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  • 1
    ISSN: 1434-4475
    Keywords: 1,2-Amino-alcohols, enantiomerically pure ; Lithium aluminium hydride reduction
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Description / Table of Contents: Summary A synthesis of β-aminoalcohols is described starting from racemic or enantiomerically pure α-hydroxynitriles which were O-protected using enantiomerically pure acetal type protective groups. Reduction with lithium aluminium hydride yielded O-protected β-aminoalcohols. Whenever diastereomeric O-protected cyanohydrins could not be separated, the mixture was reduced and the resulting O-protected aminoalcohols were separated. Removal of the protective group using hydrogen chloride and methanol yielded enantiomerically pure β-aminoalcohols or their corresponding hydrochlorides.
    Notes: Zusammenfassung Die Reduktion enantiomerenreiner O-MBF- bzw. O-MBE-geschützter Cyanhydrine mit LiAlH4 führt unter Einhaltung definierter Reaktionsbedingungen zu den entsprechenden geschützten Aminoalkoholen, in denen der Anteil der durch Epimerisierung gebildeten Nebenprodukte kleiner als 3% ist. Die Abtrennung der unerwünschten Diastereomere erfolgt im Zuge der Reinigung der Produkte. Durch Schutzgruppenabspaltung mit Salzsäure/Methanol können die enantiomerenreinen Aminoalkohole erhalten werden. Die meist sehr guten Trennfaktoren der O-MBF- bzw. O-MBE-geschützten Verbindungen erlauben für viele Verbindungen sowohl im Cyanhydrin- als auch im Aminoalkoholstadium eine präparative Trennung und machen das Verfahren deshalb vielseitig verwendbar.
    Type of Medium: Electronic Resource
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  • 2
    ISSN: 1434-4475
    Keywords: 1,2-Amino-alcohols, enantiomerically pure ; N-Alkylation ; Clorprenaline ; Propranolol ; Midodrine
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Description / Table of Contents: Summary A synthesis of N-substituted β-aminoalcohols is described starting from enantiomerically pure O-MBF- or O-MBE-protected β-aminoalcohols which can be preparedvia LiAlH4 reduction of O-protected cyanohydrines.
    Notes: Zusammenfassung Clorprenalin und Propranolol können mit dem vorgestellten Verfahren in sehr guter Ausbeute aus den O-MBF-geschützten Aminoalkoholen durch reduktive Alkylierung in enantiomerenreiner Form hergestellt werden. Bei der Synthese von enantiomerenreinem Midodrin, bei der in der letzten Stufe gemeinsam mit der O- auch die N-Schutzgruppe (BOC) abgespalten wird, müssen bestimmte Reaktionsparameter (Zeit, Temperatur) präzise eingehalten werden, um eine entsprechende Enantiomerenreinheit der Endprodukte (〉95% ee) zu gewährleisten.
    Type of Medium: Electronic Resource
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  • 3
    ISSN: 1432-0584
    Keywords: Key words BMT ; Quality of life ; FACT-BMT ; EORTC-QLQ C30
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract  Quality of life (QoL) was investigated in 56 BMT recipients. The objective was to compare QoL in terms of physical, emotional, and social functioning between patients within the first year after BMT (n=15) and patients who were alive more than 1 year after BMT (n=41). The Functional Assessment of Cancer Therapy Scale (FACT-BMT) and the EORTC-Quality of Life Questionnaire (EORTC-QLQ C30) were used to evaluate QoL as perceived by the patients. Results show a significantly reduced general QoL in patients within the first year after BMT. Specific differences were identified on the dimensions of physical and emotional well-being and the symptom scales of appetite loss, fatigue, pain, dyspnea, and nausea and vomiting. QoL improves significantly with time after BMT. We suggest that there should be more integration of QoL expectancy into the pre-BMT information process. Patients should be informed about potential deficits in physical and emotional well-being within the first year after BMT. This could enhance insight and compliance in the critical period early after BMT.
    Type of Medium: Electronic Resource
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  • 4
    ISSN: 1432-2072
    Keywords: Schizophrenia ; D1-dopamine antagonists ; SCH 39166 ; Antipsychotic ; Negative symptoms
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract In the present open study the effects of the D1-dopamine antagonist SCH 39166 on positive and negative symptoms of schizophrenia (DSM-IIIR) were investigated. SCH 39166 was given orally according to a fixed dosage schedule (day 1: 25 mg b.i.d; day 4: 50 mg b.i.d.; day 7: 100 mg b.i.d; day 18: 200 mg b.i.d.; day 21: 225 mg b.i.d.). Seven patients completed 2 weeks, and five patients completed the study. The reason for premature withdrawal was lack of efficacy or refusal to take SCH 39166. In none of the patients a reduction of the BPRS or CGI score was found. As measured with the PANSS, a significant reduction was observed in the score of the negative subscale, whereas the positive symptoms scale and general psychopathology score remained unaffected. Akathisia, rigidity and hypokinesia were reported occasionally, although only mild in severity. The results of the present study do not support the hypothesis that D1-dopamine antagonists are clinically effective antipsychotics in schizophrenia, considering the fact that SCH 39166 had no effect on positive symptoms. The present study provides circumstantial evidence for an effect of SCH 39166 on negative symptoms.
    Type of Medium: Electronic Resource
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  • 5
    ISSN: 1432-2072
    Keywords: Clozapine ; Haloperidol ; Eosinophilia ; Neutropenia ; Agranulocytosis
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract The atypical antipsychotic clozapine carries a high risk of inducing agranulocytosis. We attempted to investigate whether eosinophilia during clozapine treatment has predictive value for subsequent neutropenia/agranulocytosis. One hundred and seventy-seven patients were studied in a prospective naturalistic design using haloperidol as the reference compound. Clozapine was found to differ from haloperidol in respect to their influence on neutrophil granulocytes. In the clozapine group patients with eosinophilia showed a decrease in neutrophil count (less than 2000/mm3 neutrophil granulocytes) significantly more often than patients without eosinophilia.
    Type of Medium: Electronic Resource
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  • 6
    Electronic Resource
    Electronic Resource
    Springer
    Psychopharmacology 118 (1995), S. 52-56 
    ISSN: 1432-2072
    Keywords: Antipsychotics ; Neuroleptics ; Clozapine Drug monitoring ; Side-effects ; Parkinsonism Tremor ; Bradykinesia ; Tardive dyskinesia Akathisia ; Haloperidol
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract Neuroleptic-induced extrapyramidal side effects (EPS) were evaluated in 92 patients treated with clozapine for the first time and 59 patients treated with haloperidol followed in a drug monitoring program. Side effects were measured by the Columbia University Rating Scale, the Simpson Dyskinesia Scale and the Hillside Akathisia Scale. The cumulative incidence rate for tremor was found to be 24.4% in the clozapine group and 39.3% in the haloperidol group. This did not amount to a statistically significant group difference. Bradykinesia was observed in 21.8% of the patients treated with clozapine and in 47.7% of the patients of haloperidol (P=0.011). In the clozapine group the akathisia incidence rate was 5.6%, whereas haloperidol patients showed a higher rate of 31.7% (P=0.005). Our results show higher incidence rates of tremor and bradykinesia during clozapine treatment than previous studies. We conclude that clozapine is not entirely free of EPS, but they are usually less severe and of a different quality than side effects induced by typical antipsychotics.
    Type of Medium: Electronic Resource
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  • 7
    Electronic Resource
    Electronic Resource
    Springer
    Monatshefte für Chemie 128 (1997), S. 53-59 
    ISSN: 1434-4475
    Keywords: Propafenone ; Enantiomeres ; Synthesis of ; Chiral pool ; Acetalization
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Description / Table of Contents: Zusammenfassung Eine kurze und effiziente Synthese der Enantiomere des Antiarrhythmikums Propafenon (1) unter Verwendung von sowohl (R)-Isopropylidenglycerintosylat als auch von (S)-Glycidyltosylat als chirale Bausteine wird beschrieben. Der Schlüsselschritt der in sehr guter Ausbeute verlaufenden Synthese ist die Acetalisierung der Carbonylgruppe in 1-(2-Hydroxyphenyl)-3-phenyl-1-propanon (2), welche die Anwendung milder Reaktionsbedingungen bei der anschließenden Alkylierung der phenolischen Hydroxylgruppe ermöglicht.
    Notes: Summary A short and efficient synthesis of the enantiomers of the antiarrhythmic drug propafenone (1) is described using both (R)-isopropylideneglycerol tosylate and (S)-glycidyl tosylate as chiral building blocks. The key step of the high yield synthesis is the acetalization of the carbonyl group in 1-(2-hydroxyphenyl)-3-phenyl-1-propanone (2) which allows application of mild reaction conditions in the subsequent alkylation of the phenolic hydroxy group.
    Type of Medium: Electronic Resource
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  • 8
    ISSN: 1433-0407
    Keywords: Schlüsselwörter Eisenbahn ; Suizid ; Fernsehen ; Werther-Effekt ; Key words Train ; Suicide ; Television ; Werther effect
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Description / Table of Contents: Summary Suicide on railways (either by being run over by or jumping in front of a train) is one of the ’hardest' suicide methods. In Austria, 617 suicides or attempted suicides on railways were registered between 1990 and 1994. This amounts to 5.73 % of all suicides committed in this period with women showing a higher percentage than men. In both men and women there was a predominance of younger age groups; the mean age was higher in women than in men (48.0 vs 40.4 years). There was a significant increase in suicides or attempted suicides on railways after a television report on the stress suffered by train drivers concerning possible suicides. Persuading the mass media to treat the subject of ’suicide' with reserve and with greater caution, even when not presenting a distinct suicide model, may be of importance in general suicide prevention.
    Notes: Zusammenfassung Selbstmord durch Überrollenlassen oder Werfen vor einen Zug stellt eine der härtesten Suizidmethoden dar. In den Jahren von 1990–1994 wurden in Österreich 617 versuchte oder vollzogene Eisenbahnsuizide registriert. Der Anteil an den Gesamtsuiziden betrug 5,73 %, wobei der Anteil bei den Frauen höher lag. Insgesamt waren v. a. jüngere Altersgruppen betroffen; das Durchschnittsalter der weiblichen Opfer war mit 48,0 Jahren höher als das der Männer (40,4 Jahre). Ein signifikanter Anstieg fand sich nach einer Fernsehsendung, in der über die psychische Belastung von Zugführern durch einen möglichen Eisenbahnsuizid berichtet wurde. Ein zurückhaltender Umgang der Medien mit dem Thema Suizid und eine größere Vorsicht in der Berichterstattung, auch wenn kein konkretes Suizidimitationsmodell dargestellt wird, scheint von bisher unterschätzter Bedeutung für die Suizidprävention zu sein.
    Type of Medium: Electronic Resource
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