bluuebunny/crossref_metadata_2025_split huggingface dataset:
Ringverengung von 1,4‐Benzodiazepinen zu 3,4‐Dihydrochinazolinen bei präparativer Elektrolyse (Beispiel 5: Cyprazepam
Authors: Oelschläger Herbert , Martienssen Doris , Belal F. 
Published: October 2006

AbstractCyprazepam (1) wird in 3 Stufen unter Verbrauch von insgesamt 6 θ an der DME und auch im präparativen Maßstab an einer gerührten Hg‐Kathode reduziert. Dabei tritt unter Eliminierung von Cyclopropylmethylamin Ringverengung zum 6‐Chlor‐2‐methyl‐4‐phenyl‐3,4‐dihydrochinazolin ein. Dies ist das fünfte Beispiel einer zuerst von uns beobachteten reduktiven Ringverengung, die nur an einer Hg‐Elektrode, nicht aber bei der katalytischen Hydrierung eintritt.
Aminopeptidase Inhibitory Properties and Analgesic Activity of (2S,3,7‐3,7‐Diamino‐2‐hydroxy‐heptanoic Acid Containing Tripeptide Analogues of the N‐Terminal Tripeptide of Probestin
Authors: Herranz Rosario , Vinuesa Soledad , Pérez Concepción , García‐López M. Teresa , De Ceballos María L. , Murillo Francisco M. , Del Río Joaquín 
Published: October 2006

Abstract(2S,3R)‐3,7‐Diamino‐2‐hydroxy‐heptanoyl‐Leu‐Pro‐OH [(2S,3R)‐DAHHA‐Leu‐Pro‐OH, 4], analogue of the N‐terminal tripeptide of probestin, has been synthesized, and tested as inhibitor of AP‐B, Leu‐AP, AP‐M, and enkephalin‐degrading APs, and as analgesic. In order to establish structure‐activity relationships the dipeptide (2S,3R)‐DAHHA‐Pro‐OH (5) and the tripeptide (2S, 3R)‐DAHHA‐Ala‐Pro‐OH (6) were also prepared. Compounds 4 and 6 were potent and selective inhibitors of enkephalin‐degrading APs and showed a prolonged antinociceptive effect.
2‐Amino‐2‐oxazolines, VI: Study of the Tautomerism by Experimental and Theoretical Methods
Authors: Forfar Isabelle , Jarry Christian , Fayet Jean‐Pierre , Carpy Alain 
Published: October 2006

AbstractThe tautomeric equilibrium of 2‐amino‐2‐oxazolines with a C‐5 lateral amino chain has been studied by dipole moments measurement and theoretical calculations (MNDO and ab initio). The results show the predominance of the amino tautomers in solution. The X‐ray crystal structure of 5‐morpholinomethyl‐2‐amino‐2‐oxazoline confirms this tendency in the solid state.
Biotransformation of the Sympathomimetic Tetraminol in vitro
Authors: Drandarov Konstantin , Kvasničková Eva , Hais I. M. 
Published: October 2006

AbstractOn incubation with the postmitochondrial fraction of the liver homogenate of rabbits, guinea‐pigs, rats, and mice in the presence of NADPH and oxygen, the α‐sympathomimetic trans‐3‐(2‐hydroxyethylamino)‐5,8‐dimethoxy‐1,2,3,4‐tetrahydro‐2‐naphthol (Tetraminol, 1) is preferentially O‐demethylated in position 8, yielding metabolite 3. In male rats O‐demethylation is stronger than in females.
Synthesis of Biologically Active [2.2]Paracyclophanes
Authors: Aly Ashraf A. , Hassan Alaa A. , Mourad Aboul‐Fetouh E. , Hopf Henning 
Published: October 2006

AbstractClaisen reaction of 4‐acetyl[2.2]paracyclophane (1) with ethyl acetate and diethyl oxalate affords 4‐acetoacetyl[2.2]paracyclophane (2) and ethyl(4‐oxaloacetyl[2.2]paracyclophane) (6), respectively. Reaction of 2 and 6 with hydrazines and CuCl2 gave the pyrazole derivatives 4 and 8 in addition to the metal complexes 5 and 9. Mannich reaction of 2 with benzylamine and paraformaldehyde yielded the piperidinone derivative 3. The biological activity of all new compounds was tested.
Heterocyclische Spirocyclohexadienone, 1. Mitteilung
Authors: Möhrle Hans , Schake Dieter , Bluhme‐Hensen Karin 
Published: October 2006

AbstractDie als Methylenamin 3 beschriebene Verbindung wird als heterocyclisches Spirocyclohexadienon 9 erkannt, wobei die katalytische Hydrierung entgegen den Literaturangaben nicht zum Methylaminderivat 4, sondern zum Spiroketon 10 und einem Gemisch diastereomerer, spirocyclischer Alkohole 11a/11b führt. Die Reaktivität von 9 gegenüber Protonensäuren und Carbonylreagentien wird untersucht.
Untersuchungen zur Benzylierung von Tetrahydroisochinolinen mit Benzaldehyd bzw. substituierten Benzaldehyden (Rügheimer‐Burrows‐Reaktion)
Authors: Dannhardt Gerd , Roelcke Julius 
Published: October 2006

AbstractDie unter Aromatisierung verlaufende Benzylierung von Piperidin‐ bzw. Tetrahydroisochinolin‐Derivaten mit Benzaldehyden (Rügheimer‐Burrows‐Reaktion) ist eine vielstufige Reaktion, für die verschiedene Mechanismen diskutiert werden. Durch die Isolierung und Charakterisierung der nachfolgend beschriebenen Intermediate bzw. Nebenprodukte werden Teilschritte der Gesamtsequenz plausibel erklärbar.
Zur Pharmakokinetik von Lipidsenkern, 9.Mitt.: Zur Frage der biliären Ausscheidung des Lipidsenkers Ciprofibrat (1) (2‐[4‐(2,2‐Dichlorcyclopropyl)‐phenoxy]‐2‐methylpropionsäure)
Authors: Oelschläger Herbert , Rothley Dietrich , Schröder Dieter , Scherm Sabine 
Published: October 2006

AbstractNach oraler Gabe von 200 mg Ciprofibrat (1) an 10 cholezystektomierte Patienten, denen ein T‐Drain in den Ductus choledochus eingelegt worden war, findet sich 1 in der im 12 h‐Rhythmus gesammelten Galle nur als 1‐ O‐β‐Acylglukuronid in sehr geringer Menge. Approximative Berechnungen ergaben, daß nach Einzeldosis in 2 Tagen weniger als 0.5% der verabfolgten Dosis biliär exkretiert wurden. Ob bei Langzeittherapie die biliäre Ausscheidung zunimmt, ist noch eine offene Frage.
Oxazepines and Thiazepines, XXV: Chemical Transformations of 2,3‐Dihydro‐1,5‐benzothiazepin‐4(5H)‐ones
Authors: Lévai Albert 
Published: October 2006

Abstract2,3‐Dihydro‐1,5‐benzothiazepine‐4(5H)‐thiones 13‐22 were prepared by the reaction of the appropriate 2,3‐dihydro‐1,5‐benzothiazepin‐4(5H)‐ones with Lawesson's reagent. N‐Acyl (23‐25) and N‐alkyl (26‐28) derivatives have also been synthesized. Oxidation with 3‐chloroperoxybenzoic acid afforded sulfoxides 29‐32, and sulfones 33‐40 were obtained by using H2O2 as an oxidizing agent.
Synthesen von 13C‐ und 14C‐markiertem trans‐2‐Amino‐2‐methyl‐N‐(4‐nitroxycyclohexyl)‐propionsäureamid (BM 12.1179)
Authors: Neidlein Richard , Strein Klaus , Preßmar Friedburg , Kramer Walter , Michel Helmut 
Published: October 2006

AbstractVon dem gefäßwirksamen Salpetersäureester trans‐2‐Amino‐2‐methyl‐N‐(4‐nitroxycyclohexyl)‐propionsäureamid (BM 12.1179) (1) sind, ausgehend von der sterisch gehinderten α‐Aminoisobuttersäure (2), die 13C‐ und 14C‐markierten Verbindungen synthetisiert worden. Verschiedene Amino‐Schutzgruppen sowie Methoden zur Aktivierung der Carboxylfunktion werden verglichen.
Preparation and Diuretic Properties of Novel Amiloride Analogues
Authors: Russ Thomas , Ried Walter , Ullrich Frank , Mutschler Ernst 
Published: October 2006

AbstractFifteen novel amiloride analogues were synthesized and their diuretic properties compared to amiloride and triamterene in white wistar rats. Whereas none of the 6‐substituted derivatives exhibited significant natriuretic and antikaliuretic effects, five of the compounds modified in the 2‐position were found equal or better than standards. The results are discussed with respect to chemical structure and physicochemical properties.
Synthesis of Some Guanylhydrazones and Imidazolinylhydrazones as Thromboxane‐Synthase and Platelet Aggregation Inhibitors
Authors: Desideri N. , Sestili I. , Piccardoni P. , Rotondo S. , Cerletti C. , Stein M. L. 
Published: October 2006

AbstractThe imidazolinylhydrazones of (3‐pyridinyloxy)‐acetaldehyde and of 6‐[3‐(2‐formyl‐pyridinyl)oxy]hexanoic acid were synthesized as cyclic analogues of the corresponding guanylhydrazones which were found to be selective inhibitors of human thromboxane‐synthase. The benzene isosters were also prepared in order to define the importance of the ring nitrogen for the activity.‐ Moreover, the guanyl‐ and imidazolinyl‐hydrazones of two 6‐[(3‐pyridinyl)oxy]hexanoic acids showing in the 2 position an alkyl chain with an α,β‐unsaturated ketonic function were prepared.‐ Imidazolinylhydrazones 7 and 18 are selective inhibitors of thromboxane‐synthase, while the two guanylhydrazones 14 and 15 which do not affect prostanoid biosynthesis seemed to be antagonists at the thromboxane receptor.
Hypolipidemic Effects of 2‐Furoic Acid in Sprague‐Dawley Rats
Authors: Hall Iris H. , Wong Oi T. , Reynolds David J. , Chang J. J. 
Published: October 2006

Abstract2‐Furoic acid was shown to be effective in lowering both serum cholesterol and serum triglyceride levels significantly in rats with an elevation of HDL cholesterol level at 20 mg/kg/day orally. LDL receptor activity was reduced in hepatocytes, aorta foam cells, small intestinal epithelium cells and fibroblasts. HDL receptor activity was elevated in the rat hepatocytes and small intestinal cells. These activities were correlated with inhibition of acyl CoA cholesterol acyl transferase activity. Neutral cholesterol ester hydrolase activity was elevated in rat hepatocytes and human fibroblasts. Thus, 2‐furoic acid appears to interfere directly with activity of intracellular enzymes rather than affecting high affinity‐mediated lipoprotein membrane receptors. In vivo treatment with 2‐furoic acid led to reduction in the liver and small intestine ATP dependent citrate lyase, acetyl CoA synthetase, acyl CoA cholesterol acyl transferase, sn‐glycerol 3‐phosphate acyl transferase, phosphatidylate phosphohydrolase and heparin induced lipoprotein lipase activities.2‐Furoic acid reduced biliary cholesterol levels but the agent increased bile salts which are lithogenic. Acute toxicity studies in mice suggest that the agent has some hepatic toxicity effects. The LD50 was relatively low at 250 mg/kg IP in mice.
Microsomal N‐Oxygenation of Adenine to Adenine 1‐N‐Oxide
Authors: Clement Bernd , Kunze Thomas 
Published: October 2006

AbstractDuring investigations on the N‐oxygenation of adenine (1) the enzymatic formation of adenine 1‐N‐oxide 3 was demonstrated for the first time. The identity of this metabolite was confirmed by its chromatographic behaviour and UV‐spectrum recorded after HPLC separation. Adenine 1‐N‐oxide (3) and similar oxygenated derivatives of adenine were synthesized as reference substances. The enzymatic formation of 3 exhibits the typical characteristics of a reaction catalysed by microsomal mono‐oxygenases. In induction experiments, an increase in the rate of formation of 3 after pretreatment with phenobarbital was observed. A participation of those isoenzymes of the cytochrome P‐450 enzyme system which can be induced by phenobarbital is assumed.
Lactone, 23. Mitt.: Synthese und Stereochemie „γ‐lactonisierter”︁ Neuroleptika vom Butyrophenon‐Typ
Authors: Lehmann Jochen , Radwansky Anja 
Published: October 2006

Abstract„γ‐Lactonisierte”︁ Neuroleptika (1,2a‐c) können aus den α‐Formyl‐, α‐Carboxy‐ und α‐Methylenlactonen 5‐7a,b durch Umsetzen mit den Aminen 8a‐c erhalten werden. 6a und 1a‐c fielen als cis/trans‐Gemische mit über‐wiegender cis‐Form, 6b und 2a als cis/trans‐Gemische mit überwiegender trans‐Form an. Bei 2b,c wurden reine trans‐Isomere isoliert.
Stereoselektive Synthese neuer zentral wirksamer Tricyclen vom Benzomorphan‐Typ mit 2‐Phenylethylamin Partialstruktur
Authors: Wünsch Bernhard , Höfner Georg , Bauschke Gerd 
Published: October 2006

AbstractDie Addition des mit LDA deprotonierten Glycinesters 6 an das Homophthalaldehydmonoacetal 5 liefert den β‐Hydroxyester 7, der sich nach Reduktion zu den racemischen 2,6‐Epoxy‐3‐benzoxocin‐5‐aminen (+/−)‐12 und (+/−)‐13 cyclisieren läß. Die Schlüsselverbindungen für die Gewinnung von 12 und 13 in enantiomerenreiner Form sind die Hydroxyacetale (R,S,R)‐22 und (R,S,S)‐23: (R,S,R)‐22 läßt sich stereoselektiv durch Addition der Aryllithiumverbindung 21b bzw. der Aryltitanverbindung 21c an das neue Serinal‐Äquivalent (R,S)‐20 gewinnen; die Reduktion des Ketons (R,S)‐24 mit LiAlH4 bei −78°C führt überwiegend (>95%) zu dem diastereomeren Hydroxyacetal (R,S,S)‐23. Mit Säure werden (R,S,R)‐22 und (R,S,S)‐23 in die tricyclischen Urethane (S,S,R)‐25 und (R,S,S)‐30 überführt, die sich zu den Dimethylaminen (S,S,R)‐12 und (R,S,S)‐13 reduzieren und methylieren lassen (ee > 97%). Analog werden die enantiomeren Amine (R,R,S)‐12 und (S,R,R)‐13 ausgehend von (R)‐Serin dargestellt. Die relative Konfiguration von (R,S,R)‐22 wird mit Hilfe von Molecular Dynamics Rechnungen (Sybyl 5.4) in Kombination mit NOE‐Messungen bewiesen.‐ Nach Applikation beider Enantiomere von 12, 13, 27 und 32 lassen sich bei Mäusen typische Symptome für eine zentrale Dämpfung beobachten. Im Essigsäure Writhing‐Test sind (S,S,R)‐12, (S,R,R)‐13, (R,S,S)‐13, (S,S,R)‐27, (R,R,S)‐27 und (R,S,S)‐32 stark analgetisch wirksam mit ED50 Werten in der Größenordnung des ED50‐Wertes von Tramadol‐HCl.
2,6‐Epoxy‐3‐benzazocine: Zentral wirksame N/O‐Acetale durch Ringschluß von Amino‐ und Amidoacetalen
Authors: Wünsch Bernhard , Höfner Georg , Bauschke Gerd 
Published: October 2006

AbstractUnter sauren Bedingungen cyclisierten die sekundären Amine 10a und 10b, das primäre Amin 15, das Amid 17a und das Urethan 17b zu den 2,6‐Epoxy‐3‐benzazocinen 11a, 11b, 16, 18a und 18b. Der Ringschluß des inversen Amids 5a zum tricyclischen N/O‐acetal 6 gelang jedoch nicht. Mit LiAlH4 ließ sich die Epoxybrücke des Urethans 18b zum bicyclischen 3‐Benzazocin 20 öffnen. ‐ Während das N‐(2‐Methoxyethyl)‐Derivat 11b das Verhalten der Mäuse nicht beeinflußte, zeigte das N‐Methyl‐Derivat 11a starke ZNS‐Wirkung.
Nonsteriodal Antiinflammatory Agents, XVII: Inhibition of Bovine Cyclooxygenase and 5‐Lipoxygenase by N‐Alkyldiphenyl‐pyrrolyl Acetic and Propionic Acid Derivatives
Authors: Dannhardt G. , Lehr M. 
Published: October 2006

AbstractA series of 19 N‐alkyl‐diarylpyrrolyl‐acetic and ‐propionic acid derivatives was synthesized and tested. Using bovine blood as enzyme source the inhibition of cyclooxygenase and 5‐lipoxygenase, respectively, was applied to determine the antiinflammatory activity. In general all compounds tested inhibit 5‐lipoxygenase more effectively than cyclooxygenase. A structure‐activity relationship is discussed.
Platelet Aggregation Inhibiting and Anticoagulant Effects of Oligoamines, XIX: 4,4′‐Phenylene‐bis‐sydnone Imines
Authors: Rehse Klaus , Kämpfe Michael , Martens Antje 
Published: October 2006

AbstractFourteen 4,4′‐m‐phenylene‐ and two 4,4′‐p‐phenylene‐bis‐sydnone imine hydrochlorides have been synthesized. All compounds exhibited good solubility in water. In the m‐series the 3‐(3‐phenylpropyl)‐derivative 5c and the 3‐hexyl compound 51 showed antiplatelet activities at or below 10 μmol/L (IC50, Born‐test with collagen). The corresponding p‐compounds had the same (61) or slightly lower (6c) activity. No effect on the fibrin formation (Quick‐test) could be observed.
Cer(IV)oxidationen von β‐Aminoketonen, 8. Mitt.: Synthese von im Piperidinteil verschieden substituierten 1,2,3,4‐Tetrahydroisochinolinen
Authors: Holzgrabe Ulrike , Inkmann Elisabeth 
Published: October 2006

Abstract1‐ und 3‐alkyl‐ und/oder arylsubstituierte 1,2,3,4‐Tetrahydroisochinoline sind durch oxidative Cyclisierung von N‐Benzyl‐β‐aminoketonen mit Cer(IV)sulfat zugänglich. In nahezu allen Fällen werden Diastereomerengemische erhalten. Nach Austausch der Ketofunktion des Aminoketones gegen COOR‐, CN‐, CHO‐ oder NO2‐Gruppen gelingt unter den Standardreaktionsbedingungen keine Cyclisierung, da die Hydrolyse zu N‐Benzyl‐N‐methylaminopropionsäure und die Oxidation in benzylischer Stellung zu Benzaldehyden und Benzoesäuren Überhand gewinnt. Im Fall der Oxidation des Benzylaminopropionaldehydacetal‐Derivates 1k wurde ein Isochinolindion 4k isoliert.
Zyklische Harnstoffe, 2. Mitt.: Racemate und Enantiomere von Imidazolidin‐2‐onen Synthese, Konfiguration und sedativ‐hypnotische Wirkung
Authors: Knabe Joachim , Büch Horst P. , Biwersi Joachim 
Published: October 2006

AbstractDie Racemate und die Enantiomere der Imidazolidin‐2‐one 2a und 2b, die man als zyklische Harnstoffe auffassen kann, werden aus den Racematen und den Enantiomeren der Hydantoine 1a und 1b durch Reduktion mit LiAlH4/AlCl3 gewonnen. Die in Ethanol rechtsdrehenden Enantiomere von 2a und 2b besitzen S‐Konfiguration. ‐ In Versuchen an Wistar‐Ratten waren 2a und 2b sedativ‐hypnotisch wirksam. Zwischen den Enantiomeren traten beachtliche enantioselektive Wirkungsunterschiede auf.
High‐Performance Liquid Chromatographic Analysis of Cyclosporine A in Human Skin
Authors: Husek Aleš , Eibler Ernst , Wiegrebe Wolfgag 
Published: October 2006

AbstractA three‐dimensional high‐performance liquid chromatography (HPLC) method is described for the determination of cyclosporine A in human skin. The method allows to determine at least 3 ng cyclosporine A in 10 mg skin (total sample amount needed) and is suitable for cyclosporine A level monitoring in the skin of psoriatic patients.
Dimethyl 3,3′‐(4‐Methyl‐1,3‐naphthylene)dipropionate as a Singlet Oxygen Trap in Biological Systems
Authors: Müller Klaus , Ziereis Klaus 
Published: October 2006

AbstractThe utility of dimethyl 3,3′‐(4‐methyl‐1,3‐naphthylene)dipropionate (DMNDP) as a singlet oxygen trap in biological systems is described. The determination of the rate constant for the reaction of DMNDP with singlet oxygen in acetonitrile gave a value of 9.8 · 10−7 M−1s−1; the half‐life of the corresponding endoperoxide at 37°C in phosphate buffered saline is 412 min. DMNDP does not possess sensitizing properties, and its usefulness for the detection of singlet oxygen is demonstrated in the photooxidation of liposomes by 5,10,15,20‐tetraphenyl‐21H, 23H‐porphine (TPP).
Synthesis and Anti‐HIV Activity of 5‐Alkoxymethyl‐3′‐azido‐2′,3′‐dideoxyuridines
Authors: Abdel‐Megied Ahmed E.‐S. , Hansen Poul , Pedersen Erik B. , Nielsen Claus , Nielsen Carsten M. 
Published: October 2006

AbstractMethyl 3‐azido‐5‐O‐tert‐butyldiphenylsilyl‐2,3‐dideoxy‐D‐erythro‐furanoside (3) was coupled with silylated 5‐hydroxymethyluracil (1a) and its C1‐C6 alkyl ethers 1b–g to give the corresponding protected nucleosides 4a‐g which were deprotected with Bu4NF to afford 3‐azido nucleosides 5a‐g and 6a‐g. The α‐anomers 6f,g show moderate activity against HIV. No significant activity against HSV‐1 was found for the compounds 5 and 6.
Synthesis and Evaluation of Sulfur‐Containing Glutethimide Derivatives for Aromatase and Desmolase Inhibitory Activity
Authors: Bednarski Patrick J. , Hartmann Rolf W. 
Published: October 2006

AbstractNovel sulfur‐containing glutethimide derivatives, substituted with either thiol or methylsulfide groups in the ortholpara positions of the aromatic ring, were synthesized and tested for both human placental aromatase and bovine adrenocortical desmolase inhibitory activities. The synthesis was achieved by the chlorosulfonation of gluthethimide, which yielded a 3:1 mixture of the para to ortho sulfonyl chlorides 2a/b. The sulfonyl chlorides of gluthethimide were reduced with Zn/H2SO4 to give the thioglutethimides 3a/b, which in turn were methylated with MeI/EtOH to give the corresponding methylsulfides 4a/b. In comparison to aminoglutethimide (AG). 3a/b and 4a/b were weak inhibitors of aromatase, with 3a/b being more potent than 4a/b. Aromatase inhibition by the thiol compound was pH‐dependent; 3a/b was most potent at higher pH (7.4) than at lower (6.6). This suggested that the thiolate form of 4 coordinates with the ferric heme of aromatase. Likewise, both 3a/b and 4a/b were less potent at inhibiting bovine adrenal desmolase than AG. Possible reasons for the surprisingly poor aromatase inhibitor activity of these compounds are discussed.
Synthesis and Biological Activity of Bromolignans and Cyclolignans
Authors: Feliciano Arturo San , Medarde Manuel , de Clairac Rafael Pelaez Lamamie , López Jose Luis , Puebla Pilar , Gravalos M Dolores García , Lázaro Pilar Ruiz , de Quesada M Teresa García 
Published: October 2006

AbstractNine lignan derivatives (4‐12) have been obtained from (‐)‐yatein by treatment with DDQ and NBS. They showed moderate antineoplastic activity (P‐388, A‐549, HT‐29) compared with podophyllotoxin, but some of them have a better therapeutic index. None of the tested compounds shows antiviral (HSV‐1, VSV) or enzyme inhibitor (ADA, DHFR, GST) activities.
Properties and Reactions of Substituted 1,2‐Thiazetidine 1,1‐Dioxides: Alkylation and Acylation of 3‐Haloalkyl β‐Sultams and Synthesis of Bicyclic β‐Sultams
Authors: Schwenkkraus Peter , Otto Hans‐Hartwig 
Published: October 2006

AbstractAlkylation of the 3‐chloroethyl substituted β‐sultam 1 with bromoacetates yields the N‐ and 3‐substituted β‐sultams 2; exchange of halogens affords esters 3. Reactions of 1 or of the analogues 8 with isocyanates make the carbamoyl derivatives 5, 6, and 9 available. While cyclization of 6 with n‐BuLi in the presence of HMPT yields the bicyclic β‐sultams 7, the analogous reaction of 9 failed. The bicyclic β‐sultams 12 and 14 are obtained from 3‐hydroxyalkyl β‐sultams 11 and 13 and carbonyl compounds. None of the prepared β‐sultams showed any antibacterial activity.
Heterocyclisch anellierte Indolizine durch intramolekulare [3 + 2]‐Cycloaddition mit Nicotinium‐dicyanmethyliden
Authors: Seitz Gunther , Tegethoff Ralph 
Published: October 2006

AbstractThermisch induzierte intramolekulare [3 + 2]‐Cycloadditionsreaktionen der Nicotinium‐dicanmethylide 4a‐c, die am Pyrrolidinstickstoff mit verschieden langen ω‐Alkinseitenketten substituiert sind, führen in guten Ausbeuten zu entspr. neuen, heterocyclisch anellierten Indolizinen 6‐8. Das mit einem aktivierten Seitenkettendipolarophil versehene Dicyanmethylid 9 liefert neben dem Indolizin 11 in geringen Mengen das Naphthyridin 14.
Chemical and Electrochemical Synthesis of Some Substituted N,N′‐Diacyl‐p‐phenylenediamines
Authors: Šuprina Mihela , Vorkapić‐Furač Jasna 
Published: October 2006

AbstractSome N,N′‐diacyl‐p‐phenylenediamines substituted with halogens (2a‐c) were prepared. Their polarographic reduction in N,N‐dimethylformamide with Et4NClO4 was performed and discussed. The mechanism of the electrochemical reduction is stated. Large‐scale electrolytic reductions of 2a‐b to 3a‐b were performed.
Synthese von potentiellen Naftopidil‐Metaboliten
Authors: Kutscher Bernhard , Engel Jürgen , Fleischhauer Ilona , Niebch Georg 
Published: October 2006

AbstractEs wird über die Synthese von vier potentiellen Metaboliten [Desmethyl‐Naftopidil (1), 4‐(Phenyl)‐hydroxy‐Naftopidil (2), 4‐(Naphthyl)‐hydroxy‐Naftopidil (3), Desanaphthyl‐Naftopidil (4)] des selektiven α1‐Antagonisten Naftopidil berichtet.
Synthese von basisch substituierten 5H‐Pyrimido[4,5‐c]‐2‐benzazepinen
Authors: Troschütz Reinhard , Grün Lothar 
Published: October 2006

AbstractDie potentiell ZNS‐wirksamen Titelverbindungen 19a‐c lassen sich durch eine neunstufige Synthese ausgehend von Phthalaldehydsäure herstellen. Durch Knoevenagel‐Kondensation von 5 mit den Acetonitrilen 2a‐g und folgender Reduktion mit NaBH4 erhält man die Dihydrozimtsäurenitrile 3. Nur 3a läßt sich zu den 2‐Benzazepinnitrilen 9a,b cyclisieren. Ammonolyse von 9a führt zum Enaminonitril 10, das mit den Orthoestern 11a‐c die Imidsäureester 12a‐c gibt. Nachfolgende Ammonolyse liefert die Tricyclen 16a,b. Nach Umwandlung der Lactamfunktion von 16 in das Imidoylchlorid 17 folgt Aminolyse mit den Aminen 18a‐c zu den Titelverbindungen 19a‐c.
Nitrosierungen an Hydrazinderivaten, 10. Mitt.: Oxidationen an Thiourethanen, 11. Mitt.: Reaktionen von 3‐Aminorhodaninen unter nitrosierenden Bedingungen
Authors: Hanefeld Wolfgang , Helfrich Volker , Hunz Ingrid , Jalili Mohamed A. , Schlitzer Martin 
Published: October 2006

AbstractC‐5‐unsubstituierte 3‐Aminorhodanine 1 werden durch NaNO2/HCl, Nitrosyl‐ und Nitroniumtetrafluoroborat in 5‐Hydroximinorhodanine 2 überführt, durch HNO3 in 5‐Hydroximinothiazolidin‐2,4‐dione 3. 5‐Aralkyliden‐3‐aminorhodanine 7 werden durch HNO2 unter drastischen Bedingungen in 2‐Stellung oxidativ desulfuriert.
Regioselektive Kondensationen sowie N‐Acylierungen an 3‐Aminorhodaninen
Authors: Hanefeld Wolfgang , Schlitzer Martin 
Published: October 2006

Abstract3‐Aminorhodanin wurde regioselektiv an der 3‐Amino‐ oder der 5‐Methylengruppe mit Aldehyden kondensiert. Mit Carbonsäurechloriden oder ‐anhydriden gelingt die Acylierung der 3‐Aminofunktion.