- 2-Naphthol as a powerful chromophore for the configurational assignment of carboxylic acid groups via the CD exciton chirality method
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A novel approach for the stereochemical assignment of carboxylic acid groups via the circular dichroism (CD) exciton chirality method using the 2- naphthyl chromophore is described. Direct esterification of carboxyl groups with 2-naphthol was effectively achieved with the employment of N,N-bis[2- oxo-3-oxazolidinyl]phosphorodiamidic chloride as the activating reagent. The method was tested with several model compounds, including both cyclic and acyclic dicarboxylic acids, and also applied to the natural product abietic acid. (C) 2000 Elsevier Science Ltd.
- Hartl, Michaela,Humpf, Hans-Ulrich
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- Synthesis and antimicrobial activity of 3-[(4-substituted) (2-oxo-1,3-oxazolidin-3-yl) phosphoryl]-1,3-oxazolidin-2-ones
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3-[(4-Substituted) (2-oxo-1,3-oxazolidin-3-yl)-phosphoryl]-1,3-oxazolidin- 2-ones (4a-j) were synthesized through a two-step process. Bis-(2-oxo-1,3- oxazolidin-3-yl)-phosphonic chloride (2) prepared by the reaction of two moles of oxazolidin-2-one (1) with phosphorus oxychloride in dry tetrahydrofuran in the presence of triethylamine and treatment with various heterocyclic aromatic and aliphatic amines under the same experimental conditions afforded the title compounds (4a-j). They were characterized by elemental analysis, IR, NMR ( 1H, 13C and 31P) and mass spectroscopy. Their antimicrobial activities were also evaluated.
- Reddy, Mudumala V. N.,Ravi Sankar,Siva Kumar,Suresh Reddy,Naga Raju
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experimental part
p. 43 - 46
(2009/04/06)
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- Non-Imuunosuppressive cyclosporins and their use in the prevention and treatment of HIV infection
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Disclosed are cyclosporin analogs having amino acid residue substitutions at positions 1, 3, or 7 of the cyclosporin peptide backbone. Also disclosed are conjugates of these cyclosporin analogs in which an HIV protease inhibitor moiety is conjugated to the position-7 amino acid residue of the cyclosporin. These compounds simultaneously bind to and inhibit cyclophilin and HIV protease. The compounds have good bioavailability and potent HIV inhibitory activity. They are useful in the treatment and prevention of HIV-mediated disorders, including AIDS.
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- NOTE ON THE PREPARATION OF VERY ACTIVE N,N-BIS(2-OXO-3-OXAZOLIDINYL)-PHOSPHORODIAMIDIC CHLORIDE (Bop-Cl), AN EXTREMELY EFFECTIVE REAGENT FOR PEPTIDE FORMATION.
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A preparation of high-quality coupling reagent Bop-Cl is reported.It fulfills the expectations of reproducibility in efficient peptide coupling reactions that are characterized by the formation of little side products and by clean work-up.
- Auwera, C. Van der,Anteunis, M. J. O.
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p. 203 - 206
(2007/10/02)
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- NEW ACTIVATION OF CARBOXYLIC ACIDS BY REACTION WITH N,N-BIS-(2-OXO-3-OXAZOLIDINYL) PHOSPHORODIAMIDIC CHLORIDE (ClSPO)
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Pentacoordinated and quinquevalent phosphorus intermediates, have been isolated by reaction between the title reagent and carboxylic acids, prior to conversion into amides.
- Cabre-Castellvi, Juan,Palomo-Coll, Antonio Luis
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p. 4179 - 4182
(2007/10/02)
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