Disclosed are methods for preparing 2-alkynyladenosine derivatives of
formula A:
or a stereoisomer, pharmaceutically acceptable salt, hydrate, solvate,
acid salt hydrate or isomorphic crystalline form thereof, the method
comprising the step of: contacting 2-iodoadenosine-5'-N-ethyluronamide
with a compound of formula B:
wherein Z is --C(.dbd.O)OR or --CH.sub.2C(.dbd.O)R, where R is a
C.sub.1 to C.sub.5 alkyl, preferably
The methods are useful for preparing 2-alkynyladenosine derivatives that
are, in certain embodiments, adenosine receptor agonists.