The present disclosure relates to site-selective labeling compounds, and methods of using such compounds.

The present invention provides a means capable of selectively introducing a disulfide bond with respect to two free thiol groups located in a molecule of an organic compound such as a peptide, or the like, in a short time by a simple treatment and also by a chemically stable method.

A nitrogen-containing compound represented by Chemical Formula 1 below or a salt thereof:

##STR00001##

The symbols shown in Chemical Formula 1 are the same as defined in the specification.

An improved method for coupling carboxylic acids and amines is disclosed that includes the steps of combining a hyper-acid sensitive linker connecting an amine and a resin, a carboxylic acid, a carbodiimide, an activator additive, and a base, and carrying out the activation and coupling at a temperature greater than 30 C.

The present invention refers to a method for preparing a glucagon-like peptide, comprising precipitation of the peptide or of a precursor peptide by means of mixing with an anti-solvent comprising diisopropyl ether and acetonitrile. Further, the present invention also relates to a peptide conjugated to a solid phase and a pharmaceutical composition comprising a Liraglutide peptide obtainable from a method according to the present invention.

The present invention refers to a method for preparing a glucagon-like peptide, comprising precipitation of the peptide or of a precursor peptide by means of mixing with an anti-solvent comprising diisopropyl ether and acetonitrile. Further, the present invention also relates to a peptide conjugated to a solid phase and a pharmaceutical composition comprising a Liraglutide peptide obtainable from a method according to the present invention.

The present invention relates to -PNA monomers according to Formula I where substituent groups R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, B and P are defined as set forth in the specification. The invention also provides methodology for synthesizing compounds according to Formula I and methodology for synthesizing PNA oligomers that incorporate one or more Formula I monomers.

The present invention relates to -PNA monomers according to Formula I where substituent groups R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, B and P are defined as set forth in the specification. The invention also provides methodology for synthesizing compounds according to Formula I and methodology for synthesizing PNA oligomers that incorporate one or more Formula I monomers.

Disclosed is a new process and intermediates for preparing dipyrrolidine peptide compounds such as, for example, rapastinel. Advantageously, the process may be industrially scalable and cost-effective and use less toxic reagents and/or solvents. Further, the process may be used to prepare peptide compounds having improved purity.

Disclosed is a new process and intermediates for preparing dipyrrolidine peptide compounds such as, for example, rapastinel. Advantageously, the process may be industrially scalable and cost-effective and use less toxic reagents and/or solvents. Further, the process may be used to prepare peptide compounds having improved purity.

Disclosed herein are formulations, substrates, and arrays for amino acid and peptide synthesis on microarrays. In certain embodiments, methods for manufacturing and using the formulations, substrates, and arrays including one-step coupling, e.g., for synthesis of peptides in a C.fwdarw.N orientation are disclosed. In some embodiments, disclosed herein are formulations and methods for high efficiency coupling of biomolecules to a substrate.