Hoffmann-la Roche Inc.

Max Hoffer

Emanuel Grunberg

2,2'-Anhydro-1.beta.-D-arabinofuranosyl-5-fluorocytosine (hereafter AAFC) and its acid addition salts are known compounds. AAFC may now be conveniently prepared in extremely high yield by selective acid catalyzed hydrolysis of the corresponding 3'-O-acyl analogs of AAFC which unexpectedly hydrolyzes at the acyl group while the 2,2'-anhydro linkage remains intact.

Process for preparing 2,2'-anhydro-1.beta.-D-arabi

2,4-Diamino-5-(3-alkoxy-4,5-methylenedioxybenzyl)-pyrimidines, such as, for example, 2,4-diamino-5-(3-methoxy-4,5-methylenedioxybenzyl)pyrimidine, prepared from the corresponding benzaldehydes, are described. The end products are useful as potentiators of the antibacterial activity of sulfonamides, as well as antibiotics.

Antibacterial compositions

2,4-Diamino-5-(3-alkoxy-4,5-methylenedioxybenzyl)pyrimidines, such as, for example, 2,4-diamino-5-(3-methoxy-4,5-methylenedioxybenzyl)pyrimidine, prepared from the corresponding benzaldehydes, are described. The end products are useful as potentiators of the antibacterial activity of sulfonamides, as well as antibiotics.

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Nutley, NJ, United States of America

Max Hoffer