bluuebunny/crossref_metadata_2025_split huggingface dataset:
The Reactions of Pindolol, Mepindolol, Carazolol, and Related Model Compounds with Triethyl Orthoformate: Pathways and Products of a New Colour Reaction
Authors: Pindur Ulf , Witzel Helmut 
Published: October 2006

AbstractThe acid‐catalysed electrophilic tandem substitutions of pindolol, mepindolol, and carazolol and some related model compounds with triethyl ortho formate give rise to new derivatives from the trishetaryl methan series. In some cases also further functionalised heterocycles were isolated. The structural aspects of the new trishetarylmethanes were discussed as C3‐symmetric molecular propellers, respectively. The importance of the described reaction as colour reaction was mentioned.
Bestimmung von Formaldehydspuren in wäßrigen Lösungen Determination of Traces of Formaldehyde in Aqueous Solutions
Authors: Spreitzer Helmut , Jäger Walter 
Published: October 2006

AbstractIm Zuge der Untersuchungen an Herzklappentransplantaten1) bestimmten wir die Glutaraldehyd‐Freisetzung mit dem Hydrazin 1 als Reagens2).
Molecular Pharmacological Aspects of Antiarrhythmic Activity, II1): Interaction of Class I Compounds with Calmodulin
Authors: Mannhold Raimund , Voigt Werner , Bast Aalt , Timmerman Hendrik 
Published: October 2006

AbstractWe have tested the calmodulin (CaM) inhibitory potency of class I antiarrhythmics in the phosphodiesterase (PDE) assay. The lipophilicity of the test compounds has been quantified by two experimental (log P, RM) and two calculative (Σf, C log P) procedures. Five antiarrhythmics (asocainol, aprindine, lorcainide, propafenone, and ethmozine) exhibit IC50 values < 250 μM for the inhibition of the CaM‐stimulated PDE activity. Lipophilicity seems to be a prime, but not the sole descriptor of CaM inhibitory potency. The functional means of CaM inhibition by the test compounds for their antiarrhythmic properties remains to be clarified in further investigations.
Synthesis and Reactions of 2(5)‐[Benzyl or Cyanomethyl]‐1,3,4‐oxadiazoles
Authors: Hamad M. M. 
Published: October 2006

AbstractA series of five membered heterocycles, namely 5‐(benzyl or cyanomethyl)‐3‐acetyl‐2,2‐disubstituted‐1,3,4‐oxadiazolines (3a‐e), 2,5‐disubstituted‐1,3,4‐oxadiazoles (4a, b), 2‐hydroxy‐5‐(benzyl or cyanomethyl)‐1,3,4‐oxadiazoles (5a, b), 1,2,5‐trisubstituted‐1,3,4‐triazoles (6a, b), and 2‐(benzyl or cyano‐methyl)‐1,3,4‐oxadiazole‐5‐thiols (10a, b), were synthesized. Also 5‐chloro‐2‐benzyl‐1,3,4‐oxadiazole 7 was prepared. Reaction of amines, hydrazines, and sodium azide with 7 gave the corresponding 2‐arylamino (8a, b), 5‐hydrazino or phenylhydrazino (8c, d) and 2‐azido derivatives 9, respectively. Mannich bases (11a, b) were prepared by the reaction of sec. amines with 9a. 5‐Carboxymethylthio‐1,3,4‐oxadiazoles (12a, b) and their ethyl esters (13a, b) were also prepared. The ester 13a reacted with amines and hydrazines to give the corresponding amides (14a‐d).
Hydrolysis and Oxidation of 1H‐Benzotriazole‐carboxylic Acid Esters by Rat Liver Microsomes
Authors: Jacobi Sylvia , Hoffmann Hermann 
Published: October 2006

AbstractThe 1H‐benzotriazole‐carboxylic acid esters under investigation were almost ‐ with the exception of the tert.‐butylester ‐ completely hydrolyzed by rat liver microsomes. Some substrates were metabolically oxidized to a very small extent (< 1 %) yielding small amounts of possibly toxic metabolites after inhibition of the esterases with paraoxone.
Anellierte Thiopyrone, 6. Mitt.: 2‐Acyl‐thiopyrone aus 1‐Indanon, 3‐Cumaranon und Thioindoxyl
Authors: Görlitzer Klaus , Vogt Regina 
Published: October 2006

AbstractAusgehend von den Thiopyranon‐2‐carbonsäuren 1 gelingt in einer 4‐stufigen Synthese die Darstellung der 2‐Formyl‐thiopyrone 7. Diese lassen sich über ihre Oxime 9 und Nitrile 10 zu den Tetrazolen 11 umsetzen. Die Boran‐Reduktion der Thiopyranon‐2‐carbonsäureester 2 führt diastereoselektiv zu den Diolen 5. Die alkalische Hydrolyse von 2d liefert das Disulfid 8.
Eine neue Synthese von 8‐donatorsubstituierten 5‐Thia‐ und 5‐Deaza‐riboflavin‐Derivaten
Authors: Fenner Helmut , Hochhuth Dieter 
Published: October 2006

AbstractDurch gezielte Verwendung von Schutzgruppen konnte die Synthesemöglichkeit für 5‐Thia‐ und 5‐Deaza‐riboflavine auch auf die 8‐Elektronendonator‐substituierten Derivate 2 und 3 ausgedehnt werden. Die Polyole 4 werden transketalisiert und anschließend mit 2,4,6‐Trichlorpyrimidin zu 8 und 9 umgesetzt Einführung der Benzyloxy‐Gruppe und Hydrierung gibt als zentrale Vorstufen die Uracile 11. Deren Cyclisierung erfolgte in bekannter Weise. Abspaltung der O‐Schutzgruppen gibt die Zielverbindungen 2 und 3. Die Methode mit 3–7% Gesamtausbeute (bezogen auf D‐Ribose) kann auch Synthesemöglichkeiten für komplexere Flavine eröffnen, da sich die Uracile 11 auch zu “normalen” Flavinen cyclisieren lassen.
Glutaraldehydrückstände in Herzklappentransplantaten
Authors: Spreitzer Helmut , Jäger Walter , Grimm Michael , Eybl Elisabeth , Müller Matthias 
Published: October 2006

AbstractHerzklappentransplantate aus Kälberperikard erleiden im Laufe der Zeit Schäden durch Mineralisation. Diese Schäden und mögliche toxische Nebenwirkungen können eventuell auf Glutaraldehydrückstände, die aus der notwendigen Vorbehandlung stammen, verursacht werden. Unterschiedliche Waschmethoden, die vor der Transplantation durchgeführt werden, wurden hinsichtlich ihrer Fähigkeit, Glutaraldehyd zu entfernen, untersucht.
2‐Amino‐2‐oxazolines, III: Synthesis, Structure, and Preliminary Pharmacological Evaluation of Cycloaddition Compounds with Unsaturated Carboxylic Esters
Authors: Forfar Isabelle , Jarry Christian , Leger Jean‐Michel , Carpy Alain 
Published: October 2006

AbstractThe reaction of 5‐substituted 2‐amino‐2‐oxazolines with unsaturated carboxylic esters yielded 2,3,5,6‐tetrahydro‐ and 2,3‐dihydro‐7H‐oxazolo[3,2‐a]pyrimidin‐7‐ones. The structure of these compounds was established by IR‐ and NMR‐spectra and by X‐ray crystallography. They were tested for anti‐arrhythmic and hypocholesterolemic activities.
Potentiell ZNS‐wirksame, tricyclische Verbindungen mit verbrücktem Mittelring, 4. Mitt.: Synthese und Konfiguration von partiell hydrierten 9,10‐Epithioanthracen‐S‐oxiden
Authors: Linde Hermann F. G. , Krämer Norbert H. 
Published: October 2006

AbstractEs wird über Arbeiten zur Darstellung von 9,10‐Epithioanthracensulfoxiden berichtet. Als Oxidationsmittel wurden Natriummetaperiodat, Wasserstoffperoxid/Essigsäure und Oxone® verwendet. Für die endo‐Verbindungen wurde mittels Einsatz von Eu(FOD)3 die thermodynamisch stabilere anti‐Konfiguration ermittelt. Eine Isomerisierung von 8‐anti in 8‐syn gelingt mit Hilfe von Trimethyloxoniumtetrafluoroborat, ist aber bereits bei 0°C vollständig reversibel. Die Konfigurationen in der exo‐Reihe wurden durch 1H‐NMR‐Spektroskopie aus denen der endo‐Verbindungen abgeleitet.
Syntheses of Metabolites of S‐Carboxymethyl‐L‐cysteine and S‐Methyl‐L‐cysteine and of Some Isotopically Labelled (2H, 13C) Analogues
Authors: Meese Claus O. , Specht Dagmar , Hofmann Ute 
Published: October 2006

AbstractThe chemical syntheses of human metabolites of S‐carboxymethyl‐L‐cysteine (3) and S‐methyl‐L‐cysteine (12) are described. The additional preparation of some 2H‐ and 13C‐labelled isotopomers enabled the direct evaluation of the stabilities of 3 and 12 under physiological conditions and also facilitated the unambiguous assignments of the signals in the 13C‐NMR spectra of all compounds mentioned.
Asymmetrische elektrophile α‐Amidoalkylierung, 8. Mitt.: Gewinnung optisch aktiver α‐Phenacylpyrrolidinamide und erste asymmetrische Totalsynthese des Norruspolins
Authors: Wanner Klaus T H. , Höfner Georg 
Published: October 2006

AbstractDurch Reaktion des chiralen nicht‐racemischen α‐Methoxyamids 1 mit den Silylenolethern 2a‐d werden stereoselektiv die α‐Phenacylpyrrolidinamide (R)‐4/(S)‐5a‐e synthetisiert. Die geminalen Bisamide (R)‐12/(S)‐13 werden durch Umsetzung von 1 mit dem Bistrimethylsilylimidat 11 erhalten. (R)‐4d wird für die Gewinnung des optisch aktiven Norruspolins (R)‐16 (ee ≧ 84%) eingesetzt.
Einfluß des Vasokonstriktors Glycylpressin auf die Verfügbarkeit von Mitomycin C
Authors: Czejka Martin , Jäger Walter , Schüller Johann 
Published: October 2006

AbstractIm Rahmen einer intra‐arteriellen Chemotherapie von Patienten mit Lebermetastasen wurden die Blutspiegelverläufe von Mitomycin C (1) nach Verschluß der Arteria hepatica communis durch den Vasokonstriktor Glycylpressin (2) ermittelt. Der Gefäßverschluß mit 2 führt bei gleicher Dosierung im Gegensatz zu einer Bolusgabe von 1 ohne 2 zu signifikant (p < 0.01) erniedrigten Blutspiegelwerten. Durch diese Verringerung der systematischen Verfügbarkeit um rund 50% wird die Verfügbarkeit im Tumorbereich entsprechend gesteigert.
In vitro Testing of Triamterene Derivatives for Antiarrhythmic Activity
Authors: Busch Andreas E. , Ullrich Frank , Mutschler Ernst 
Published: October 2006

AbstractA series of para‐substituted triamterene derivatives (Table 1) were evaluated for their antiarrhythmic properties in vitro. Pharmacological evaluation of the compounds and some class‐I‐ (quinidine, lidocaine, and propafenone) as well as class‐III‐antiarrhythmic drugs (±)‐sotalol and amiodarone was carried out by measuring the functional refractory period (FRP), the maximal driving frequency (MDF) and the force of myocardial contractions (FC) of electrically stimulated guinea pig atria. The increase in FRP and the decrease in MDF was most pronounced with the class‐I‐antiarrhythmic drugs, but these compounds showed the typical negative inotropic effects, too. For the class‐III‐antiarrhythmics only a weak influence on FRP and MDF could be demonstrated, while FC was not altered in the presence of (±)‐sotalol and amiodarone. Neutral substituted triamterenes like compounds 2—5 as well as most of the benzyltriamterene derivatives showed similar or stronger effects on FRP and MDF as (±)‐sotalol and amiodarone. With the exception of 4 and 5, these effects were combined with an increase of FC. Compounds 6 and 7, well known potent diuretics, showed no influence to FRP, MDF and FC. Therefore, we conclude different mechanisms for the antikaliuretic and cardiac activity.
Zur Reaktion von Nifedipin mit Pyridiniumbromidperbromid
Authors: Görlitzer Klaus , Bartke Ulrich , Schmidt Eckhardt 
Published: October 2006

AbstractNach derYoung‐Methode wird aus Nifedipin das 1,4‐Dihydropyridin‐bislacton4hergestellt. Als Nebenprodukt dieser Reaktion werden die Pyridiniumverbindung3sowie die bromierten 1,4‐Dihydropyridinlactone5und6isoliert.4wird durch Redox‐ und photochemische Reaktionen charakterisiert. Die Halbstufenpotentiale der Dihydropyridin‐ und Pyridin‐Verbindungen werden bestimmt.
Synthesis and Calcium Antagonistic Activity of Some New 2‐Thioxo‐1,2,3,4‐tetrahydropyrimidine Derivatives
Authors: Ertan Mevlüt , Balkan Ayla , Saraç Selma , Uma Serdar , Renaud Jean Francois , Rollad Yves 
Published: October 2006

AbstractA series of 1,2,3,4‐tetrahydro‐6‐methyl‐4‐(substituted phenyl)‐2‐thioxo‐5‐pyrimidinecarboxylic acid methyl esters were synthesized by condensing thiourea with methyl acetoacetate and nonsubstituted or differently substituted benzaldehydes in absol. ethanol using HCl as a catalyst according to the Biginelli reaction. The structures of the compounds were confirmed by elemental and spectroscopic analysis. ‐ The compounds were evaluated for their calcium antagonistic activity on the basis of their potency in inhibiting [3H] PN 200—110 binding on microsomes obtained from rat skeletal muscle.
N‐[4‐(3H‐1,3,4‐Oxadiazoline‐2‐thion‐5‐yl)phenyl]‐N′‐substituted Thioureas: Synthesis and Antimicrobiological Activities
Authors: Rollas Sevim , Büyüktimkin Servet , Çevikbas Adile 
Published: October 2006

AbstractDiverse pharmacological properties are associated with 3H‐1,3,4‐oxadiazoline‐2‐thione derivatives. These include anticonvulsant1—4) and fungicidal5) properties. On the other hand thiourea derivatives possess antiphytoviral6), virucidal7), growth inhibitory8—10), and herbicide11) activities. All these data prompted us to combine these moieties into a single molecule. The compounds synthesized were tested for their antimicrobial activities against seven microorganisms.
Properties and Reactions of Substituted 1,2‐Thiazetidine 1,1‐Dioxides: Fluoride Catalyzed Reactions of Silylated β‐Sultams with Electrophiles
Authors: Müller Martin , Otto Hans‐Hartwig 
Published: October 2006

AbstractN‐Silylated β‐sultams 1 and 4 react with ketones and aldehydes in the presence of fluoride ions to O‐silylated carbinolsulfonamides 3. Under similar conditions, N‐aminoalkylated 4‐silylated β‐sultams react to O‐silylated C‐4 aldol adducts 7, which are deprotected and desilylated to 8 and 10. The (α‐hydroxy‐α‐methylethyl)‐substituted β‐sultam 16 is prepared from 14 via 15. Reactions of 5b and 14 with aromatic aldehydes yield the Peterson olefination products 11, 12, and 19. E‐ and Z‐isomers of these compounds are separated by CC.
Synthesis of New Benzimidazole Derivatives as Potential Antimicrobial Agents
Authors: Badawey El‐Sayed A. M. , Hassan Ahmed M. M. , Kappe Thomas 
Published: October 2006

AbstractBarbiturates 3 as possible antimicrobial agents were obtained by reacting the N,N′‐disubstituted urea 1a or the thiourea analogues 1b,c with the magic malonates 2a,b. On the other hand, reaction of 1a with ethoxycarbonyl isocyanate (4) yielded the substituted s‐triazine‐2,4,6(1H,3H,5H)‐trione 5. The reaction of 4 with 2‐aminomethyl‐benzimidazole (6) gave the allophanate 7 which upon treatment with Na2CO3 yielded N‐(1H‐benzimidazol‐2‐yl)urea 8.
Rapid Assay for the Quantification of Piretanide in Biological Fluids
Authors: Spahn‐Langguth Hildegard , Hahn Gabriele , Mutschler Ernst 
Published: October 2006

AbstractPiretanide was determined from plasma and urine using reversed‐phase high‐performance liquid chromatography. Plasma was extracted with diethylether at pH 4 using bumetanide as internal standard. The chromatographic separation was performed on an octadecylsilane column (ODS) with acetonitrile/pH 7 phosphate buffer (3:7, v/v). In order to determine piretanide in urine, bumetanide was added to a urine aliquot. Then the sample was centrifuged and the supernatant directly injected without extraction followed by chromatography on an ODS column with a mixture of methanol and pH 7 phosphate buffer (12:13, v/v). The compounds were detected by their intrinsic fluorescence, monitoring the eluate at 287/450 nm. Total chromatography times were 8 min for plasma and 13 min for urine samples. The method was applied for the assay of piretanide in plasma of healthy volunteers after i.v. or p.o. dosage of 6 mg piretanide.
Synthesis and Binding Properties to GABA Receptors of 3‐Hydroxypyridinyl‐ and 3‐Hydroxypiperidinyl‐Analogues of Baclofen
Authors: Desideri Nicoletta , Galli Alessandro , Sestili Isabella , Stein Maria Luisa 
Published: October 2006

AbstractThe synthesis of 3‐(3‐hydroxy‐2‐pyridinyl)propanoic acid, 3‐(3‐hydroxy‐2‐pyridinyl)‐4‐aminobutanoic acid, their corresponding piperidine compounds, and of some cyclized derivatives is described.In in vitro assays none of the new compounds shows any noteworthy affinity for GABAA or GABAB receptors; only (R,S)‐3‐(3‐hydroxy‐2‐pyridinyl)‐4‐aminobutanoic acid and its lactam inhibited in some degree [3H]GABA binding, at 10−4 M concentration, with low specificity as regards the two receptors.
Analysis of Drugs by Polarography, XXXV: The Polarographic Behaviour of Cinolazepam. [1‐(2‐Cyanoethyl)‐7‐chloro‐3‐hydroxy‐5‐(2‐fluorophenyl)‐1,3‐dihydro‐2H‐1,4‐benzodiazepin‐2‐one] and Assay of its Tablets
Authors: Oelschläger H. , Volke J. , Belal F. 
Published: October 2006

AbstractCinolazepam is reduced at the Dropping Mercury Electrode (DME) over the entire pH range in Britton Robinson buffers (BRB) containing 20% DMF as a solubilizer. A well‐defined cathodic wave is obtained over the pH range 3‐5, which is very suitable for analytical purposes. The wave was characterized as being irreversible, diffusion‐controlled and free from adsorption phenomena. In acid buffers, 4 electrons are consumed in the reduction process, while in alkaline buffers the electrode reaction is somewhat complicated. Tablets containing 40 mg cinolazepam were analysed using the polarographic and a developed HPLC method. The results obtained with both methods are in good accordance as revealed by statistical analysis. The details of the complicated mechanism of the reduction process at the DME are still under investigation but elucidated in principle.
Synthesis, Decarboxylation, and Nitrosation of 1‐Acyl‐2‐pyrrolidone‐3‐carboxylic Acids: A Convenient Novel Entry to 2,3‐Dioxopyrrolidine Derivatives
Authors: Gailius Viktoras , Stamm Helmut 
Published: October 2006

AbstractEsters 1 of 1‐acyl‐2‐pyrrolidone‐3‐carboxylic acids 2 were hydrolized to 2 with acetic acid/HCl at 60–70°C. Reaction of 1a with formic acid/HCl at 60–75°C led to (not isolated) 2a which began to decarboxylate to 3a during the conversion of 1a to 2a even at this low temp. Decarboxylation of 2c‐f was accomplished at 160°C without solvent. Decarboxylative nitrosation of 2c‐f yielded the oximes 4c‐f of 1‐acyl‐2,3‐dioxopyrrolidines. Treatment of 4f with magic methyl provided the enol ether 5f of the respective dioxopyrrolidine.
Pyridazines, LVII: Synthesis and Cyclocondensation Reactions of (2‐Aminophenyl)‐(4‐pyridazinyl)‐ketone, a New Diaza Isoster of 2‐Aminobenzophenone
Authors: Haider Norbert , Heinisch Gottfried , Moshuber Jöran 
Published: October 2006

AbstractA convenient approach to the new 2‐aminobenzophenone analogue 4 is reported. Condensation reactions of 4 with ortho esters or amide acetals, respectively, followed by intramolecular cyclisations were found to provide smooth access to (4‐pyridazinyl)‐substituted quinolines 10, 13a,b, and the quinazoline derivative 15.
Researches on Antibacterial and Antifungal Agents, XIV: Thiophene Analogues of Bifonazole
Authors: Stefancich Giorgio , Silvestri Romano , Retico Augusta , Artico Marco , Simonetti Giovanna 
Published: October 2006

AbstractSome thiophene analogues of bifonazole have been synthesized by standard procedures and their antifungal activity has been tested against Candida albicans. Among test derivatives biphenyl‐4‐yl‐5‐chloro‐thien‐2‐ylimidazol‐1‐ylmethane and its 5‐deschlorothien‐2‐yl analogue resulted to be the most active. Their antifungal potency was almost comparable to that of control substances, such as miconazole, ketoconazole, and bifonazole. Replacement of benzene by the pyrrole ring in the biphenyl portion retained almost quantitatively the antifungal activity, whereas substitution with other azoles and with nitrogen alicyclic rings led always to less potent derivatives.
Kurzmitteilungen: Passiflora and Lime‐blossoms: Motility Effects after Inhalation of the Essential Oils and of Some of the Main Constituents in Animal Experiment.
Authors: Buchbauer G. , Jirovetz L. , Jäger W. 
Published: October 2006

AbstractPassionsblume und Lindenblüten: Motorik bei Tieren nach Inhalation der ätherischen Öle und einiger Hauptbestandteile
Relationship of Hypolipidemic and Antineoplastic Activities of Tricyclohexyl‐ and Triphenylphosphine Boranes, Carboxyboranes, Cyanoboranes, and Related Derivatives
Authors: Das Mrinal K. , Maiti Pradip K. , Roy Sarbari , Mittakanti Malaiah , Morse Karen W. , Hall Iris H. 
Published: October 2006

AbstractA series of tricyclohexyl‐ and triphenylphosphine boranes, carboxyboranes and cyanoboranes were synthesized. These compounds have potent hypolipidemic effects, antineoplastic and antiinflammatory activities in rodents. Furthermore, they demonstrated potent cyctotoxicity against standard human tissue culture lines. The compounds which afforded the best hypolipidemic activity, i.e. greater than 40% reduction of serum cholesterol and triglyceride levels, were diphenyl‐(4‐methylphenyl)‐phosphine borane and triphenylphosphine carboxyborane. Other derivatives demonstrated more potent antineoplastic activity against the Ehrlich ascites carcinoma growth including triphenylphosphine cyanoborane, 2‐amino‐4‐methyl‐pyridine cyanoborane and 2‐amino‐pyridine cyanoborane. Most of the derivatives showed good activity against murine L1210 lymphoid leukemia, Tmolt3 human leukemia, uterine HeLaS cells, and human glioma cell growth. Select compounds were active against colon adenocarcinoma, KB nasopharynx, lung bronchogenic and osteosarcoma cell growth. Tricyclohexyl‐ and triphenylphosphine boranes and the carboxy derivatives of the latter borane demonstrated good antiinflammatory activity.
An Efficient Synthesis of Buspirone and its Analogues.
Authors: Cybulski Jacek , Chilmonczyk Zdzislaw , Szelejewski Wieslaw , Wojtasiewicz Krystyna , Wróbel Jerzy T. 
Published: October 2006

AbstractEine leistungsfähige Synthese von Buspiron und Buspiron‐ähnlichen Verbindungen
Zur bromometrischen Bestimmung von Vinylbital
Authors: Görlitzer Klaus , Boventer Kristin 
Published: October 2006

AbstractVinylbital (1) reagiert mit Br−/BrO3− in Eisessig/HCl unter Addition von BrCl zu 2. Der Ersatz von HCl durch HBr führt zur Dibrom‐Verbindung 4, die unter O‐Alkylierung zum Furo[2, 3‐d]pyrimidin 5 cyclisiert.
Untersuchungen an Lokalanästhetika, 99. Mitt.: Synthese und lokalanästhetische Wirkung von Alkoxyphenylcarbamaten
Authors: Búciová Lubiča , Csöllei Jozef , Račanská Eva , Švec Pavel 
Published: October 2006

AbstractZum Studium des Einflusses von Veränderungen der Verbindungskette in einer Gruppe von Lokalanästhetika wurde eine Serie von 24 Verbindungen aus der Gruppe der 1‐Propoxymethyl‐2‐(1‐pyrrolidinyl)‐, 2‐(1‐Piperidino)‐und 2‐(1‐Perhydroazepinyl)‐ethylester der o‐ und m‐Alkoxyphenylcarbamidsäure hergestellt. Die untersuchten Verbindungen wiesen bei verhältnismäßig geringer akuter Toxizität hohe relative anästhetische Aktivität im Vergleich mit den Standardverbindungen Cocain und Procain auf.
Synthesis and Antimicrobial Activity of 3‐(Substituted‐phenyl)‐sydnones
Authors: Moustafa M. A. A. , Eisa H. M. 
Published: October 2006

Abstract3‐(3 or 4‐Acetylphenyl)‐sydnones 7, 8 have been synthesized by formation of the glycines 3, 4, followed by nitrosation to 5, 6 and cyclization with acetic anhydride to sydnones. Sydnone derivatives carrying chalcone moieties 15, 16 were prepared by formation of the chalcone analogues 11, 12 through condensation of the glycines 3, 4 with the appropriate aldehydes, followed by the reactions applied for the preparation of 7, 8. The sydnone derivatives were screened for antimicrobial activities.
Amino Acids, XII: (±)Pipecolic Acid Derivatives ‐ Part 2: An Expedient Synthetic Entry to Substituted Pipecolic Acids
Authors: Herdeis Claus , Engel Wolfram 
Published: October 2006

AbstractThe Diels‐Alder product 1 is transformed by Noyori reaction and catalytic hydrogenation to 4. Hydrolysis with concomitant decarboxylation of 4 furnishes the trans configuration amino acid 5. Functional group transformation (reduction, lactonization) of 5 provides 7, ring opening affords the pipecolic acid derivative 9. On the other hand 1 is hydrolyzed to 10 and 4‐oxo‐pipecolic acid 11. Reduction of 10 and subsequent hydrolysis with decarboxylation of 12 affords the amino acid 13a/13b in a cis/trans ratio of 1:1. Contrary to this result, reduction of 11 provides 13a/13b in a ratio of ≧ 95/5.
Synthesis of Pyranoid Analogues of the Anti‐HIV Active 3′‐Deoxy‐2′,3′‐didehydrothymidine (D4T)
Authors: Hansen H. Bue , Pedersen Erik B. , Vestergaard Bent Faber 
Published: October 2006

AbstractThe primary hydroxy group of ethyl 2,3‐dideoxy‐α‐D‐erythro‐hex‐2‐enopyranoside (1) was selectively protected and the secondary hydroxy group was deoxygenated via the dithiocarbonate 3 from which ethyl 6‐O‐(4‐methoxybenzoyl)‐2,3,4‐trideoxy‐α‐D‐trideoxy‐α‐2‐enopyranoside (4) and its regioisomer (5) were produced. These were converted into didehydro nucleosides by glycosylation of silylated heterocyclic bases in the presence of trimethylsilyl trifluoromethanesulfonate as catalyst. The configurations of the anomeric products were assigned by 1H‐NMR analysis of the corresponding saturated compounds which were obtained by hydrogenation of the double bond in the carbohydrate moiety. The compounds 9a,b,d, 10a, b, 14a,b,e,f, and 15a,b,e,f did not show any significant activity against HIV or HSV‐1.