0000000000073473

AUTHOR

Eva M. Brun

0000-0003-0118-6911

Enediolates and dienediolates of carboxylic acids in synthesis. Synthesis of β,γ-epoxyacids from α-chloroketones

Abstract Lithium dienolates of saturated or α,β-unsaturated acids react with α-chloroketones provide a convenient method for preparation of highly sustituted β,γ-epoxyacids. These highly reactive compounds lead in most cases to variable ammounts of the corresponding β-lactones and allylic alcohols.

research product

ChemInform Abstract: Enantioselective α-Alkylation of Unsaturated Carboxylic Acids Using a Chiral Lithium Amide.

Abstract The regio- and stereochemistry of the alkylation of dienediolates from unsaturated carboxylic acids with benzylic halides, which often results in mixtures of isomers, can be controlled by means of changes in the lithium amide, allowing the α-regioisomer to be obtained as the major diastereoisomer. In addition, when chiral amines are used, moderate enantiomeric excesses can be attained.

research product

Antibody-Capped Mesoporous Nanoscopic Materials: Design of a Probe for the Selective Chromo-Fluorogenic Detection of Finasteride

[EN] The synthesis of capped mesoporous silica nanoparticles (MSN) conjugated with an antibody (AB) as a gatekeeper has been carried out in order to obtain a delivery system able to release an entrapped cargo (dye) in the presence of a target molecule (antigen) to which the conjugated antibody binds selectively. In particular, MSN loaded with rhodamine B and functionalized on the external surface with a suitable derivative of N-(t-butyl)- 3-oxo-(5a,17b)-4-aza-androst-1-ene-17-carboxamide (finasteride) have been prepared (S1). The addition of polyclonal antibodies against finasteride induced capping of the pores due to the interaction with the anchored hapten-like finasteride derivative to g…

research product

Lithium enediolates and dienediolates of carboxylic acids in synthesis: Alkylation with secondary halides

Abstract High yields in the alkylation of dianions of α,β-unsaturated carboxylic acids with secondary halides can be obtained despite elimination reactions occurring. α-Regioselectivity for the alkylation of but-2-enoic acids ( 1–4 ) is seldom obtained. Although double bond stereoselectivity is higher than 99% for γ-alkylated products, stereoselectivity is rather poor for most of the α-alkylated products.

research product

ChemInform Abstract: Enediolates and Dienediolates of Carboxylic Acids in Synthesis. Synthesis of β,γ-Epoxyacids from α-Chloroketones.

Abstract Lithium dienolates of saturated or α,β-unsaturated acids react with α-chloroketones provide a convenient method for preparation of highly sustituted β,γ-epoxyacids. These highly reactive compounds lead in most cases to variable ammounts of the corresponding β-lactones and allylic alcohols.

research product

ChemInform Abstract: New Conditions for the Generation of Dianions of Carboxylic Acids.

Abstract Lithium carboxylic acid enediolates are generated efficiently using lithium amides prepared from thienyllithium or butyllithium and either diethylamine, piperazine, N,N′-dibenzylethylenediamine, N-benzylpiperazine or 1,3,3-trimethyl-6-azabicyclo[3.2.1]octane, even in catalytic amounts.

research product

New conditions for the generation of dianions of carboxylic acids

Abstract Lithium carboxylic acid enediolates are generated efficiently using lithium amides prepared from thienyllithium or butyllithium and either diethylamine, piperazine, N,N′-dibenzylethylenediamine, N-benzylpiperazine or 1,3,3-trimethyl-6-azabicyclo[3.2.1]octane, even in catalytic amounts.

research product

Enantioselective α-alkylation of unsaturated carboxylic acids using a chiral lithium amide

Abstract The regio- and stereochemistry of the alkylation of dienediolates from unsaturated carboxylic acids with benzylic halides, which often results in mixtures of isomers, can be controlled by means of changes in the lithium amide, allowing the α-regioisomer to be obtained as the major diastereoisomer. In addition, when chiral amines are used, moderate enantiomeric excesses can be attained.

research product

ChemInform Abstract: Lithium Enediolates and Dienediolates of Carboxylic Acids in Synthesis: Alkylation with Secondary Halides.

Abstract High yields in the alkylation of dianions of α,β-unsaturated carboxylic acids with secondary halides can be obtained despite elimination reactions occurring. α-Regioselectivity for the alkylation of but-2-enoic acids ( 1–4 ) is seldom obtained. Although double bond stereoselectivity is higher than 99% for γ-alkylated products, stereoselectivity is rather poor for most of the α-alkylated products.

research product

New approach to condensed pyrid-2-ones

We wish to report a simple procedure for the preparation of 5-substituted-thienopyridin-7-ones and 7-substituted-1,6-naphthyridin-5(6H)-ones, in good yields, from the dianions of 3-methylthiophene-2-carboxylic and 2-methylnicotinic acids on treatment with nitriles. Brun Sanchez, Eva Maria, Eva.M.Brun@uv.es ; Gil Grau, Salvador, Salvador.Gil@uv.es ; Parra Alvarez, Margarita, Margarita.Parra@uv.es

research product