Synthesis of [5-methyl-H-3]-nitrendipine by means of a new method was
described. Methyl-[H-3]methanol was reacted with diketene forming meth
yl-[H-3]acetoacetate, followed by treatment with ammonia to give [meth
yl-H-3]-3-aminoacrotonate, which was reacted with methyl 2-[(3-nitroph
enyl)-3-methylene]-3-oxobutanoate to synthesize [5-methyl-H-3]-nitrend
ipine. Its specific activity and radiochemical purify were 23 Ci/mmol
and >98%, respectively.