Synthese de sesquiterpenoiedes par l'addition d'alcynylvinylcarbenes sur des cyclenones

SIGLEINIST T 73132 / INIST-CNRS - Institut de l'Information Scientifique et TechniqueFRFranc

One-Step Conversion of Methyl Ketones to Acyl Chlorides

Treatment of aromatic and heteroaromatic methyl ketones with sulfur monochloride and catalytic amounts of pyridine in refluxing chlorobenzene leads to the formation of acyl chlorides. Both electron-rich and electron-poor aryl methyl ketones can be used as starting materials. The resulting C₁-byproduct depends on the precise reaction conditions chosen

Organic Synthesis on Solid Phase. (Supports, Linkers, Reactions)

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Short and Safe Synthesis of Ethyl 3‑(Trifluoromethyl)pyrazine-2-carboxylate

The treatment of ethyl 2-hydroxyimino-4,4,4-trifluoro-3-oxobutanoate (<b>3</b>) with trialkyl phosphites, ethylenediamine, and an excess of a carboxylic acid in pyridine or picoline leads to the formation of an intermediate, which can be aromatized to a pyrazine by treatment with bromine or other oxidants. This synthesis can be performed either with the isolated oxime <b>3</b> or from ethyl 4,4,4-trifluoro-3-oxobutanoate (<b>1</b>) in a one-pot fashion, without any solvent change and without having to isolate any intermediates

Título: Jotas de baile.

Etiqueta roja.Intérpretes: Intérpretes : Agrupación de Coros y Danzas de Zaragoza ; Rondalla Santamaría ; dir. Florencio Santamaría.Copia digital : BNE.Fuente de ingreso: César Rodríguez XaixoDatos de publicación tomados de BNE [consulta 25/06/2018

Design, synthesis and biological activity of novel peptidyl benzyl ketone FVIIa inhibitors

Herein is described the synthesis of a novel class of peptidyl FVIIa inhibitors having a C-terminal benzyl ketone group. This class is designed to be potentially suitable as stabilization agents of liquid formulations of rFVIIa, which is a serine protease used for the treatment of hemophilia A and B inhibitor patients. A library of compounds was synthesized with different tripeptide sequences, N-terminals and D-amino acids in the P3 position. Cbz-D-Phe–Phe–Arg–bk (33) was found to be the best candidate with a potency of Ki = 8 lM and no substantial inhibition of related blood coagulation factors (thrombin and FXa). Computational studies revealed that 33 has a very stable binding conformation due to intramolecular hydrogen bonds, which cannot be formed with L-Phe in the P3 position. Nonpolar amino acids were found to be superior, probably due to a minimization of the cost of desolvation upon binding to FVIIa