Disclosed are novel conjugates and processes for the preparation thereof. A process for the preparation of alkene- or alkyne-phosphonamidates comprises the steps of (I) reacting a compound of formula (III) ##STR00001## with an azide of formula (IV) ##STR00002## to prepare a compound of formula (V) ##STR00003## (II) reacting a compound of formula (V) with a thiol-containing molecule of formula (VI) ##STR00004## resulting in a compound of formula (VII) ##STR00005##

Amine substituted morpholino oligonucleotides, other than the classical N,N-dimethylamino PMO analogue, and methods of efficiently synthesizing these oligonucleotides with high yield are provided. Morpholino oligonucleotides having thiophosphoramidate, phosphoramidate, and alkyl phosphoramidate linkers. Chimeras containing unmodified DNA/RNA and other analogs of DNA/RNA can be prepared. These oligonucleotides form duplexes with complementary DNA or RNA that are more stable than natural DNA or DNA/RNA complexes, are active with RNAse H1, and may be transfected into cells using standard lipid reagents. These analogues are therefore useful for numerous applications.

Disclosed are novel conjugates and processes for the preparation thereof. A process for the preparation of alkene- or alkyne-phosphonamidates comprises the steps of (I) reacting a compound of formula (III)

##STR00001## with an azide of formula (IV)

##STR00002## to prepare a compound of formula (V)

##STR00003## (II) reacting a compound of formula (V) with a thiol-containing molecule of formula (VI)

##STR00004## resulting in a compound of formula (VII)

##STR00005##