Synthesis of 1‐[(2‐Hydroxyethoxy)Methyl]‐6‐(5,6,7,8‐Tetrahydronaphthylmethyl‐1)Thymine as Novel Inhibitor against Drug‐Resistant HIV Mutants

Abstract

Synthesis of two new 1‐[(2‐hydroxyethoxy)methyl]‐6‐(5,6,7,8‐tetrahydronaphthylmethyl‐1)thymine derivatives 10a–b, as potent inhibitors against a mutant type of HIV, starting from thymine, is described. In the preparation of the corresponding 10a–b from compounds 9a–b, the three‐step reaction via deprotection, hydrogenolysis, and hydrogenation was carried out in a one‐pot procedure.

Keywords:

• HEPT
• HEPT analogues
• HIV‐1 RT inhibitors