Search results for "synthesis"

A generalizability measure for program synthesis with genetic programming

2021

The generalizability of programs synthesized by genetic programming (GP) to unseen test cases is one of the main challenges of GP-based program synthesis. Recent work showed that increasing the amount of training data improves the generalizability of the programs synthesized by GP. However, generating training data is usually an expensive task as the output value for every training case must be calculated manually by the user. Therefore, this work suggests an approximation of the expected generalization ability of solution candidates found by GP. To obtain candidate solutions that all solve the training cases, but are structurally different, a GP run is not stopped after the first solution …

Intragenic G-quadruplex structure formed in the human CD133 and its biological and translational relevance.

2016

Cancer stem cells (CSCs) have been identified in several solid malignancies and are now emerging as a plausible target for drug discovery. Beside the questionable existence of CSCs specific markers, the expression of CD133 was reported to be responsible for conferring CSC aggressiveness. Here, we identified two G-rich sequences localized within the introns 3 and 7 of the CD133 gene able to form G-quadruplex (G4) structures, bound and stabilized by small molecules. We further showed that treatment of patient-derived colon CSCs with G4-interacting agents triggers alternative splicing that dramatically impairs the expression of CD133. Interestingly, this is strongly associated with a loss of C…

A hardware skin-segmentation IP for vision based smart ADAS through an FPGA prototyping

2017

International audience; In this paper we presents a platform based design approach for fast HW/SW embedded smart Advanced Driver Assistant System (ADAS) design and prototyping. Then, we share our experience in designing and prototyping a HW/SW vision based smart embedded system as an ADAS that helps to increase the safety of car's drivers. We present a physical prototype of the vision ADAS based on a Zynq FPGA. The system detects the fatigue state of the driver by monitoring the eyes closure and generates a real-time alert. A new HW/SW codesign skin segmentation step to locate the eyes/face is proposed. Our presented new approach migrates the skin segmentation step from processing system (S…

Stereoselective synthesis of oligosaccharides by de novo saccharide welding

2012

Synthetic Inhibitors of Cell Adhesion: A Glycopeptide from E-Selectin Ligand 1 (ESL-1) with the Arabino Sialyl Lewisx Structure

2001

Particularly selective methods are required for the synthesis of arabino sialyl Lewisx glycopeptides owing to the acid-labile β-arabinopyranoside bond. It is important for the inhibition of cell adhesion that the arabino sialyl Lewisx glycopeptide 1, which contains the Gly 672 -Asp 681 sequence of the E-selectin Ligand 1 (ESL-1), binds ten times more strongly than sialyl Lewisx to E-selectin, although it is monovalent and does not contain L-fucose, which is considered essential.

Electrosynthesis and electrochemistry

2015

Since the pioneering work of Kolbe, electrochemistry and electrosynthetic methods have been a part of the repertoire of the organic synthesis toolbox [1–2]. In general, only electrons are employed as reagents or the reagents are electrochemically regenerated. Consequently, waste can be avoided, and limited resources can be used in a careful and economic manner. Because alternative reaction pathways are employed by electrosynthetic methods, scarce and toxic elements can be replaced or are not required at all [3]. Moreover, in the foreseeable future regenerative sources of electricity, for example, photovoltaics and wind power, will provide a surplus of electricity as the current unsteady sup…

Copper-Catalyzed One-Pot Synthesis of 3-(N -Heteroarenyl)acrylonitriles through Radical Conjugated Addition of β-Nitrostyrene to Methylazaarenes

2020

Designing Silylatedl-Amino Acids using a Wittig Strategy: Synthesis of Peptide Derivatives and18F-Labelling

2017

An efficient semisynthesis of silylated l-amino acids by reaction of silylated benzaldehydes with a phosphonium l-amino acid used as a Wittig reagent is described. The efficiency of the silylated l-amino acids in peptide synthesis was investigated by coupling both the carboxylic acid and the amino moiety with l-alanine and phenylalanine derivatives, respectively. The silylated derivatives were treated with KF or tetrabutylammonium fluoride to give the corresponding fluorosilyl derivatives without racemization. The hydrolysis of the fluorosilylated derivatives in phosphate buffer at pH 7.2 was checked. Finally, the 18F-labelling of di-tert-butylsilylated saturated and unsaturated dipeptides …

Synthesis of Optically Active Hydroxyalkyl Cycloheptatrienes: A Key Step in the Total Synthesis of 6,11-Methylene-LXB4

2020

AbstractStarting from methyl cycloheptatrienyl-1-carboxylate, 6-acylation was successfully achieved employing glutaryl chloride in the presence of AlCl3 under controlled reaction conditions to furnish keto carboxylic acid product. After protection of this keto carboxylic acid as tert-butyl ester, reagent-controlled enantioselective reductions delivered configuration-defined methyl-6-hydroxylalkyl cycloheptatriene-1-carboxylates with up to 80% ee. Whereas simple NaBH4 reduction of the keto carboxylic acid and subsequent lactonization afforded a methyl-6-tetrahydropyranonyl cycloheptatriene-1-carboxylate. Resolution using chiral HPLC delivered the product enantiomers with up to >99% ee Fin…

Recent Developments in the Chiral Brønsted Acid-catalyzed Allylboration Reaction with Polyfunctionalized Substrates

2016

Asymmetric allylboration has played a central role in organic synthesis ever since the pioneering work by Hoffman and Brown, having found applications in the total synthesis of many natural products. A new dawn for this 40 year-old reaction occurred with the beginning of the new century when the first catalytic asymmetric methods came into play. In less than one decade, several methodologies, able to achieve the desired homoallylic alcohols with ee ranges in the high 90s, were developed. Among them, in the present account, we will disclose our contribution to the development of the chiral binolphosphoric-derived BrOnsted acid-catalyzed allylboration of aldehydes originally reported by Antil…