Tetrahedron p. 393 - 400 (1998)
Update date:2022-08-25
Topics:
Li, Jun
Chen, Shu-Hui
Li, Xiuyan
Niu, Chuansheng
Doyle, Terrence W.
An efficient synthesis of potent ribonucleotide reductases inhibitors 3- amino-pyridine-2-carboxaldehyde thiosemicarbazone (3-AP) end 3-amino-4- methyl-pyridine-2-carboxaldehyde thiosemicarbazone (3-AMP) is described. The synthesis of 3-AP and 3-AMP was achieved in 4 and 5 steps, with overall yields of 61% and 39%, respectively. The synthesis featured a convergent approach utilizing a Stille coupling strategy to prepare vinylpyridine derivatives. A more economic way to synthesize vinylpyridine using Heck reaction was also discussed.
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