Process for the production of 02,2'-anhydro-1-(beta-D-arabinofuranosyl)thymine.

摘要

In the disclosed process, an O<2>,2 min anhydro-1-( beta -D-arabinofuranosyl)thymine is formed by condensing a 2-amino- beta -arabinofurano[1 min ,2 min :4,5,]-2-oxazoline with a compound of the formula wherein R1 is C1-C4 alkyl; X is halogen or OR2, wherein R2 is H, C1-C4 alkyl or phenyl; in the presence of a suitable solvent at about 0 DEG C to about 150 DEG C. Catalytic agents such as dimethylaminopyridine and triethylamine may also be added to accelerate the reaction. Protected intermediates of the anhydronucleosides and aminooxazolines are also disclosed.