Disclosed are methods for preparing 2-alkynyladenosine derivatives of
formula A: ##STR00001## 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:
##STR00002## 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.