A new family of compounds made of a 5-aryl-1H-imidazole motif included in a macrocycle has been designed and synthesized. The synthesis of the imidazole core makes use of our previously developed method for the regioselective preparation of 1,2,5-trisubstituted imidazoles while the construction of the macrocycle is based on a three steps sequence: SNAr, Suzuki coupling, and RCM reaction. Biological evaluation of synthesized imidazole-containing macrocycles revealed that they display actual binding activity toward A3 adenosine (h) receptor, dopamine D1 (h) receptor, chloride channel (GABA-gated), and choline transporter (h) CHT1. 相似文献
The use N‐sulfonyl‐protected hydroxylamines as bi‐nucleophiles in iron‐catalyzed propargylic substitutions allows the selective one‐pot synthesis of four classes of substituted isoxazoles or isoxazolines from the same propargylic alcohols (21 examples) by simply tuning the nature of the base. By using an iron(III) catalyst and a base such as triethylamine (3 equiv), isoxazoles 3 are obtained in good isolated yields (56–95%), whereas N‐sulfonyl‐protected isoxazolines 6 are selectively obtained (77–93% yield) by using iron and gold catalysts in the presence of a catalytic amount of pyridine (10 mol%). 相似文献
Dispacamide A and new analogs of this marine alkaloid were prepared in seven steps with an overall yield ranging from 12 to 33%. The key step of the strategy was a stereocontrolled Knoevenagel condensation under microwave dielectric heating in the last step. In this condensation, the 2-aminoimidazolin-4-one hydrochloride partners 10a-c were synthesized in three steps with good overall yields (33-79%) via the ring closure of N-guanidino acetic acids 9a-c and the aldehydes 5a,b as the two others building-blocks, in 3 steps with 60-66% overall yields. The six synthetic products have been obtained with a Z geometry about their exocyclic bond on the basis of (13)C/(1)H long-range coupling constants using a gHSQMBC experiment. 相似文献
Acousto-optical coherence tomography (AOCT) consists in using random phase jumps on ultrasound and light to achieve a millimeter resolution when imaging thick scattering media. We combined this technique with heterodyne off-axis digital holography. Two-dimensional images of absorbing objects embedded in scattering phantoms are obtained with a good signal-to-noise ratio. We study the impact of the phase modulation characteristics on the amplitude of the acousto-optic signal and on the contrast and apparent size of the absorbing inclusion. 相似文献
A passively Q-switched dual-wavelength solid-state laser is presented. The two wavelengths are emitted by two different crystals in order to avoid gain competition, and the synchronization between the pulses is obtained by external triggering of the saturable absorber. Sum frequency mixing is demonstrated, proving the interest of this source for terahertz generation in the 0.3-0.4 THz range through difference frequency generation. 相似文献
The reactivity of the 7-chloro-8-iodo- and 8-chloro-7-iodoimidazo[1,2-a]pyridines 1a-e diversely substituted on the 2 position, towards Suzuki-Miyaura, Sonogashira, and Buchwald-Hartwig cross-coupling reactions as well as cyanation was evaluated. Various methodologies are proposed to introduce aryl, heteroaryl, alkyne, amine or cyano groups in the two positions depending on the nature of the substituent present in position 2. In both series, the substitution of the iodine atom was totally regioselective and the difficulty was to substitute the chlorine atom in a second step. Until now, only hetero(aryl) groups could be introduced though Suzuki-Miyaura cross-coupling. We overcame this problem evaluating both regioisomers in parallel. The double coupling approach was also studied allowing the one pot Suzuki/Suzuki, cyanation/Sonogashira and cyanation/Buchwald reactions leading to polyfunctionnalized imidazo[1,2-a]pyridines. 相似文献
A simple and reliable method based on capillary electrophoresis with electrochemical detection (CE–ED) was applied to study the effect of aerobic exercises on creatinine and uric acid concertration in saliva and urine. The pH value, the running buffer concentration, the SDS concentration, separation voltage, injection time and the potential applied to the working electrode were investigated to find the optimum conditions. The detection limits (S/N = 3) for creatinine and uric acid were 3.6 μmol L−1 and 0.86 μmol L−1, respectively. This method was successfully used in the rapid analysis of creatinine and uric acid in saliva samples. After aerobic exercises, creatinine concentration decreased, and uric acid concentration increased in saliva. In urine, the concentrations of creatinine and uric acid both increased after exercise.
Industrial optimization applications must be “robust” i.e., they must provide good solutions to problem instances of different size and numerical characteristics, and continue to work well when side constraints are added. This paper presents a case study that addresses this requirement and its consequences on the applicability of different optimization techniques. An extensive benchmark suite, built on real network design data, is used to test multiple algorithms for robustness against variations in problem size, numerical characteristics, and side constraints. The experimental results illustrate the performance discrepancies that have occurred and how some have been corrected. In the end, the results suggest that we shall remain very humble when assessing the adequacy of a given algorithm for a given problem, and that a new generation of public optimization benchmark suites is needed for the academic community to attack the issue of algorithm robustness as it is encountered in industrial settings. 相似文献
The study of separating invariants is a recent trend in invariant theory. For a finite group acting linearly on a vector space, a separating set is a set of invariants whose elements separate the orbits of G. In some ways, separating sets often exhibit better behavior than generating sets for the ring of invariants. We investigate the least possible cardinality of a separating set for a given G-action. Our main result is a lower bound that generalizes the classical result of Serre that if the ring of invariants is polynomial then the group action must be generated by pseudoreflections. We find these bounds to be sharp in a wide range of examples. 相似文献