Simple entry to 3'-substituted analogues of anti-HIV agent stavudine based on an anionic O --> C stannyl migration

J Org Chem. 2002 May 31;67(11):3541-7. doi: 10.1021/jo0107958.

Abstract

Reaction of 5'-O-protected derivatives of the anti-HIV agent stavudine (d4T) with LTMP was investigated with the aim to lithiate the vinylic hydrogens (H-3' and H-2'). When the lithiation of the 5'-O-tert-butyldiphenylsilyl derivative 5 was carried out in the presence of HMPA, an anionic silyl migration took place to give the 3'-C-silylated product 4a. The stannyl version of this reaction was found to be also possible, which has disclosed a highly simple entry to the d4T analogues variously substituted at the 3'-position by manipulating the 3'-C-stannyl d4T as a common intermediate.

MeSH terms

  • Anions
  • Anti-HIV Agents / chemical synthesis*
  • Lithium / chemistry
  • Stavudine / analogs & derivatives*
  • Stavudine / chemical synthesis
  • Vinyl Compounds / chemistry

Substances

  • Anions
  • Anti-HIV Agents
  • Vinyl Compounds
  • Lithium
  • Stavudine