Réductions chimique et électrochimique de 5H-benzopyranno[4,3-d]pyrimidines

The chemical reduction of 5H-[1]benzopyranno[4,3-d]pyrimidines with lithium aluminum hydrrde leads to 3,4-dihydro derivations. The electro-chemical reducation in acidic medium shows two monoelectronic cathodic waves. In netural or basic medium, substituted compounds in 2 position show a single bielectronic wave while two bielectronic waves are observed for unsubstituted compounds In all cases, preparative electrolysis lead to a hydrodimer in the 4,4′-positiom.     

Enantioselective Synthesis of Both Enantiomers of a Isoproterenol Analogue and of Di-O-pivaloylepinephrine

An asymmetric synthesis of the analogue 4a of isoproterenol and of di-o-pyvaloylepinephrine 3 which provides both enantiomers in optically pure state is reported. The key step of the method is the highly diastereo-selective reduction (using DIBAL or DIBAL/ZnCl₂) of a β-ketosulfoxide 7 which leads, as desired, to the (S)- or the (R)-configuration at C(1) (Schemes 4 and 5).     

Direct evidence for highly organized networks of circular surface micelles of surfactant at the air-water interface

We report the first direct evidence for the formation of circular surface micelles (hemimicelles) on the surface of water. These highly monodisperse 30 nm hemimicelles, made from a semifluorinated alkane deposited as a Langmuir monolayer, form organized hexagonal arrays as determined by small-angle X-ray diffraction conducted directly on the water surface at grazing incidence.     

C 1-generic billiard tables have a dense set of periodic points

We prove that the set of periodic points of a generic C ¹-billiard table is dense in the phase space.     

New Quinoxaline Derivatives as Dual Pim-1/2 Kinase Inhibitors: Design,Synthesis and Biological Evaluation

Proviral integration site for Moloney murine leukemia virus (Pim)-1/2 kinase overexpression has been identified in a variety of hematologic (e.g., multiple myeloma or acute myeloid leukemia (AML)) and solid (e.g., colorectal carcinoma) tumors, playing a key role in cancer progression, metastasis, and drug resistance, and is linked to poor prognosis. These kinases are thus considered interesting targets in oncology. We report herein the design, synthesis, structure–activity relationships (SAR) and in vitro evaluations of new quinoxaline derivatives, acting as dual Pim1/2 inhibitors. Two lead compounds (5c and 5e) were then identified, as potent submicromolar Pim-1 and Pim-2 inhibitors. These molecules were also able to inhibit the growth of the two human cell lines, MV4-11 (AML) and HCT-116 (colorectal carcinoma), expressing high endogenous levels of Pim-1/2 kinases.     

Synthesis of 3-aminochroman derivatives by radical cyclization

[reaction: see text] Enantiomerically pure 5-acetyl-3-amino-3,4-dihydro-2H-1-benzopyran and methyl 3-amino-3,4-dihydro-2H-1-benzopyran-5-carboxylate were successfully synthesized starting from d- or l-serine. The formation of the benzopyran ring involved a radical cyclization step. The enantiomeric purities of the final aminochroman derivatives were determined by capillary electrophoresis using beta-cyclodextrins as a chiral selector.     

Measurement of Total and Unbound Mycophenolic Acid and Its Glucuronide by LC Coupled with MS. Application to a Pharmacokinetic Study of Mycophenolate Mofetil in Patients with Autoimmune Diseases

Liquid chromatography coupled with mass spectrometry for the determination of total and unbound mycophenolic acid and its major metabolite in human plasma has been developed. Sample preparations were based on a fully automated solid-phase extraction process and ultrafiltration. Mass spectrometric data were acquired in a single-ion monitoring method. The analytes and nevirapine (internal standard) were well separated in an isocratic mode over 8 min. Validation study exhibited excellent linearity, with intra- and inter-day precision and accuracy of less than 12%. The assay was successfully applied to the pharmacokinetic study of mycophenolic acid in patients with autoimmune diseases.     

Rheological characterization of a solder paste for surface mount applications

Solder pastes used in surface mount soldering techniques (SMT) are very complex suspensions containing high volumes of metallic powder in a carrier fluid. The rheological complexity results largely from the carrier fluid itself, which is a suspension of colloidal particles. In this work, we have characterized the rheological properties of a typical carrier fluid and its solder paste containing 64 vol.% metallic powder. A six-blade vane geometry was used to avoid wall slip and sample fracture. All measurements were carried out following pre-shearing and rest time in order to obtain reproducible results. Steady shear experiments showed that the solder paste was highly shear-thinning and thixotropic. In oscillatory shear, the linear viscoelastic domain was found to be very narrow for both the suspending fluid and the paste. Frequency sweep tests in the linear domain revealed a gel-like structure with a nearly constant G′ for the suspending fluid and a slightly increasing G′ for the solder paste. From creep experiments, a yield stress of about 40 Pa was determined for the suspending fluid at temperatures between 25 and 40°C, and of 100 Pa at 4°C. A much larger yield stress, 480 Pa, was determined for the solder paste at 25°C.     

Prediction of the flow field over an orbiter entering the Mars atmosphere

This paper presents the methodology and the physical models implemented in our computational code to predict the flow field over a Mars Sample Return Orbiter entering a Mars-like atmosphere. Because no validation against flight data or experiments can be done at present, the results obtained here are compared to other computed results for verification purpose. The predicted flow fields show that the chemical species CO and CO₂, that are highly radiative species, are present in a large amount and at high temperature in the shock layer and in the wake of the flow past the orbiter.