Synthesis of 5-azacytidine-6-13C and -6-14C.
5-Azacytidine (1) labeled with 13C or 14C at the chemically labile C-6 position was synthesized. A method utilizing hydrolytic opening of the triazine ring followed by recyclization with dimethylformamide dimethyl acetal was used. Urinary and biliary excretion was measured in rabbits following intravenous doses of 1-4-14C and 1-6-14C. Differences in recoveries of the dose from 4-14C and 6-14C demonstrate that ring cleavage of 1 with loss of the C-6 carbon represents a major metabolite route.
D000818:Animals; D001374:Azacitidine / Q000138:chemical synthesis* / Q000378:metabolism / Q000652:urine; D001646:Bile / Q000378:metabolism; D002247:Carbon Isotopes; D002250:Carbon Radioisotopes; D007553:Isotope Labeling; D008297:Male; D008722:Methods; D011817:Rabbits
D002247:Carbon Isotopes; D002250:Carbon Radioisotopes; D001374:Azacitidine