Synthesis of Aristotelia-Type Alkaloids. Part III. (3R,4R)- and (3R,4S)-1-p-menthene-3,8-diol and the corresponding racemates: Preparation and assignment of configuration

A 1:1 mixture of the racemic trans- and cis-1-p-menthene-3,8-diols ((±)- 3 and (±)- 4 , resp.) was readily prepared in 3 steps starting from 3-methyl-2-cyclohexen-1-one. The relative configuration of the diols, purified via the corresponding cyclocarbonates, was assigned by ¹H-NMR spectroscopy and found to be at variance with tentative claims in the literature. Optically active samples of 3 and 4 were prepared by resolution of the racemates with (R)-1-phenylethylamine. The absolute configuration of the resulting diols was determined by chemical correlation with standards of known absolute configuration.     

Synthesis of Aristotelia-Type Alkaloids.. Part IV. Synthesis of (±)-aristoserratine

A convergent diastereoselective synthesis of racemic aristoserratine ((±)- 24 ) via an intramolecular iminium-ion cyclization is described. The pivotal imine (±)- 19 was prepared by condensation of the two building blocks (± )-trans-8-amino-3-(2,6-difluorobenzyloxy)-1-p-menthene ((±)- 11 ) and N-(p-methoxybenzenesulfonyl)-3-indo-leacetaldehyde ( 18 ) which were synthesized from (±)-trans-1-p-menthene-3,8-diol ((±)- 7 ) and 3-indoleacetic acid, respectively. On the route to the target (±)- 24 , two previously unknown indole alkaloids have been characterized, namely (±)-‘anti’-hobartin-15-ol ((±)- 22 ) and (±)-‘anti’-aristotelin-15-ol ((±)- 23 ).     

Inner hair cell loss and steady-state potentials from the inferior colliculus and auditory cortex of the chinchilla

Steady-state evoked potentials were measured from unanesthetized chinchillas both before and after carboplatin-induced selective inner hair cell loss. Recordings were made from both the inferior colliculus (IC) and the auditory cortex (AC). The steady-state potential was measured in the form of the envelope following response (EFR), obtained by presenting a two-tone stimulus (f1 = 2000 Hz; f2 = 2020, 2040, 2080, 2160, or 2320 Hz), and measuring the magnitude of the Fourier coefficient at the f2-f1 difference frequency. From the IC, precarboplatin, EFR amplitude vs difference tone frequency showed a bandpass pattern, with maximum amplitude at either 160 or 80 Hz, depending upon stimulus level. Postcarboplatin, the preferred difference frequency was 80 Hz for all stimulus levels. From the AC, EFR amplitude versus difference tone frequency also showed a bandpass pattern, with the maximum amplitude at 80 Hz both pre- and postcarboplatin. EFR amplitude from the IC was decreased for some conditions postcarboplatin, while the amplitude from the AC showed no significant change.     

Quadratic assignment problems

This paper surveys quadratic assignment problems (QAP). At first several applications of this problem class are described and mathematical formulations of QAPs are given. Then some exact solution methods and good heuristics are outlined. Their computational behaviour is illustrated by numerical results. Further recent results on the asymptotic probabilistic behaviour of QAPs are outlined.     

A heuristic for quadratic Boolean programs with applications to quadratic assignment problems

A heuristic for quadratic Boolean programs is presented. Computational tests with quadratic assignment problems (QAP) showed that it finds very good suboptimal solutions in moderate time and behaves computationally stable. In the appendix a FORTRAN-program for QAP is listed which improves an earlier code published by Burkard and Derigs.     

Untersuchungen zum Optimum-Mix Problem

Zusammenfassung Zur Lösung vonm Aufgaben stehen jeweilsn Hilfsmittel zur Verfügung. Die Kostenfunktion für ein Hilfsmittel ist eine nichtlineare, monoton wachsende und konkave Funktion. Es wird zugelassen, daß eine Aufgabe durch mehrere Hilfsmittel gelöst wird. Gesucht ist eine Strategie, so daß die Gesamtkosten des Problems minimal werden. Es wird gezeigt, daß in der optimalen Strategie eine Aufgabe durch genau ein Hilfsmittel gelöst wird und ein Kriterium für Optimalität wird hergeleitet. Ferner wird ein Algorithmus angegeben, der es gestattet, die in Betracht kommenden Möglichkeiten stark einzuschränken, ohne die spezielle Gestalt der Kostenfunktionen zu kennen.

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Summary m tasks are to be carried out, each by a given number of resources of one particular kind.n different kinds are available. The cost function for resources is assumed to be nonlinear, monotonic, and strictly concave. It is admissible to carry out a task by simultaneous use of several resources. The problem is to find a strategy which minimizes the total costs. It will be shown that in an optimal strategy one task is carried out by exactly one kind of resource. A criterion for optimialization will be given. Further an algorithm is stated which permits to reduce the number of possibilities to be encountered without information about the special form of the cost functions.

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Vorgel. v.:N. Hofreiter     

Dephasing of a superconducting qubit induced by photon noise

We have studied the dephasing of a superconducting flux qubit coupled to a dc-SQUID based oscillator. By varying the bias conditions of both circuits we were able to tune their effective coupling strength. This allowed us to measure the effect of such a controllable and well-characterized environment on the qubit coherence. We can quantitatively account for our data with a simple model in which thermal fluctuations of the photon number in the oscillator are the limiting factor. In particular, we observe a strong reduction of the dephasing rate whenever the coupling is tuned to zero. At the optimal point we find a large spin-echo decay time of .     

On the Kleinewillinghöfer types of flat Laguerre planes

Kleinewillinghöfer classified in [7] Laguerre planes with respect to central automorphisms and obtained a multitude of types. For finite Laguerre planes many of these types are known to be empty. In this paper we investigate the Kleinewillinghöfer types of flat Laguerre planes with respect to the full automorphism groups of these planes and completely determine all possible types of flat Laguerre planes with respect to Laguerre translations.     

Synthesis of rel-(3RS,3aSR,7aSR)-3-(4-Chlorophenyl)-3a,4,5,6,7,7a-hexahydro-1-methylindolin-6-one,the Main Metabolite of the Analgesic Ro 15-8081: A Potent Amine-Uptake Inhibitor

The synthesis of the title compound 2 and its diastereoisomer 3 was accomplished using tricarbonyl[1-5-n-(4-methoxycyclohexa-2,4-dien-1-yl)]iron tetrafluoroborate ( 4 ) as a precursor to the cyclohexanone ring. The assignments of the relative configurations of 2 and 3 are based on the X-ray analysis of compound 3 . Both compounds 2 and 3 are potent inhibitors of neuronal noradrenaline uptake in rats with similar potencies in vitro as compared to amitriptyline and desipramine. Compounds 2 and 3 are less potent as serotonin-uptake inhibitors, very weak inhibitors of dopamine uptake, and virtually devoid of antinociceptive activity.