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The present invention relates to novel derivatives of 2”-deoxyuridine substituted in the 5-, 3”- or 5”-position by alpha-aminoacyl groups, to a process for their preparation and the drugs in which they are present.These derivatives have the following general formula: STR1 in which R is selected from an alkyl or alkenyl radical having from 1 to 4 carbon atoms, an aryl radical or a halogen, it being possible for said alkyl, alkenyl and aryl radicals to contain at least one halogen substituent, and a radical of the formula –NH–R 1, in which R 1 is an amino acid residue or a peptide residue containing from 2 to 6 amino acids; andR” and R”” are selected from a hydroxyl radical and a radical of the formula –NH–R 1, in which R 1 is as defined above,with the proviso that R” and R”” are not simultaneously –NH–R 1 and that, when R is –NH–R 1, R” and R”” are simultaneously a hydroxyl group.Application: treatment of cancers and viral infections.

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A route to the preparation of enantiopure ligands based on a 2-phenylimidazol ring is described. The stereogenic centre is placed into the chain bonded to the fourth carbon of the imidazole ring. The synthesis starts from inexpensive and readily available N-protected alpha-amino acids, as the source of chirality, which are converted into appropriate alpha-diazoketones and, consequently, into alpha-bromoketones. These alpha-bromoketones are good precursors for reactions with amidines to provide the imidazole ring. The deprotection into the final products was carried out using hydrogen.

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Catalysts function by providing an alternate reaction mechanism that has a lower activation energy than would be found in the absence of the catalyst. In a patent, Recommanded Product: 3-Phenyl-6-chloropyridazine, molecular formula is C10H7ClN2, introducing its new discovery. Recommanded Product: 3-Phenyl-6-chloropyridazine

The reaction of the activated form of N-protected amino acids 6 and 10 or peptides 14 and 18 with chiral amino alcohols derived from the corresponding alpha-amino acids affords peptide alcohols which can be oxidized under Swern conditions to produce the corresponding peptide aldehydes 9, 12, 16 and 20. The rational synthesis of diastereomeric di- and tripeptide aldehydes, e.g., (S,S)- or (R,S)-dipeptides as well as (S,S,S)- or (R,S,S)-tripeptides is possible by proper choice of the respective building blocks [(S)- versus (R)-amino acids]. The compounds can be prepared without any undesired alpha-epimerization. However, the long-term configurational stability depends upon the configuration at the remote stereogenic center, e.g., (R,S)-dipeptide aldehydes epimerize faster than the (S,S) diastereomers. Di- and tripeptide aldehydes 9, 12, 16 and 20 undergo chelation-controlled Grignardtype additions with Me2CuLi that involve little or no undesired alpha-epimerization. The (S,S)- and (R,S)-dipeptide aldehydes 9 and 12 undergo chelation-controlled pinacol reactions induced by the low-valent vanadium reagent [V2Cl3(THF)6]2[Zn2Cl 6]. The major products in both cases are the corresponding C2-symmetric diols 33 and 36, respectively, which are of interest as potential HIV-protease inhibitors. The degree of stereoselectivity is significantly higher in the case of the (S,S)-dipeptide aldehydes relative to the (R,S) analogs, an observation which can be explained on the basis of three-point binding of the peptides to vanadium. VCH Verlagsgesellschaft mbH, 1996.

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A proton NMR method has been used to monitor racemisation during the coupling of N-methylated amino acids by the diphenylphosphinic mixed anhydride procedure.No racemisation was observed when urethane protection employed, but use of the benzoyl group led extensive racemisation.The reagent was subsequently used for the assembly of several extensively N-methylated peptides.

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The peptide compound represented by the formula: STR1 which is useful as a germicide or disinfectant, is produced by reducing a compound of the formula: STR2 wherein Y is amino group which may optionally be protected; R1 is hydrogen or protective group; and R2 is hydrogen or protective group; and subjecting the reduction product compound to deprotection reaction when required. A compound of the formula: STR3 wherein Z is amino group which may optionally be protected; R1 is hydrogen or protective group; and R2 is hydrogen or protective group, is a useful as intermediate for production of the first-mentioned compound.

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A novel macrobicycle featuring an amidopyridine unit as a carboxylic acid binding site, and amide functionality to provide further hydrogen bonding interactions with suitable guests has been prepared. The ability of this novel macrobicycle to bind peptide derivatives has been investigated.

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A readily available and inexpensive natural alpha -amino acid is converted into a compound represented by formula (1), which is then reacted with an organometallic reagent represented by formula (2) to give an optically active 5-hydroxyoxazolidine represented by formula (3), which is then treated with an acid to provide an optically active aminoketone represented by formula (4). The product is then converted into an optically active aminoalcohol represented by formula (5) or (6) by, for example reduction.The above process can provide an optically active aminoalcohol represented by formula (5) or (6) useful as a production intermediate for a medicine or pesticide from a readily available and inexpensive natural alpha-amino acid as a starting material stereoselectively and stably with a higher optical purity and a lower cost without racemization. This invention can also provide an optically active 5-hydroxyoxazolidine represented by formula (3) and an aminoketone represented by formula (4) as important intermediates for production of the above product as well as preparation processes therefor.

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The asymmetric epoxidation of chalcone and other electron-poor olefins in a triphase system (water-organic solvent-polyaminoacid) affords optically active oxiranes.The influence of the molecular structure of catalysts and of their secondary conformation on the enantioselectivity of the reaction has also been examined.

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The present invention provides a novel compound having a superior activity as an ERR-alpha modulator and useful as an agent for the prophylaxis or treatment of ERR-alpha associated diseases. The present invention relates to a compound represented by the formula (1) wherein each symbol is as defined in the specification, or a salt thereof

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A procedure for the cyclization of dipeptidoyl benzotriazolides containing proline derivatives promoted by triethylamine under MW activation is introduced. The reaction is general for a variety of dipeptidoyl benzotriazolides and represents a very practical and convenient method for the preparation of Pro- or Hyp-derived 2,5-diketopiperazines (2,5-DKPs) and bis-DKPs with a disulfide linker. This method can be used for the construction of 2,5-DKP compound libraries and for the synthesis of natural products with diketopiperazine cores. This journal is

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