The first general synthesis of 4,6-disubstituted 5-pyrimidinesulfonamides is described. Treatment of 4,6-dichloro-5-benzylthiopyrimidine (3) with ethoxide or trifluoroethoxide, oxidation of the benzylthio group to a sulfonyl chloride and reaction with ammonia gave 4,6-dialkoxy-5-pyrimidinesulfonamides 5a,b. Stepwise displacement of the trifluoroethoxy groups in 5a gave a variety of symmetrical and non-symmetrical 4,6-disubstituted 5-pyrimidinesulfonamides 5b-h.
|Number of pages||3|
|Publication status||Published - 1 Jan 1998|