The Synthesis Of (14)～C Labeled Quinocedox And The Design Of Pharmacokinetical Experiment In Animal

Quinocedox has been studied many yesrs by our grouP, It is a novel feedadditive by clinic study.In order to efficiently study its phannacokinetic andmetabolism in animals, firStly we synthesize the isotope labeled Qulnocedox.We synthesized l4C Iabeled quinocedox. According to its scheme,at first wesynthesized intermedi ate, acetyl aceton e. It needs seven step s frOm C O2 to acety lacetone,chemical total yield is less than l0 percent,and it can not be promoted anymore by many experiments.Because radioactivity seriously reduced duringradioaCtive experiment,the scheme is useless.We had to give uP it.We began to synthesize another i ntermedi at6,benzal dehyde. It is 4 steps tosynthesize benzal dehyde frOm CO2,and we can gain Quinocedox next step.By aserial experimental ricingMe chose a corresponing scheme which is simpler andmaterial is cheaPerrtfter the failure of the fiot radioachve exPerimen We imNdthe scheme, and total yield is more than 40%.At laSt, the 8econd traced exPerindand the rdiolabeled experiment are successful.Later, we test and determined theradioactive and the radio-purity, which corresponds to the demand of the animalexperiment (the radioactive purity>96%).There are a few methods to do phannacokinetic experiment by usingradio-labeled isotope.According to the imsimment's test limitation and thepharmaceutical infOrmation, we design the pharmacokinetic method and dose inanimals.