Process for the production of o , 2'-anhydro-1-...

C - Chemistry – Metallurgy – 07 – H

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C07H 19/09 (2006.01) C07H 19/06 (2006.01) C07H 23/00 (2006.01)

Patent

CA 1315776

64680 494 PROCESS FOR THE PRODUCTION OF O2,2'- ANHYDRO-1-(.beta. -D-ARABINOFURANOSYL)THYMINE Abstract In the disclosed process, an O2,2' anhydro-1- (.beta.-D-arabinofuranosyl)thymine is formed by condensing a 2-amino-.beta.-arabinofurano¦1',2':4,5,]-2-oxazoline with a compound of the formula Image 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°C to about 150°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.

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