Synthesis of functionalised β-keto amides by aminoacylation/domino fragmentation of β-enamino amides
作者:Pavel Yanev、Plamen Angelov
DOI:10.3762/bjoc.14.238
日期:——
Ethylenediamine-derived β-enamino amides are used as equivalents of amide enolate synthons in C-acylation reactions with N-protected amino acids. Domino fragmentation of the obtained intermediates leads to functionalised β-keto amides, bearing a protected amino group in their side chain.
Process and intermediates for .beta.-lactam antibiotics
申请人:Harvard University
公开号:US04665171A1
公开(公告)日:1987-05-12
1-Benzyl (or substituted benzyl)-3.beta.-[4(S)-aryloxazolidin-2-one-3-yl]-4.beta.-(2-arylvinyl)azet idin-2-ones are provided via cycloaddition of a 4(S)-aryloxazolidin-2-one-3-ylacetyl halide and an imine formed with a benzylamine and a 3-arylacrolein, e.g. cinnamaldehyde. The azetidinones are useful chiral intermediates in an asymmetric synthesis of 1-carba(1-dethia)-3-hydroxy-3-cephem-4-carboxylic acids and esters and to monocyclic .beta.-lactam antibiotics.
7.beta.-Acylamino-3-trifluoromethylsulfonyloxy-1-carba-3-cephem-4-carboxyli c acid antibiotic compounds, esters and salts thereof, and the corresponding 7-amino and protected 7-amino 1-carbacephalosporins are provided. The 3-trifluoromethylsulfonyloxy-substituted 1-carbacephalosporins also are useful in a process for preparing 3-halo-1-carbacephalosporins which comprises reacting a 3-triflate ester with a lithium halide in an aprotic polar solvent.
[EN] PROCESS OF PREPARATION OF OPTICALLY ACTIVE ALPHA AMINOACETALS<br/>[FR] PRÉPARATION D'ALPHA AMINOCÉTALS OPTIQUEMENT ACTIFS
申请人:CLARIANT SPECIALTY FINE CHEM
公开号:WO2009106386A1
公开(公告)日:2009-09-03
The invention relates to a process for preparing optically active α-aminoacetals by resolution of a racemic mixture or of a mixture of enantiomers via the formation of diastereoisomeric salts, and also novel intermediates in the form of diastereoisomeric salts.
Composition containing a penem or carbapenem antibiotic
申请人:SANKYO COMPANY LIMITED
公开号:EP0178911A2
公开(公告)日:1986-04-23
57 Administration of an N-acylated amino acid (ornithine, lysine, phenylglycine or phenylalanine) in association with a penem or carbapenem antibiotic relieves or eliminates the renal problems associated with administration of the antibiotic alone. The amino acid and antibiotic may be formulated together as a composition or administered separately, either simultaneously or sequentially. A pharmaceutical composition may be prepared simply by mixing the two components.