieved by the Grignard reaction of 17β‐acetoxy‐5α, 10α‐epoxy‐estrane‐3‐cycloethyleneketal with deuterium labeled methyl magnesium bromide (CD3MgBr). The synthesis resulted in a product with 97.8% d3 isotopic purity, which is selectively deuterated at C‐19 and chemically pure.
Preparation of [1‐14C]‐ and [9,10‐3H]‐Trans‐9‐Octadecenoic Acids from the Corresponding cis‐Compounds
Authors: Christie William W.
Published: October 2006

[1‐14C]‐Trans‐9‐octadecenoic acid was obtained in 60 per cent overall yield and [9,10‐3H]‐trans‐9‐octadecenoic acid in 30 percent yield by stereomutation of the double bonds in the corresponding cis ‐compounds with nitrous acid in toluene. The products were purified by silver nitrate chromatography and contained no detectable positional isomers.
125I‐Labeled 1‐(2′‐acetyl‐4′‐[ortho‐iodobenzoyl]‐aminophenoxy)‐3‐isopropyl‐ aminopropan‐2‐ol
Authors: Hanson Robert N. , Davis Michael A. , Holman B. Leonard
Published: October 2006

The preparation of the iodine‐125 labeled beta adrenergic antagonist, 1‐ (2′‐acetyl‐4′‐[ortho‐iodobenzoyl] ‐aminophenoxy)‐3‐isopropylamino‐propan‐2‐ol, suitable for biodistribution studies is described. Synthesis of the unlabeled precursor proceeds in a 44% yield and the iodine‐125 exchange results in 89% incorporation of label. The final product is radiochemically pure (98‐99%) with a specific activity of 3.2 Ci/mmol.
11C‐Labelled radiopharmaceuticals: Synthesis and high pressure liquid chromatography of nicotinic‐11C acid amide
Authors: Machulla H.‐J. , Dutschka K.
Published: October 2006

Starting with 11CO2, [carboxyl‐11C]‐nicotinic acid amide was synthesized via 3‐pyridyl‐lithium in practically carrier‐free amounts within 60 minutes. Overall radiochemical yields between 20% and 30% were obtained. Identification and purification of the labelled product was carried out by high pressure liquid chromatography using water as eluent.
Synthesis of carbon‐14 and carbon‐13 labeled chlorinated polycyclic pesticides
Authors: Heys J. R. , Duncan W. P. , Perry W. C. , Ebert D. A. , Radolovich G. , Haile C. L.
Published: October 2006

The preparations of the pesticides 1,1a,2,2,3,3a,4,5,5,5a,5b,6‐dodecachlorooctahydro‐1,3,4‐metheno‐1H‐cyclobuta[cd]pentalene‐U‐C14 (mirex‐U‐C14), 1,1a,3,3a,4,5,5,5a,5b,6‐decachlorooctahydro‐l,3,4‐metheno‐2H‐cyclobuta[cd]pentalen‐2‐one‐U‐C14 (Kepone™‐U‐C14), ethyl 5‐(1,1a,3,3a,4,5,5,5a,5b,6‐decachlorooctahydro‐2‐hydroxy‐l,3,4‐metheno‐1H‐cyclobuta[cd]pentalen‐2‐Y1‐1,1a,2,3,3a,4,5,5a,5b,6‐C1410)‐ levulinate (kelevan‐C14), 1,4,5,6,7,8,8‐heptachloro‐3a,4,7,7a‐tetra‐hydro‐4,7‐methanoindene‐4,5,6,7,8‐C514 (heptachlor‐4,5,6,7,8‐C514) and 1,4,5,6,7,8,8‐heptachloro‐2,3‐epoxy‐3a,4,7,7a‐tetrahydro‐4,7‐methanoindan‐4,5,6,7,8‐C514 (heptachlor epoxide‐4,5,6,7,8‐C514) from hexachlorocyclopentadiene‐U‐C14 are described. Specific activities were in the range of 1.8 to 3.2 mCi/mmol.

Further, the synthesis of mirex‐C213 and Kepone™‐C213 from isopropyl formate‐C13 is reported. The determination of the carbon‐13 enrichment of these compounds was accomplished by selected ion monitoring (SIM) of seven ions in the molecular clusters of mirex and Kepone™, followed by calculation of the relative abundance of the various carbon‐13 containing molecules from the areas of the SIM plots.
The synthesis of non‐exchangeable deuterated internal standards for imipramine and its metabolites
Authors: Woodard R. W. , Craig J. Cymerman
Published: October 2006

The synthesis of 10,11‐dihydro‐5‐(3‐dimethylaminopropyl)‐5H‐dibenz[b,f]azepine (imipramine) and its 3‐methylamino analogue (desipramine)labelled with deuterium in either the 1‐ or the 3‐position of the side chain in high isotopic purity is described. The 3,3‐d2 compounds are obtained from the common precursor 5‐(2‐cyanoethyl)‐10,11‐dihydro‐5H‐dibenz[b,f]azepine by reduction and alkylation, while the 1,1‐d2 products are accessible from the 5‐(3‐chloropropionyl) derivative by amination and reduction. These compounds are required for use as non‐exchangeable mass spectrometric stable isotope internal standards for the simultaneous determination of imipramine and desipramine in biological fluids.
Synthesis of trans‐2,2‐Dimethyl‐3‐phenyl‐4‐(p‐β‐pyrrolidinoethoxy)phenyl‐7‐methoxy‐[2‐14C]chroman
Authors: Kole P. L. , Ray Suprabhat
Published: October 2006

The synthesis of trans‐2,2‐dimethyl‐3‐phenyl‐4‐(p‐β‐pyrrolidinoethoxy) phenyl‐7‐methoxy‐[2‐14C]chroman (Centchroman), a post‐coital antifertility agent from [1‐14C]phenylacetic acid is reported.
Synthesis of 2‐14c‐labelled 3H‐1,4‐benzodiazepines
Authors: Tegyey Z. S. , Maksay G. , Ötvös L.
Published: October 2006

2‐14C‐oxazepam (7) 2‐14C‐(+)‐ and ‐(‐)‐7‐chloro‐1‐methyl‐5‐phenyl‐1,3,4,5‐tetrahydro‐3H‐1,4‐benzodiazepine‐2‐one (8a and 8b) as well as 2‐14‐7‐chloro‐4‐carbamoyl‐1‐methyl‐5‐phenyl‐1,3,4,5‐tetrahydro‐3H‐l,4‐benzodiazepine‐2‐one (9) were synthesised from carbobenzoxy‐glycine‐1‐14C. The overall radiochemical yields from carbobenzoxy‐glycine‐1‐14C were 28.9 % (7), 9.5 % (8a and 8b) and 25.3 % (9), respectively.
Convenient syntheses of N‐CD3 labelled nicotine and nicotine analogues
Authors: Seeman Jeffrey I. , Secor Henry V. , Forrest Gary
Published: October 2006

Two procedures for the preparation of N‐CD3 labelled nicotine and nicotine analogues are reported. These include: (a) the deuteroiodomethylation of the lithium amide of the corresponding secondary amine; and (b) the alkylation of the corresponding cyclic imine followed by sodium cyanoborohydride reduction of the resulting alkyl iminium salt. Products having both high chemical and isotopic purity are formed.
Synthesis of labelled histamine H2‐receptor antagonists I. Synthesis of deuterium, sulfur and tritium labelled cimetidine and metiamide by exchange
Authors: Hesselbo T. , Slade S. W. , Villani A. J. , Petka L.
Published: October 2006

The H2‐antagonists, metiamide and cimetidine were lahelled with deuterium and tritium in the 2‐position of the imidazole ring by the uncatalyzed exchange reaction with deuterium and tritium oxide at 100°C. The sulfur‐35 labelled metiamide was prepared by an exchange reaction with elemental sulfur‐35 in refluxing pyridine and by the reaction of 2[(4‐methyl‐5‐imidazolyl)methylthio]ethylamine with methylisothiocyanate‐35S in refluxing ethanol.
Labelled organophosphorus pesticides. III. Synthesis of carbon‐14 labelled o‐(2,6‐dichloro‐4‐methylphenyl) O,O‐dlmethyl phosphorothioate
Authors: Yoshitake Akira , Kanamaru Hiroshi , Shono Fumiaki , Nakatsuka Iwao
Published: October 2006

O‐ (2,6‐Dichloro‐4‐methylphenyl) O,O‐dimethyl phosphorothioate (5‐3349) (1), a fungicide in soil, was labelled with carbon‐14 individually at the aryl methyl and the phenyl ring for use in metabolic studies. The synthetic procedures are illustrated in Fig. 1. 4‐Cyano‐14C‐phenol was quantitatively converted to 4‐methyl‐14C‐Phenol (3a) by catalytic hydrogenation using 10% Pd‐C as a catalyst. Dichlorination of 3a with chlorine gave 2,6‐di‐chloro‐4‐methyl‐14C‐phenol (4a). Condensation of 4a with O,O‐dimethyl phosphorochloridothioate gave S‐3349‐(aryl methyl‐14C) (1a) in the overall yield of 22% from potassium cyanide‐14C. By the similar procedures, 4‐methylphenol‐14C6 (3b) was converted to S‐3349‐(Phenyl‐14C6) (1b) in 70% yield.
The synthesis of cholesterol‐2,2,4,4,6‐d5
Authors: Gruenke Larry D. , Craig J. Cymerman
Published: October 2006

Cholesterol‐3,4‐d2 and ‐2,2,4,4,6‐d5 have been synthesized from Δ4 ‐ cholestene‐3‐one for use as mass spectrometric stable isotope internal standards. Conversion of Δ4 >‐cholesten‐3‐one to the enol acetate followed by reduction with sodium borodeuteride in a deuterated solvent yielded cholesterol‐3,4‐d2. Similarly Δ4‐cholesten‐3‐one‐2,2,4,6,6‐d5 obtained by base‐catalyzed exchange of Δ4‐cholesten‐3‐one in ethanol‐O‐d1 was converted to the enol acetate, followed by reduction with sodium borohydride in a deuterated medium to give cholesterol‐2,2,4,4,6‐d5.
Synthesis of the labeled gibberellin, GA9‐17‐14C
Authors: Lin Jiann‐Tsyh , Heftmann Erich
Published: October 2006

GA9‐17‐14C was synthesized by introducing 14C into GA9‐17‐norketone by the Wittig reaction. The NMR and mass spectra of free GA9 and GA9‐17‐norketone are presented. The diphenylmethyl‐14C‐phosphine oxide is formed as a byproduct.
Rapid synthesis of 2‐deoxy‐D (1‐14C) glucose suitable for labelling with 11C
Authors: Mestelan Geneviève , Aubert Francis , Beaucourt Jean‐Pierre , Comar Dominique , Pichat Louis
Published: October 2006

D‐arabitol (I) treated with acetone gave 2,3–4,5 and 1,2–4,5 di‐O‐isopropylidene‐D‐arabitol (II) as shown by 13C NMR. This mixture was converted into the corresponding mixture of mesylates from which 2,3–4,5‐di‐0‐isopropylidene‐1–0‐methane sulfonyl‐D‐arabitol (III) was isolated. The latter was converted into 1‐deoxy‐2,3–4,5‐di‐O‐isopropylidene‐1‐iodo‐D‐arabitol (IV). (IV) and sodium (14C) cyanide gave 2‐deoxy‐3,4–5,6‐di‐0‐isopropylidene‐D‐(1‐14C)‐glucononitrile (V) which was hemihydrogenated into 2‐deoxy‐D‐(1‐14C)‐glucose (VI). The overall yield based on sodium‐(14C)‐cyanide was 30 % and the radiochemical purity was 98 %. The overall time of synthesis was about one hour. This is suitable for working with 20 minutes halflived 11C.
Preparation of L‐cysteine‐35S hydrochloride by reduction of L‐cystine‐35s
Authors: Skakun‐Todorovi M. B. , Albahari S. R.
Published: October 2006

The method for the synthesis of L‐cysteine hydrochloride labelled with 35S is described. L‐cystine‐35S obtained from baker's yeast was reduced with tin in hydrochloric acid and radiochemically pure L‐cysteine‐35S hydrochloride was isolated by ion‐exchange chromatography on a column.

The obtained L‐cysteine‐35S hydrochloride was stable in aqueous solution, pH 2, for six months and had specific activity of 20–125 mCi/mmol and radiochemical purity better than 95%.
Synthesis of glycyl‐L‐prolyl‐L‐leucyl‐[14C(U)] glycyl‐L‐proline as a substrate for collagenase
Authors: Lam‐Thanh Hung , Heindl Marie‐Christine , Fermandjian Serge
Published: October 2006

The synthesis of the 14C labelled peptide glycyl‐L‐leucyl‐[14C(U)] glycyl‐L‐proline (I) with the specific activity of 50 μCi/mMole was performed by the Merrifield solid phase method. The peptide (I) was degraded by Achromobacter iophagus collagenase.
Nouvelles Syntheses du Chloropractolol: Marquage au 14C, 2H, 3H
Authors: Pilichowski Jean‐François , Godeneche Denise
Published: October 2006

Le chlorure de l'acide chloracétique(1‐14C a été obtenu, avec de bons rendements, par réaction d'échange entre le chlorure de benzoyle et l'acide chloracétique‐[1‐14C]. L'acylation de l'[(amino‐4 phénoxy)‐l, isopropylamino‐3, propanol‐2], par Ie réactif ainsi préparé a permis d'obtenir Ie Chloropractolol [1‐14C]avec une activité spécifique de 230 μCi/mmole. Nous décrivons également la synthèse du Chloropractolol deutérié et tritié (Activité Spécifique : 6,1 mCi/mmole) sur la position géminée avec le groupement hydroxyle.
The labeling of 4‐alkylamino‐iodoquinolines with radioactive iodine by isotopic exchange
Authors: Bakker Cees N. M. , Kaspersen Frans M.
Published: October 2006

4‐alkylamino‐iodoquinolines can be labeled as their phosphate salts in high yields and in a short period of time by nucleophilic exchange in a melt with radioactive iodide. The iodide must be free of NaCl and reducing agents.
General methods for the synthesis of methyl isotope labelled catecholamine metabolites. Preparation of 4‐hydroxy‐3‐methoxy‐d3‐ (mandelic acid, phenylacetic acid, and phenylethylene glycol)
Authors: Markey S. P. , Powers K. , Dubinsky D. , Kopin I. J.
Published: October 2006

Two general schemes for the synthesis of isotope labelled monomethyl catecholamine metabolites are described. Catechol was converted to 2‐methoxy‐d3‐phenol (2) with deuteromethyl iodide and reacted with sodium glyoxylate to form 4‐hydroxy‐3‐methoxy‐d3‐mandelic acid (3). Hydrogenolysis of the methyl ester‐diacetate of 3 with excess sodium borohydride in water yielded 4‐hydroxy‐3‐methoxy‐d3‐phenylacetic acid (4). Reduction of 3 with diborane produced 4‐hydroxy‐3‐methoxy‐d3‐phenylethylene glycol (5). An alternative route was to alkylate 3,4‐dihydroxybenzaldehyde (6) and produce 3 or its 3‐hydroxy‐4‐methoxy isomer via the nitrile mandelic acid synthesis. Suitability of these isotopic and isomeric variants as internal standards for quantitation by gas chromatography‐mass spectrometry is discussed.
Synthesis of 5‐deuteromethyl‐2′‐deoxyuridine (thymidine‐α,α,α‐d3) and related compounds
Authors: Shiue C.‐Y. , Wolf A. P. , Slatkin D. N.
Published: October 2006

Thymine‐α,α,α‐d3 (4) was synthesized from perdeuterated methyl iodide and pyrimidine‐lithium. Thymidine‐α,α,α‐d3 (8) was then synthesized by coupling compound 4 with 1α‐chloro‐2‐deoxy‐3,5‐bis(p‐toluoyl)‐α‐D‐ribofuranosyl chloride in the presence of Friedal‐Crafts catalyst. Thymidine‐α,α,α‐d3 (8), a metabolic precursor of deoxyribonucleic acid, has potential application for study of human tissue growth kinetics in vivo using a sensitive deuterium micromapping technique.