The present invention provides modified cycloalkyne compounds; and method of use of such compounds in modifying biomolecules. The present invention features a cycloaddition reaction that can be carried out under physiological conditions. In general, the invention involves reacting a modified cycloalkyne with an azide moiety on a target biomolecule, generating a covalently modified biomolecule. The selectivity of the reaction and its compatibility with aqueous environments provide for its application in vivo (e.g., on the cell surface or intracellularly) and in vitro (e.g., synthesis of peptides and other polymers, production of modified (e.g., labeled) amino acids).

The present invention provides modified cycloalkyne compounds; and method of use of such compounds in modifying biomolecules. The present invention features a cycloaddition reaction that can be carried out under physiological conditions. In general, the invention involves reacting a modified cycloalkyne with an azide moiety on a target biomolecule, generating a covalently modified biomolecule. The selectivity of the reaction and its compatibility with aqueous environments provide for its application in vivo (e.g., on the cell surface or intracellularly) and in vitro (e.g., synthesis of peptides and other polymers, production of modified (e.g., labeled) amino acids).

Compounds of formula I ##STR00001##
a process for preparation of compounds of formula I; precursor compounds of formula II ##STR00002##
a process for preparation of precursor compounds of formula II; compounds of formula III ##STR00003##
a process for the preparation of compounds of formula IV from compounds of formula III ##STR00004##
and the use of compounds of formula I for the preparation of compounds of formula IV.

Compounds of formula I ##STR00001##
a process for preparation of compounds of formula I; precursor compounds of formula II ##STR00002##
a process for preparation of precursor compounds of formula II; compounds of formula III ##STR00003##
a process for the preparation of compounds of formula IV from compounds of formula III ##STR00004##
and the use of compounds of formula I for the preparation of compounds of formula IV.

Compounds of formula I

##STR00001##

a process for preparation of compounds of formula I; precursor compounds of formula II

##STR00002##

a process for preparation of precursor compounds of formula II; compounds of formula III

##STR00003##

a process for the preparation of compounds of formula IV from compounds of formula III

##STR00004##

and the use of compounds of formula I for the preparation of compounds of formula IV.

Compounds of formula I

##STR00001##

a process for preparation of compounds of formula I; precursor compounds of formula II

##STR00002##

a process for preparation of precursor compounds of formula II; compounds of formula III

##STR00003##

a process for the preparation of compounds of formula IV from compounds of formula III

##STR00004##

and the use of compounds of formula I for the preparation of compounds of formula IV.

The present invention provides modified cycloalkyne compounds; and method of use of such compounds in modifying biomolecules. The present invention features a cycloaddition reaction that can be carried out under physiological conditions. In general, the invention involves reacting a modified cycloalkyne with an azide moiety on a target biomolecule, generating a covalently modified biomolecule. The selectivity of the reaction and its compatibility with aqueous environments provide for its application in vivo (e.g., on the cell surface or intracellularly) and in vitro (e.g., synthesis of peptides and other polymers, production of modified (e.g., labeled) amino acids).

The present invention provides modified cycloalkyne compounds; and method of use of such compounds in modifying biomolecules. The present invention features a cycloaddition reaction that can be carried out under physiological conditions. In general, the invention involves reacting a modified cycloalkyne with an azide moiety on a target biomolecule, generating a covalently modified biomolecule. The selectivity of the reaction and its compatibility with aqueous environments provide for its application in vivo (e.g., on the cell surface or intracellularly) and in vitro (e.g., synthesis of peptides and other polymers, production of modified (e.g., labeled) amino acids).

The invention provides compounds of formulae I, II, III, and IV: ##STR00001##
and salts thereof, as well as pharmaceutical compositions comprising such compounds. The compounds are useful for treating cancers and Alzheimer's disease.

The present invention provides modified cycloalkyne compounds; and method of use of such compounds in modifying biomolecules. The present invention features a cycloaddition reaction that can be carried out under physiological conditions. In general, the invention involves reacting a modified cycloalkyne with an azide moiety on a target biomolecule, generating a covalently modified biomolecule. The selectivity of the reaction and its compatibility with aqueous environments provide for its application in vivo (e.g., on the cell surface or intracellularly) and in vitro (e.g., synthesis of peptides and other polymers, production of modified (e.g., labeled) amino acids).