Abstract: This invention relates to a process for introducing two or more 2?-modifications into an RNA, wherein the RNA has a 2?-O substituent containing an alkyl ester functional group on one or more ribose rings of a strand and a 2?-O substituent containing an alkyne functional groups on one or more ribose rings on the same strand. The process comprises a) adding an amine compound to the RNA to form amidation reactions with the alkyl ester functional groups; b) dissolving the modified RNA from step (a) in a solvent to form a solution; and c) adding an organic azide and a copper or ruthenium catalyst to the solution obtained in step (b) to form 2?-azide-alkyne cycloaddition reaction products with the alkyne functional groups.

Abstract: This invention relates to the post-synthetic chemical modifications of RNA at the 2?-position on the ribose rings via orthogonal chemistry involving amidation reactions plus metal catalyzed alkyne-azide cycloaddition (click) reactions.

Abstract: The present invention relates to a process for the efficient preparation of enantiomerically enriched beta amino acid derivatives wherein the amino group is unprotected. The product chiral beta amino acid derivatives are useful in the asymmetric synthesis of biologically active molecules. The process comprises an enantioselective hydrogenation of an amine-unprotected prochiral beta-amino acrylic acid or derivative thereof in the presence of a rhodium metal precursor complexed with a chiral mono- or bisphosphine ligand.

Abstract: The present invention relates to a process for the efficient preparation of enantiomerically enriched beta amino acid derivatives which are useful in the asymmetric synthesis of biologically active molecules. The process comprises an enantioselective hydrogenation of a prochiral beta amino acrylic acid derivative substrate in the presence of a transition metal precursor complexed with a chiral ferrocenyl diphosphine ligand.

Abstract: The present invention addresses a process for the preparation of 2,4,5-trifluorophenylacetic acid using a Cu(I) salt as a catalyst.

Abstract: &ggr;-Hydroxy-2-(fluoroalkylaminocarbonyl)-1-piperazinepentanamide compounds are inhibitors of HIV protease and inhibitors of HIV replication. These compounds are useful in the prevention or treatment of infection by HV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described. These compounds are effective against HIV viral mutants which are resistant to HIV protease inhibitors currently used for treating AIDS and HIV infection.

Abstract: Pharmaceutically acceptable hydrochloride and hydrobromide salts of Compound A are disclosed, wherein Compound A is of formula: 1

Abstract: The instant invention provides a homologation process for making a zincate homoenolate from a carbon bound enolate zincate, by treating the carbon bound enolate zincate with an alkoxy lithium reagent. The homologation step can be coupled with a homoaldol reaction, as well as with other transmetallation reactions, in a one pot process. The zincate homoenolate is a useful intermediate in the preparation of a variety of different end-products, such as HIV protease inhibitors and renin inhibitors.

Abstract: A biotransformation process for the production of an intermediate used in the chemical synthesis of an antibiotic compound.

Abstract: .beta.- or .gamma.-Ketoesters and .beta.- or .gamma.-ketoamides are asymmetrically reduced with a Ru(II)-BINAP derived catalyst at about 40.degree. C. and about 50N/mm.sup.2 of hydrogen in the presence of a strong acid.