Quinazoline antifolate thymidylate synthase inhibitors: heterocyclic benzoyl ring modifications

  • 10.1021/jm00109a011
  • Journal of Medicinal Chemistry
  • p 1594-1605, Volume 34, Issue 5,
  • journal-article


Reproducible on smaller scale

Synthesized 2-[N-( tert -Butoxycarbonyl)amino]thiophene (25) and a similar compound (2-[N-( tert -Butoxycarbonyl)amino]-5-bromothiophene) following the same procedure described in the article as method F.

For the synthesis of 25, the reaction was scaled down 100 times, with a...