A PEG linker as represented by formula (I), wherein n and m are respectively an integer from 1 to 7, providing the PEG linker with 1 to 49 linking sites. A ligand drug conjugate as represented by formula (II). The conjugate uses the PEG linker to increase a drug loading capacity and drug loading diversity, thereby improving pharmaceutical efficacy.
Y1-PEG1-{R.sup.1-PEG2-{Y4}.sub.n}.sub.m  (I)
TM-{R.sup.2-PEG1-{R.sup.1-PEG2-{R.sup.3-A′-drug}.sub.n}.sub.m}.sub.l  (II)

In one aspect, the disclosure relates to a method for the direct synthesis of complex N,N,O-trisubstituted hydroxylamines by N—O bond formation. In another aspect, the method can successfully be employed using a wide variety of commercially available alcohols and secondary amines and enables the construction of large fragment-based libraries of trisubstituted hydroxylamines for drug discovery purposes. Also disclosed are N,N,O-trisubstituted hydroxylamines having low basicity, high stability at ambient temperatures, and an inherent lack of reactivity towards acetylating and sulfonylating enzymes that confer mutagenicity on less-substituted hydroxylamines.

Disclosed herein are methods of labeling organic compounds without depending on any functional group of the compound. In some embodiments, provided are bifunctional linkers useful in the methods.

Bis(2-haloacetamido)-compounds for use as linkers to chemically cross-linking multiple thiol groups, and particularly, although not exclusively, the thiol groups of cysteine amino acids in peptide chains are described, along with their use as linking agents and resultant products which comprise antibodies, half-antibodies and antibody fragments having thiol groups bonded to said linkers (e.g. antibody-protein conjugates and antibody-drug conjugates), and methods of making said conjugates and products. (Formula I)

##STR00001##

The present invention relates to a process for producing an organofluoro compound including [.sup.18F]fluorine, and by using a solvent represented by Formula 1 in nucleophilic fluorination reaction, an organofluoro compound may be prepared at a high yield. In addition, since the solvent has very excellent solubility for a precursor compound, the solvent is suitable for the automated synthesis of .sup.18F-labeled radiopharmaceuticals.

Certain embodiments are directed to compositions and methods for capture of elements in physical proximity. In certain aspects the methods comprise (a) contacting a target with a functionalized scaffold or capture agent that comprises activatable cross-linking moieties to form a target/scaffold mixture; (b) exposing the target/scaffold mixture to an activator to activate the cross-linking moieties of the dendrimer and form a cross-linked target/scaffold complex; (c) isolating the target/scaffold complexes; and (d) identify portions of the target or targets that are cross linked with the scaffold.

Nitrogen containing compounds may have formulas (I), (II) and (IV), and such compounds may be suitable for detecting alkyne group containing organic compounds by mass spectrometry. Furthermore, methods may also include synthesizing these compounds, detecting of organic compounds containing the specific compounds, uses of the compounds in mass spectrometry for determining enzyme activity or monitoring the lipid metabolism in a cell, and a kit which contains at least one of these compounds and at least one internal standard.

Nitrogen containing compounds may have formulas (I), (II) and (IV), and such compounds may be suitable for detecting alkyne group containing organic compounds by mass spectrometry. Furthermore, methods may also include synthesizing these compounds, detecting of organic compounds containing the specific compounds, uses of the compounds in mass spectrometry for determining enzyme activity or monitoring the lipid metabolism in a cell, and a kit which contains at least one of these compounds and at least one internal standard.

The present invention provides processes for the synthesis of organic azides, intermediates for the production thereof, and compositions related thereto.

The present invention provides processes for the synthesis of organic azides, intermediates for the production thereof, and compositions related thereto.