Tetrahedron

Efficient synthesis of ribonucleotide reductase inhibitors 3-aminopyridine-2-carboxaldehyde thiosemicarbazone (3-AP) and 3-amino-4-methylpyridine-2- …

J Li, SH Chen, X Li, C Niu, TW Doyle

Index: Li, Jun; Chen, Shu-Hui; Li, Xiuyan; Niu, Chuansheng; Doyle, Terrence W. Tetrahedron, 1998 , vol. 54, # 3-4 p. 393 - 400

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Citation Number: 24

Abstract

An efficient synthesis of potent ribonucleotide reductases inhibitors 3-amino-pyridine-2- carboxaldehyde thiosemicarbazone (3-AP) and 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 ...