Synthesis of [3H]CI-980, ethyl[5-amino-1,2-dihydro-2(S)-methyl-3(3-[3H]phenyl)pyrido[3,4-b]pyr azin-7-yl]carbamate isethionate salt, a tubulin-binding, antimitotic, broad-spectrum antitumor agent

Article abstract of DOI:10.1002/jlcr.2580340103

[³H]CI-980 (10b) was synthesized in an eight-step sequence with an overall yield of 2.4%. Reaction of m-bromophenyl lithium (2) with N-ethoxycarbonyl-L-alanine gave the chiral ketone 3. Reduction of 3 with sodium borohydride followed by alkalin